2. Cell Cycle/DNA Damage TGF-beta/Smad Stem Cell/Wnt Cytoskeleton
  3. ROCK
  4. THK01

THK01 is a potent ROCK2 inhibitor with IC50 values of 5.7 and 923 nM for ROCK2 and ROCK1, respectively. THK01 inhibits breast cancer metastasis through the ROCK2-STAT3 signaling pathway. THK01 can be used in research of breast cancer.

For research use only. We do not sell to patients.

THK01 Chemical Structure

THK01 Chemical Structure

CAS No. : 2226941-26-8

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5 mg USD 320 In-stock
10 mg USD 510 In-stock
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Based on 1 publication(s) in Google Scholar

THK01 Related Antibodies

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Description

THK01 is a potent ROCK2 inhibitor with IC50 values of 5.7 and 923 nM for ROCK2 and ROCK1, respectively. THK01 inhibits breast cancer metastasis through the ROCK2-STAT3 signaling pathway. THK01 can be used in research of breast cancer[1].

IC50 & Target[1]

ROCK2

5.7 nM (IC50)

ROCK1

923 nM (IC50)

In Vitro

THK01 (1.25-10 μM; 48 h) suppresses the migration and invasion abilities of MDA-MB-231 cells in a dose-dependent manner[1].
THK01 (5 μM; 24 h; MDA-MB-231 cells) suppresses breast cancer metastasis through STAT signal pathway[1].
THK01 (1.25-10 μM; 24 h; MDA-MB-231 cells) down-regulates the phosphorylation level of STAT3Y705 in a dose-dependent manner, while slightly up-regulates the level of STAT3S727[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

THK01 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 5 μM
Incubation Time: 24 hours
Result: Down-regulated the phosphorylation levels (p-STAT) of STAT1, STAT2, and STAT3, up-regulated of p-STAT5A and STAT6.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 1.25, 2.5, 5, 10 μM
Incubation Time: 24 hours
Result: Reduced the level of p-STAT3Y705 and increased the expression of p-STAT3S727 in MDA-MB-231 cells.
In Vivo

THK01 (15 mg/kg; i.v.; Female BALB/c nude mice) suppresses cell metastasis of breast cancer in vivo[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c nude mice with MDAMB-231-Luc-mcherry xenografts (6 weeks old, weight about 20 g)[1]
Dosage: 15 mg/kg
Administration: Intravenous injection; once a day for 43 days
Result: Reduced the pulmonary metastasis of MDA-MB-231 in vivo with negligible toxicity.
Molecular Weight

327.34

Formula

C20H13N3O2
CAS No.
Unlabeled Cas

Appearance

Solid

Color

Off-white to gray

SMILES

O=C1NCC2=C3C4=C(NC3=C5NC6=C(C5=C12)C=C(C=C6)O)C=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (381.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0549 mL 15.2746 mL 30.5493 mL
5 mM 0.6110 mL 3.0549 mL 6.1099 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0549 mL 15.2746 mL 30.5493 mL 76.3732 mL
5 mM 0.6110 mL 3.0549 mL 6.1099 mL 15.2746 mL
10 mM 0.3055 mL 1.5275 mL 3.0549 mL 7.6373 mL
15 mM 0.2037 mL 1.0183 mL 2.0366 mL 5.0915 mL
20 mM 0.1527 mL 0.7637 mL 1.5275 mL 3.8187 mL
25 mM 0.1222 mL 0.6110 mL 1.2220 mL 3.0549 mL
30 mM 0.1018 mL 0.5092 mL 1.0183 mL 2.5458 mL
40 mM 0.0764 mL 0.3819 mL 0.7637 mL 1.9093 mL
50 mM 0.0611 mL 0.3055 mL 0.6110 mL 1.5275 mL
60 mM 0.0509 mL 0.2546 mL 0.5092 mL 1.2729 mL
80 mM 0.0382 mL 0.1909 mL 0.3819 mL 0.9547 mL
100 mM 0.0305 mL 0.1527 mL 0.3055 mL 0.7637 mL
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THK01 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

THK012226941-26-8THK 01THK-01ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKbreast cancerindolocarbazolemetastasisMDA-MB-231 cellsInhibitorinhibitorinhibit

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