Search Result

Results for "

phosphorylation inhibition

" in MedChemExpress (MCE) Product Catalog:

By Targets:	DYRK (1) Oxidative Phosphorylation (3) Akt (3) Anaplastic lymphoma kinase (ALK) (7) Apoptosis (9) ATM/ATR (1) Autophagy (5) c-Kit (1) c-Met/HGFR (7) CaMK (1) Casein Kinase (1) Caspase (1) CDK (1) CMV (1) EGFR (3) Endogenous Metabolite (2) ERK (1) FLT3 (1) HDAC (1) HIV (1) HSP (1) HSV (1) Influenza Virus (1) Interleukin Related (2) Isotope-Labeled Compounds (1) JAK (1) Ketohexokinase (1) MEK (1) Microtubule/Tubulin (1) Mitochondrial Metabolism (2) Molecular Glues (1) mTOR (1) NF-κB (2) NOD-like Receptor (NLR) (1) p38 MAPK (1) PDGFR (1) PI3K (3) PKA (2) PKC (2) Polo-like Kinase (PLK) (2) Proteasome (1) Raf (1) ROS Kinase (6) STAT (3) TAM Receptor (1) TGF-β Receptor (2) Tie (1) Trk Receptor (1) ULK (1) VSV (1) YB-1 (1)
By Research Areas:	Cancer (36) Cardiovascular Disease (6) Infection (1) Inflammation/Immunology (7) Metabolic Disease (2)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: Oxidative Phosphorylation DYRK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-150095

YE6144	Others	Inflammation/Immunology
YE6144 is a prototypical interferon regulatory factor 5 (IRF5) inhibitor. YE6144 selectively suppresses IRF5 activity through inhibition of IRF5 phosphorylation .

HY-P1115

AKTide-2T	Akt	Others
AKTide-2T is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a K_i of 12 nM. AKTide-2T mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position .

HY-P1115A

AKTide-2T TFA	Akt	Others
AKTide-2T TFA is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a K_i of 12 nM. AKTide-2T TFA mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position .

HY-158421

MS-L6	Oxidative Phosphorylation Mitochondrial Metabolism	Cancer
MS-L6 is a potent inhibitor of oxidative phosphorylation (OXPHOS) that can acts as electron transport chain complexes I (ETC-I) combining inhibition of NADH oxidation and uncoupling effect .

HY-145304

DX3-235	Oxidative Phosphorylation Mitochondrial Metabolism	Cancer
DX3-235 is an oxidative phosphorylation (OXPHOS) inhibitor. DX3-235 shows nanomolar inhibition of complex I function and ATP production in a galactose-containing medium resulting in significant cytotoxicity .

HY-12960

SKLB4771 FLT3-IN-1	FLT3 c-Kit Apoptosis	Cancer
SKLB4771 is a potent and selective Flt3 inhibitor with an IC₅₀ value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue .

HY-50878

Crizotinib Maximum Cited Publications 62 Publications Verification PF-02341066	Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy	Cancer
Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .

HY-50878B

Crizotinib acetate PF-02341066 acetate	Anaplastic lymphoma kinase (ALK) ROS Kinase c-Met/HGFR	Cancer
Crizotinib (PF-02341066) acetate is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib acetate inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. Crizotinib acetate is also a ROS1 inhibitor. Crizotinib acetate has effective tumor growth inhibition .

HY-150561

Trk-IN-20	Trk Receptor	Cancer
Trk-IN-20 is a kind of 3-vinylindazole derivatives. Trk-IN-20 suppresses Trk kinases functions by phosphorylation inhibition of TrkA/B/C with IC₅₀ values of 1.6 nM, 2.9 nM and 2.0 nM, respectively .

HY-118528

TP0427736	TGF-β Receptor	Cancer
TP0427736 is a selective inhibitor of ALK5 with an IC₅₀ of 2.72 nM. TP0427736 inhibits Smad2/3 phosphorylation in A549 cells. TP0427736 decreases the growth inhibition of human outer root sheath cells .

HY-149987

LY3522348 KHK-IN-3	Ketohexokinase	Cardiovascular Disease Metabolic Disease Inflammation/Immunology
KHK-IN-3 (Example 1) is a ketohexokinase (KHK) inhibitor. KHK-IN-3 can be used in the study of kidney disease, nonalcoholic steatohepatitis (NASH), diabetes and heart failure. KHK is a rate-limiting enzyme and fructokinase involved in fructose metabolism. KHK catalyzes the phosphorylation of fructose to fructose-1-phosphate (FIP) at the expense of ATP. The lack of feedback inhibition of fructose metabolism triggers the accumulation of downstream intermediates such as lipogenesis, gluconeogenesis, and oxidative phosphorylation .

HY-112391

SD-1029	JAK STAT	Cancer
SD-1029 is a JAK2/STAT3 inhibitor . SD-1029 inhibits STAT3 nuclear translocation. SD-1029 is an inhibitor of STAT3 activation due to inhibition of JAK2 phosphorylation .

HY-15614

SC144 5 Publications Verification	Interleukin Related Apoptosis	Cancer
SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells .

HY-15614A

SC144 hydrochloride 5 Publications Verification	Interleukin Related Apoptosis	Cancer
SC144 hydrochloride is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 hydrochloride binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 hydrochloride shows potent inhibition of gp130 ligand-triggered signaling. SC144 hydrochloride induces apoptosis in human ovarian cancer cells .

HY-50878S

Crizotinib-d5 PF-02341066-d₅	Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy	Cancer
Crizotinib-d₅ is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .

HY-N1956

Rubiadin-1-methyl ether	NF-κB	Metabolic Disease
Rubiadin-1-methyl ether is a natural anthraquinone isolated from Morinda officinalis How, and inhibits osteoclastic bone resorption via inhibition on the phosphorylation of NF-κB p65 and the degradation of IκBα as well as decrease in the nuclear translocation of p65 .

HY-145072

BSJ-01-175	CDK	Cancer
BSJ-01-175 is a potent and selective CDK12/13 covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells .

HY-15838

ID-8 4 Publications Verification	DYRK	Cancer
ID-8 is an inhibitor of *dual-specificity tyrosine phosphorylation-regulated kinase (DYRK). ID-8 sustains embryonic stem cell (ESC) self-renewal and pluripotency. ID-8 enhances Wnt-mediated hESC survival and proliferation via inhibition* of DYRKs .

HY-147566

ATR-IN-14	ATM/ATR	Cancer
ATR-IN-14 (compound 1) is a potent ATR kinase inhibitor. ATR-IN-14 inhibits ATR signaling pathways downstream CHKI protein phosphorylation, with inhibition of 98.03% at 25 nM. ATR-IN-14 shows good anticancer activity in LoVo cells, with an IC₅₀ of 64 nM .

HY-50878A

Crizotinib hydrochloride Maximum Cited Publications 62 Publications Verification PF-02341066 hydrochloride	Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy	Cancer
Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .

HY-50878R

Crizotinib (Standard)	Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy	Cancer
Crizotinib (Standard) is the analytical standard of Crizotinib. This product is intended for research and analytical applications. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .

HY-137506

XST-14 1 Publications Verification	ULK p38 MAPK TGF-β Receptor Anaplastic lymphoma kinase (ALK) CaMK Apoptosis	Cancer
XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC₅₀ of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects .

HY-P10462

SAP15 Synthetic anti-inflammatory peptide 15	HDAC NF-κB	Inflammation/Immunology
SAP15 (Synthetic anti-inflammatory peptide 15) is a synthetic anti-inflammatory peptide consisting of 15 amino acids designed from human beta-defensin 3. SAP15 has the ability to penetrate cells and is able to induce downregulation of intracellular inflammation. SAP15 inhibits inflammation by inhibiting the phosphorylation of HDAC5 and thereby reducing the phosphorylation of NF-κB p65. In LPS-induced macrophages, SAP15 inhibits HDAC5 and NF-κB p65 phosphorylation. In addition, SAP15 treatment increased the expression of aggrecan and type II collagen and decreased the expression of osteocalcin in LPS-induced chondrocytes. SAP15 can be used in the study of inflammation regulation and anti-inflammatory therapy of biomaterials .

HY-149292

SR-4133	Casein Kinase	Cancer
SR-4133 is a potent and highly CK1ε selective inhibitor with an IC₅₀ of 58 nM. SR-4133 binds to the ATP-binding site of CK1ε. SR-4133 displays nanomolar growth inhibition of bladder cancer cells, and inhibits the phosphorylation of 4E-BP1 .

HY-50878AS

Crizotinib-d9 hydrochloride PF-02341066-d₉ hydrochloride	c-Met/HGFR Autophagy Anaplastic lymphoma kinase (ALK) ROS Kinase Isotope-Labeled Compounds	Cancer
Crizotinib-d₉ hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .

HY-15798

UNC2881	VSV TAM Receptor	Cardiovascular Disease
UNC2881 is an orally active and specific Mer kinase inhibitor, inhibits steady-state Mer kinase phosphorylation with an IC₅₀ value of 22 nM. UNC2881 shows additional inhibition against Axl and Tyro with IC₅₀s of 360 nM and 250 nM, respectively. UNC2881 potently inhibits collagen-induced platelet aggregation, can be used for pathologic thrombosis research .

HY-114302

CCB02	Microtubule/Tubulin	Cancer
CCB02 is a selective CPAP-tubulin interaction inhibitor, binding to tubulin and competing for the CPAP binding site of β-tubulin, with an IC₅₀ of 689 nM, and shows potent anti-tumor activity. CCB02 shows no inhibition on the cell cycle- and centrosome-related kinases, or the phosphorylation status of Aurora A, Plk1, Plk2, CDK2, and CHK1 .

HY-P1597

Malantide	PKA PKC	Cancer
Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a K_m of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide is also an efficient substrate for PKC with a K_m of 16 μM .

HY-N7056

4'-Hydroxychalcone	Oxidative Phosphorylation Proteasome	Inflammation/Immunology Cancer
4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria .

HY-12037A

Rigosertib 5 Publications Verification ON-01910	Polo-like Kinase (PLK) PI3K Apoptosis	Cancer
Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC₅₀ of 9 nM .

HY-P1597A

Malantide TFA	PKA PKC	Cancer
Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a K_m of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide TFA is also an efficient substrate for PKC with a K_m of 16 μM .

HY-122920

Soyasaponin II	HSV CMV Influenza Virus HIV NOD-like Receptor (NLR) YB-1	Infection Inflammation/Immunology
Soyasaponin II is a saponin with antiviral activity. Soyasaponin II inhibits the replication of HSV-1, HCMV, influenza virus, and HIV-1. Soyasaponin II shows potent inhibition on HSV-1 replication. Soyasaponin II serves as a inhibitor for YB-1 phosphorylation and NLRP3 inflammasome priming and could protect mice against LPS/GalN induced acute liver failure .

HY-12037

Rigosertib sodium 5 Publications Verification ON-01910 sodium	Polo-like Kinase (PLK) PI3K Apoptosis	Cancer
Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC₅₀ of 9 nM .

HY-155156

PF-07238025	Endogenous Metabolite	Cardiovascular Disease
PF-07238025 is a BCKDC kinase (BDK) inhibitor (EC₅₀=19 nM). PF-07238025 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07238025 improved cardiometabolic endpoints and improves glucose tolerance in mice .

HY-155157

PF-07247685	Endogenous Metabolite	Cardiovascular Disease
PF-07247685 is a BCKDC kinase (BDK) inhibitor (EC₅₀=2.2 nM). PF-07247685 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07247685 improved cardiometabolic endpoints and improves glucose tolerance in mice .

HY-160496

STAT3-IN-25	STAT	Cancer
STAT3-IN-25 (compound 4c) is an orally active, potent STAT3 dual phosphorylation inhibitor with an indole-containing tetra-aromatic heterocycle scaffold. STAT3-IN-25 has luciferase activities IC₅₀ of 5.3 nM and ATP inhibition IC₅₀ of 4.2 nM.STAT3-IN-25 significantly blocks p-Tyr705 and p-Ser727 and causes the abrogation of the corresponding nuclear transcription and mitochondrial oxidative phosphorylation functions of STAT3 in the low nanomolar range by targeting the STAT3 SH2 domain (K_D=21.3 nM). STAT3-IN-25 exhibits significant suppressive effects in a pancreatic cancer xenograft model .

HY-N2484

Methylnissolin Astrapterocarpan	PDGFR ERK	Cardiovascular Disease
Methylnissolin (Astrapterocarpan), isolated from Astragalus membranaceus, inhibits platelet-derived growth factor (PDGF)-BB-induced cell proliferation with an IC₅₀ of 10 μM. Methylnissolin inhibits PDGF-BB-induced phosphorylation of extracellular signal-regulated kinase 1/2 (ERIC1/2) mitogen-activated protein (MAP) kinase. Methylnissolin inhibits PDGF-BB-induced vascular smooth muscle cell proliferation by inhibition of the ERK1/2 MAP kinase cascade .

HY-158115

NST-628	Molecular Glues Raf MEK	Cancer
NST-628 is a brain-permeable MAPK pathway molecule glue that inhibits RAF phosphorylation and MEK activation. NST-628 also binds RAF and prevents the formation of BRAF-CRAF and BRAF-ARAF heterodimers, effectively inhibiting the RAS-MAPK pathway. NST-628 inhibits RAS- and RAF-driven cancers and demonstrated potent inhibition in mutant KRAS, NRAS, BRAF class II/III, and NF1-mutant tumors .

HY-158178

EGFR T790M/L858R-IN-7	EGFR	Cancer
EGFR T790M/L858R-IN-7 (Compound 72) is a novel pyrimidine compound that inhibits the EGFR T790M and L858R mutation with a high efficacy (93% inhibition rate at 0.05 μM). EGFR T790M/L858R-IN-7 functions by specifically binding to the kinase domain of EGFR, thereby inhibiting its phosphorylation activity .

HY-129510

4-Methyl erlotinib	EGFR	Cancer
4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .

HY-111553

TAS0728	EGFR	Cancer
TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, with an IC₅₀ of 13 nM. TAS0728 also shows IC₅₀s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for BMX、HER4、BLK、EGFR、JAK3、SLK and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2HER3, and downstream effectors .

HY-132168

RMC-5552 1 Publications Verification	mTOR	Cancer
RMC-5552 is a potent and selective mTORC1 inhibitor. RMC-5552 inhibits phosphorylation of mTORC1 pS6K and p4EBP1 with IC₅₀s of 0.14 nM and 0.48 nM, respectively. RMC-5552 shows much lower pAKT inhibition (IC₅₀ of 19 nM), resulting in mTORC1/mTORC2 selectivity approaching 40-fold. RMC-5552 has anti-cancer activity .

HY-145102

NCT-58	HSP Apoptosis	Cancer
NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells .

HY-160708

Tie2 kinase inhibitor 3	Tie	Cancer
Tie2 kinase inhibitor 3 (compound 63) is a potent Tie-2 kinase inhibitor with good oral activity (IC₅₀=30 nM). Tie2 kinase inhibitor 3 inhibits phosphorylation and signaling of Tie-2 by competing with the ATP binding site of Tie-2 kinase. This inhibition affects the stability and maturity of blood vessels, which has an impact on tumor angiogenesis. Tie2 kinase inhibitor 3 can be used to restrict tumor growth and regulate angiogenesis .

HY-124843

LLL3 CLT-005	STAT Apoptosis	Cancer
LLL3 (CLT-005) is a STAT3 inhibitor. LLL3 inhibits dimerization and phosphorylation of STAT3, thereby preventing intraconuclear transfer of STAT3 and inhibits the expression of STAT3 dependent genes, which encode proteins such as Bcl-xL and cyclin D1. In addition, LLL3 can induce cell growth inhibition and apoptosis in human breast cancer and rhabdomyosarcoma cells via the caspase pathway. LLL3 can be used in the study of STAT3 persistent activation types of cancer .

HY-18696

AMG-337	c-Met/HGFR Caspase Apoptosis	Cancer
AMG-337 is a potent, orally active, selective MET kinase inhibitor with IC₅₀ values of 1, 1, 4.7, 5, 21.5, 1077 and >4000 nM of WT MET, H1094R MET, M1250T MET, HGF-stimulated pMET (PC3 cells) MET, V1092I MET, Y1230H MET, and D1228H MET, respectively. AMG 337 inhibits the phosphorylation of MET and downstream effectors in MET-amplified cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis .

HY-144450

PI3K-IN-29	PI3K Akt	Cancer
PI3K-IN-29 is a potent PI3K inhibitor. PI3K-IN-29 displays good inhibition potencies against U87MG, HeLa and HL60 cells with IC₅₀ values of 0.264, 2.04 and 1.14 µM, respectively. PI3K-IN-29 inhibits PI3K/Akt pathway by inhibiting phosphorylation of Akt that is catalyzed by PI3K .

Cat. No.	Product Name	Target	Research Area

HY-P1597

Malantide	PKA PKC	Cancer
Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a K_m of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide is also an efficient substrate for PKC with a K_m of 16 μM .

HY-P1115A

AKTide-2T TFA	Akt	Others
AKTide-2T TFA is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a K_i of 12 nM. AKTide-2T TFA mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position .

HY-P10346

smMLCK peptide Smooth-Muscle Myosin Light-Chain Kinase (796-815)	Peptides	Cardiovascular Disease Inflammation/Immunology
smMLCK peptide is a specific inhibitor of smooth muscle myosin light chain kinase (smMLCK). The smMLCK peptide mimics the substrate and competitively inhibits the binding of the actual substrate to the enzyme, thereby inhibiting the kinase activity. This inhibition prevents the phosphorylation of the myosin light chain, thus inhibiting muscle contraction .

HY-P10462

SAP15 Synthetic anti-inflammatory peptide 15	HDAC NF-κB	Inflammation/Immunology
SAP15 (Synthetic anti-inflammatory peptide 15) is a synthetic anti-inflammatory peptide consisting of 15 amino acids designed from human beta-defensin 3. SAP15 has the ability to penetrate cells and is able to induce downregulation of intracellular inflammation. SAP15 inhibits inflammation by inhibiting the phosphorylation of HDAC5 and thereby reducing the phosphorylation of NF-κB p65. In LPS-induced macrophages, SAP15 inhibits HDAC5 and NF-κB p65 phosphorylation. In addition, SAP15 treatment increased the expression of aggrecan and type II collagen and decreased the expression of osteocalcin in LPS-induced chondrocytes. SAP15 can be used in the study of inflammation regulation and anti-inflammatory therapy of biomaterials .

HY-P1834

MARCKS Peptide(151-175), Phosphorylated	Peptides	Inflammation/Immunology
MARCKS Peptide(151-175), Phosphorylated is a phosphorylated peptide corresponding to the basic effector domain of myristoylated alanine-rich protein kinase C substrate protein (MARCKS). Phosphorylation of MARCKS Peptide (151-175) reverses its inhibition of phospholipase C (PLC)-catalyzed hydrolysis of phosphatidylinositol 4,5-bisphosphate (PIP2) .

HY-P1597A

Malantide TFA	PKA PKC	Cancer
Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a K_m of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts . Malantide TFA is also an efficient substrate for PKC with a K_m of 16 μM .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N1956

Rubiadin-1-methyl ether	Quinones Structural Classification Monophenols Classification of Application Fields Anthraquinones Source classification Rubiaceae Phenols Metabolic Disease Plants Disease Research Fields Rubia cordifolia L.	NF-κB
Rubiadin-1-methyl ether is a natural anthraquinone isolated from Morinda officinalis How, and inhibits osteoclastic bone resorption via inhibition on the phosphorylation of NF-κB p65 and the degradation of IκBα as well as decrease in the nuclear translocation of p65 .

HY-N7056

4'-Hydroxychalcone	Structural Classification Classification of Application Fields Source classification Plants Endogenous metabolite Chalcones Monophenols Flavonoids Leguminosae Phenols Inflammation/Immunology Disease Research Fields Glycyrrhiza uralensis Fisch.	Oxidative Phosphorylation Proteasome
4'-Hydroxychalcone is a chalcone isolated from licorice root, with hepatoprotective activity. 4'-Hydroxychalcone inhibits TNFα-induced NF-κB activation via proteasome inhibition. 4'-Hydroxychalcone induces a rapid potassium release from mitochondrial vesicles and causes deterioration of respiratory control and oxidative phosphorylation of isolated rat liver mitochondria .

HY-122920

Soyasaponin II	Triterpenes Structural Classification Classification of Application Fields Leguminosae Terpenoids Source classification Plants Inflammation/Immunology Disease Research Fields Glycine soja Sieb. Et Zucc.	HSV CMV Influenza Virus HIV NOD-like Receptor (NLR) YB-1
Soyasaponin II is a saponin with antiviral activity. Soyasaponin II inhibits the replication of HSV-1, HCMV, influenza virus, and HIV-1. Soyasaponin II shows potent inhibition on HSV-1 replication. Soyasaponin II serves as a inhibitor for YB-1 phosphorylation and NLRP3 inflammasome priming and could protect mice against LPS/GalN induced acute liver failure .

HY-155156

PF-07238025	Cardiovascular Disease Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Source classification Endogenous metabolite Disease Research Fields	Endogenous Metabolite
PF-07238025 is a BCKDC kinase (BDK) inhibitor (EC₅₀=19 nM). PF-07238025 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07238025 improved cardiometabolic endpoints and improves glucose tolerance in mice .

HY-N2484

Methylnissolin Astrapterocarpan	Cardiovascular Disease Monophenols Flavonoids Classification of Application Fields Leguminosae Source classification Phenols Astragalus membranaceus var. mongholicus (Bunge)P.K.Hsiao Plants Other Flavonoids Disease Research Fields	PDGFR ERK
Methylnissolin (Astrapterocarpan), isolated from Astragalus membranaceus, inhibits platelet-derived growth factor (PDGF)-BB-induced cell proliferation with an IC₅₀ of 10 μM. Methylnissolin inhibits PDGF-BB-induced phosphorylation of extracellular signal-regulated kinase 1/2 (ERIC1/2) mitogen-activated protein (MAP) kinase. Methylnissolin inhibits PDGF-BB-induced vascular smooth muscle cell proliferation by inhibition of the ERK1/2 MAP kinase cascade .

Cat. No.	Product Name	Chemical Structure

HY-50878S

Crizotinib-d5

Crizotinib-d₅ is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .

HY-50878AS

Crizotinib-d9 hydrochloride

Crizotinib-d₉ hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks