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Results for "

small-molecule blocker

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adenosine Receptor (1) Amyloid-β (1) Apoptosis (2) Bacterial (1) BCL6 (1) Complement System (2) DNA/RNA Synthesis (1) EBV (1) EGFR (1) MDM-2/p53 (1) PCSK9 (1) PD-1/PD-L1 (6) Ras (1) Sodium Channel (4) TNF Receptor (1) TRP Channel (1) Wnt (1)
By Research Areas:	Cancer (17) Cardiovascular Disease (1) Infection (1) Inflammation/Immunology (7) Metabolic Disease (1) Neurological Disease (3)

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Biochemical Assay Reagents

Inhibitory Antibodies

Targets Recommended: Small Interfering RNA (siRNA) ALCAM/CD166

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-128342

Complement C5-IN-1	Complement System	Inflammation/Immunology
Complement C5-IN-1 (Compound 7) is a small-molecule inhibitor of complement component 5 protein (C5). Complement C5-IN-1 interacts with C5 to prevent its cleavage by the C5 convertase and blocks zymosan-induced the membrane-attack complex (MAC) deposition in 50% human whole blood with an IC₅₀ of 0.77 µM .

HY-117930

Danicopan 3 Publications Verification ACH-4471	Complement System	Inflammation/Immunology
Danicopan (ACH-4471), a selective and orally active small-molecule factor D inhibitor, shows high binding affinity to human Factor D with K_d value of 0.54 nM. Danicopan (ACH-4471) inhibits alternative pathway of complement (APC) activity, has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS) .

HY-W584512

Thalidomide-NH-CH2-COO(t-Bu)

Others Others

Thalidomide-NH-CH2-COO (t-Bu) is a molecular block of small-molecule degrader .

Thalidomide-NH-CH2-COO(t-Bu)	Others	Others
Thalidomide-NH-CH2-COO (t-Bu) is a molecular block of small-molecule degrader .

HY-145768

PD-1/PD-L1-IN-18	PD-1/PD-L1	Cancer
PD-1/PD-L1-IN-18 (Compound L31) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-18 blocks PD-1/PD-L1 with the IC₅₀ of 1.054 μM. Antitumor Activity .

HY-147306

ZLc-002	Others	Neurological Disease
ZLc-002 is a selective inhibitor of nNOS-Capon coupling. ZLc-002 suppresses inflammatory nociception and chemotherapy-induced neuropathic pain. ZLc-002 can be used for the research of anxiety disorder and inflammation .

HY-119053

MS7972

MDM-2/p53 Cancer

MS7972 is a small molecule that blocks human p53 and CREB binding protein association. MS7972 can almost completely block this BRD interaction at 50 μM .

MS7972	MDM-2/p53	Cancer
MS7972 is a small molecule that blocks human p53 and CREB binding protein association. MS7972 can almost completely block this BRD interaction at 50 μM .

HY-145770

PD-1/PD-L1-IN-19	PD-1/PD-L1	Cancer
PD-1/PD-L1-IN-19 (Example 22) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-19 blocks PD-1/PD-L1 with the IC₅₀ of 62.3 nM. PD-1/PD-L1-IN-19 can be used for the research of cancers, infectious diseases and autoimmune diseases .

HY-145771

PD-1/PD-L1-IN-20	PD-1/PD-L1	Cancer
PD-1/PD-L1-IN-20 (Example 21) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-20 blocks PD-1/PD-L1 with the IC₅₀ of 5.29 nM. PD-1/PD-L1-IN-20 can be used for the research of cancers, infectious diseases and autoimmune diseases .

HY-12796

Raxatrigine Vixotrigine; GSK-1014802; CNV1014802	Sodium Channel	Neurological Disease
Raxatrigine (GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.

HY-12796A

Raxatrigine hydrochloride Vixotrigine hydrochloride; GSK-1014802 hydrochloride; CNV1014802 hydrochloride	Sodium Channel	Neurological Disease
Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.

HY-145772

PD-1/PD-L1-IN-21	PD-1/PD-L1	Cancer
PD-1/PD-L1-IN-21 (Example 22) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-21 blocks PD-1/PD-L1 with the IC₅₀ of 4.99 μM. PD-1/PD-L1-IN-21 can be used for the research of cancers, infectious diseases and autoimmune diseases .

HY-145773

PD-1/PD-L1-IN-22	PD-1/PD-L1	Cancer
PD-1/PD-L1-IN-22 (Example 2) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-22 blocks PD-1/PD-L1 with the IC₅₀ of 0.732 μM. PD-1/PD-L1-IN-22 can be used for the research of cancers, infectious diseases and autoimmune diseases .

HY-157122

VJDT

Others Cancer

VJDT is a TREM1 small molecule inhibitor that effectively blocks TREM1 signaling. VJDT inhibits tumor growth and can be used in cancer research .

VJDT	Others	Cancer
VJDT is a TREM1 small molecule inhibitor that effectively blocks TREM1 signaling. VJDT inhibits tumor growth and can be used in cancer research .

HY-126005

VGSC blocker-1	Sodium Channel	Cancer
VGSC blocker-1 is a potent and small molecule blocker of neonatal isoform of the VGSC subtype, Nav1.5 (nNav1.5). VGSC blocker-1 blocks INa peak currents 34.9% at 1 μM and inhibits cell invasion 0.3% at 1 μM in human breast cancer cell line MDA-MB-231, without affecting the cell viability .

HY-16009B

Buntanetap L-Tartrate (+)-Phenserine L-Tartrate; ANVS401 L-Tartrate	Amyloid-β	Cancer
Buntanetap (L-Tartrate) is an orally administered small molecule inhibitor of several neurotoxic proteins. Buntanetap reduces amyloid precursor protein (APP) production by blocking its mRNA translation .

HY-118922

IW927	TNF Receptor	Inflammation/Immunology
IW927 is a potent small molecule antagonist that blocks the binding of TNF-α to TNFRc1 with an IC₅₀ value of 50 nM and disrupts TNFα-induced IκB phosphorylation with an IC₅₀ value of 600 nM .

HY-120836

AOH1160	DNA/RNA Synthesis Apoptosis	Cancer
AOH1160 is a potent oral small molecule proliferating cell nuclear antigen (PCNA) inhibitor that interferes with DNA replication, blocks homologous recombination-mediated DNA repair, leads to cell cycle arrest and induces apoptosis .

HY-163534

PD-1/PD-L1-IN-43	PD-1/PD-L1	Cancer
PD-1/PD-L1-IN-43 (compound Z13) is a small-molecule inhibitors targeting the PD-1/PD-L1 interaction. PD-1/PD-L1-IN-43 exhibites potent in vivo antitumor efficacy against B16-F10 melanoma. PD-1/PD-L1-IN-43 inhibits tumor growth by blocking the interaction between PD-1 and PD-L1. PD-1/PD-L1-IN-43 can be used in anti-tumor studies .

HY-162562

E28362	PCSK9	Cardiovascular Disease
E28362 is a novel small molecule PCSK9 inhibitor. E28362 blocks the interaction between PCSK9 and LDLR, thereby preventing the degradation of LDLR and maintaining cholesterol homeostasia. E28362 is a promising lead compound for the study of hyperlipidemia and atherosclerosis .

HY-117002

SRI 37892	Others	Cancer
SRI 37892 is a small molecule compound inhibitor of Frizzled protein 7 (Fzd7) with inhibitory activity against cancer cell proliferation (IC₅₀2μM). SRI 37892 significantly blocks Wnt/Fzd7 signaling. SRI 3789 can be used in the research of developing cancer therapeutic agents [1].

HY-163542

Pneumolysin-IN-1	Bacterial	Inflammation/Immunology
Pneumolysin-IN-1 (compound PB-3) is a targeted small molecule inhibitor of Pneumolysin (PLY) (IC₅₀=3.1 µM). Pneumolysin-IN-1 is a pore blocking agent and an anti-virulence factor. Pneumolysin-IN-1 can be used to study the infection caused by Streptococcus pneumoniae .

HY-125471

VK-1727	EBV	Infection Inflammation/Immunology Cancer
VK-1727 is a selective small molecule inhibitor of EBNA1. VK-1727 can reduce EBNA1 DNA binding activity. VK-1727 selectively blocks the proliferation and metabolic activity of EBV+ cells, instead of EBV- cells. VK-1727 is used in multiple sclerosis research .

HY-161138

WK369	BCL6 Apoptosis	Cancer
WK369 is a novel BCL6 small molecule inhibitor, which exhibits excellent anti-ovarian cancer bioactivity, induces cell cycle arrest and causes apoptosis. WK369 can directly bind to the BCL6-BTB domain and block the interaction between BCL6 and SMRT, leading to the reactivation of p53, ATR and CDKN1A .

HY-158107

BBO-8520	Ras	Cancer
BBO-8520 is a direct small molecule covalent inhibitor targeting KRAS ^G12C with high oral availability. BBO-8520 has the characteristics of KRAS ^G12C (OFF) inhibitor and the function of blocking KRAS ^G12C (ON) signal. BBO-8520 inhibits cell proliferation by inhibiting KRAS ^G12C (ON) by binding GTP protein. BBO-8520 can block RAS-RAF1 interaction and return KRAS ^G12C to the inactive (OFF) state .

HY-13912G

IWP-2	Wnt	Cancer
IWP-2 (GMP) is IWP-2 (HY-13912) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. IWP-2 is an inhibitor of Wnt processing and secretion with an IC₅₀ of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and blocks Wnt ligand palmitoylation .

HY-136702

L-97-1	Adenosine Receptor	Inflammation/Immunology
L-97-1 is a A1 adenosine receptor (A1AR) antagonist. L-97-1 is a water-soluble small molecule compound with high affinity and high selectivity against human A1 adenosine receptors. L-97-1 works by blocking A1 adenosine receptors. In patients with asthma, adenosine is an important signaling molecule capable of causing bronchoconstriction by activating A1AR. L-97-1 reduces airway hyperreactivity (BHR) by competitively binding to A1AR, thereby alleviating or blocking adenosine-induced bronchoconstriction and inflammation .

HY-108464A

Phenamil methanesulfonate	Sodium Channel TRP Channel	Metabolic Disease Inflammation/Immunology
Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC₅₀ of 400 nM . Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca ²⁺ transport with an IC₅₀ of 140 nM in a Ca ²⁺ uptake assay . Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway . Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease .

HY-110333

BMS-599626 dihydrochloride	EGFR	Cancer
BMS-599626 dihydrochloride is a small molecule pan-HER (human epidermal growth factor receptor) kinase inhibitor. BMS-599626 dihydrochloride primarily targets HER1 (IC₅₀=20 nmol/L) and HER2 (IC₅₀=30 nmol/L) kinase activity in the HER family. BMS-599626 inhibits the kinase activity of HER1 and HER2 by competing with their ATP-binding sites, and can inhibit the downstream signaling pathway by blocking the heterodimer formation of HER1 and HER2. BMS-599626 dihydrochloride can be used to study the antitumor effects of multiple HER1 or HER2 overexpressed tumor models .

Cat. No.	Product Name

HY-L080

Targeted Therapy Drug Library	107 compounds
Targeted cancer therapies are drugs or other substances that block the growth and spread of cancer by interfering with specific molecular targets that are involved in the growth, progression, and spread of cancer. There are several different types of targeted therapy. The most common types are small-molecule drugs and monoclonal antibodies. Small-molecule drugs are small enough to enter cells easily, so they are used for targets that are inside cells, while monoclonal antibodies are usually used for targets that are located outside the cells. Because of high specificity, low side effect and potent anticancer activity, targeted therapy has become the mainstream of new anti-tumor drugs. Various targeted therapies have been approved by FDA and used in the treatment of diseases. MCE carefully collects a unique of 107 targeted therapy drugs used in cancer treatment. MCE Targeted therapy drug library is a useful tool for the research of targeted therapy.

Targeted Therapy Drug Library

107 compounds

Targeted cancer therapies are drugs or other substances that block the growth and spread of cancer by interfering with specific molecular targets that are involved in the growth, progression, and spread of cancer.

There are several different types of targeted therapy. The most common types are small-molecule drugs and monoclonal antibodies. Small-molecule drugs are small enough to enter cells easily, so they are used for targets that are inside cells, while monoclonal antibodies are usually used for targets that are located outside the cells. Because of high specificity, low side effect and potent anticancer activity, targeted therapy has become the mainstream of new anti-tumor drugs. Various targeted therapies have been approved by FDA and used in the treatment of diseases.

MCE carefully collects a unique of 107 targeted therapy drugs used in cancer treatment. MCE Targeted therapy drug library is a useful tool for the research of targeted therapy.

HY-L153

Cysteine Targeted Covalent Library	4,566 compounds
Covalent inhibitors are small molecules that can bind specifically to target proteins through covalent bonds and inhibit their biological functions. Although for a long time, covalent targeting has been playing a subordinate role in drug discovery, with an increasing number of reports on successful clinical applications of such drugs, the potential of these agents is now being acknowledged. Currently, cysteine is the most common covalent amino acid residue in a variety of covalent drugs, and various warheads have been developed that can react with cysteine, providing the key building blocks for covalent drugs to form covalent bonds. To meet the development needs of covalent inhibitors targeting cysteine, MCE has designed a unique collection of 4,566 compounds with different covalent warheads that target cysteine. The MCE Cysteine Targeted Covalent Library is designed using the following covalent warheads: Acrylamides, Propiolic acid ester, Dimethylamine functionalized acrylamides, Chloroacetamides, Acrylonitrile, 2-Cyanoacrylamide, Aziridine, Haloacetamide, etc.

Cysteine Targeted Covalent Library

4,566 compounds

Covalent inhibitors are small molecules that can bind specifically to target proteins through covalent bonds and inhibit their biological functions. Although for a long time, covalent targeting has been playing a subordinate role in drug discovery, with an increasing number of reports on successful clinical applications of such drugs, the potential of these agents is now being acknowledged. Currently, cysteine is the most common covalent amino acid residue in a variety of covalent drugs, and various warheads have been developed that can react with cysteine, providing the key building blocks for covalent drugs to form covalent bonds.

To meet the development needs of covalent inhibitors targeting cysteine, MCE has designed a unique collection of 4,566 compounds with different covalent warheads that target cysteine. The MCE Cysteine Targeted Covalent Library is designed using the following covalent warheads: Acrylamides, Propiolic acid ester, Dimethylamine functionalized acrylamides, Chloroacetamides, Acrylonitrile, 2-Cyanoacrylamide, Aziridine, Haloacetamide, etc.

HY-L154

Cysteine Targeted Covalent Fragment Library	3,182 compounds
Covalent inhibitors are small molecules that can bind specifically to target proteins through covalent bonds and inhibit their biological functions. Although for a long time, covalent targeting has been playing a subordinate role in drug discovery, with an increasing number of reports on successful clinical applications of such drugs, the potential of these agents is now being acknowledged. Currently, cysteine is the most common covalent amino acid residue in a variety of covalent drugs, and various warheads have been developed that can react with cysteine, providing the key building blocks for covalent drugs to form covalent bonds. To meet the development needs of covalent inhibitors targeting cysteine, MCE has designed a unique collection of 3,182 fragments with different covalent warheads that target cysteine. The MCE Cysteine Targeted Covalent Fragment Library is designed using the following covalent warheads: Acrylamides, Propiolic acid ester, Dimethylamine functionalized acrylamides, Chloroacetamides, Acrylonitrile, 2-Cyanoacrylamide, Aziridine, Haloacetamide, etc. All fragments are pre-filtered with the Rule of Three restrictions which can be used for fragment-based covalent drug development.

Cysteine Targeted Covalent Fragment Library

3,182 compounds

To meet the development needs of covalent inhibitors targeting cysteine, MCE has designed a unique collection of 3,182 fragments with different covalent warheads that target cysteine. The MCE Cysteine Targeted Covalent Fragment Library is designed using the following covalent warheads: Acrylamides, Propiolic acid ester, Dimethylamine functionalized acrylamides, Chloroacetamides, Acrylonitrile, 2-Cyanoacrylamide, Aziridine, Haloacetamide, etc. All fragments are pre-filtered with the Rule of Three restrictions which can be used for fragment-based covalent drug development.

IWP-2 (GMP)	Fluorescent Dye
IWP-2 (GMP) is IWP-2 (HY-13912) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. IWP-2 is an inhibitor of Wnt processing and secretion with an IC₅₀ of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and blocks Wnt ligand palmitoylation .

IWP-2 (GMP)	Biochemical Assay Reagents
IWP-2 (GMP) is IWP-2 (HY-13912) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. IWP-2 is an inhibitor of Wnt processing and secretion with an IC₅₀ of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and blocks Wnt ligand palmitoylation .

PD-1/PD-L1-IN-20	PD-1/PD-L1	Cancer
PD-1/PD-L1-IN-20 (Example 21) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-20 blocks PD-1/PD-L1 with the IC₅₀ of 5.29 nM. PD-1/PD-L1-IN-20 can be used for the research of cancers, infectious diseases and autoimmune diseases .

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