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  3. 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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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.

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.
SMILES

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

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    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.

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THK01
Cat. No.:
HY-149266
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