1. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Cell Cycle/DNA Damage
  2. JAK CDK
  3. JAK1/CDK7-IN-1

JAK1/CDK7-IN-1 (compound 11) is a JAK1/CDK7 inhibitor and cytotoxic agent.JAK1/CDK7-IN-1 forms a stable, tightly bound complex with JAK1.JAK1/CDK7-IN-1 disrupts cell cycle, induces G2/M phase arrest, and increases Pre-G1 phase cell proportion.JAK1/CDK7-IN-1 induces apoptosis, elevates caspase 1, 3, and 9 levels, and triggers apoptotic and necrotic cell death.JAK1/CDK7-IN-1 can be used for the research of breast cancer, prostate cancer.

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

JAK1/CDK7-IN-1

JAK1/CDK7-IN-1 Chemical Structure

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Description

JAK1/CDK7-IN-1 (compound 11) is a JAK1/CDK7 inhibitor and cytotoxic agent.JAK1/CDK7-IN-1 forms a stable, tightly bound complex with JAK1.JAK1/CDK7-IN-1 disrupts cell cycle, induces G2/M phase arrest, and increases Pre-G1 phase cell proportion.JAK1/CDK7-IN-1 induces apoptosis, elevates caspase 1, 3, and 9 levels, and triggers apoptotic and necrotic cell death.JAK1/CDK7-IN-1 can be used for the research of breast cancer, prostate cancer[1].

In Vitro

JAK1/CDK7-IN-1 (compound 11) (tested across concentrations; 24 h) potently inhibits the proliferation of MCF-7, MDA-MB-231, and PC-3 cancer cells with IC50 values of 2.85, 4.61, and 7.69 µM respectively, and demonstrates selective toxicity toward cancer cells over normal WI-38 cells[1].
JAK1/CDK7-IN-1 potently inhibits JAK1 enzyme activity in MCF-7, MDA-MB-231, and PC-3 cells with IC50 values of 0.017, 0.01, and 0.10 µM respectively[1].
JAK1/CDK7-IN-1 inhibits CDK7 enzyme activity by 80.7% in MCF-7 cells, 68.1% in MDA-MB-231 cells, and 83.4% in PC-3 cells[1].
JAK1/CDK7-IN-1 upregulates apoptosis-associated caspase levels in cancer cells, with 4.60-, 3.03-, and 2.69-fold increases in caspase-1, -3, and -9 respectively in MDA-MB-231 cells, a 3.50-fold increase in caspase-1 in PC-3 cells, and 2.87- and 1.08-fold increases in caspase-1 and -9 respectively in MCF-7 cells[1].
JAK1/CDK7-IN-1 induces G2/M phase cell cycle arrest and pre-G1 apoptosis in MCF-7 cells, increasing G2/M phase cells to 35.03% and pre-G1 phase cells to 20.68%[1].
JAK1/CDK7-IN-1 significantly induces apoptosis and necrosis in MCF-7 cells, increasing total apoptosis to 10.92% and necrosis to 3.47%[1].

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

Cell Proliferation Assay[1]

Cell Line: MCF-7, MDA-MB-231, PC-3, WI-38
Concentration: tested across concentrations (to determine IC50)
Incubation Time: 24 h
Result: Exhibited potent antiproliferative activity with IC50 values of 2.85 µM (MCF-7), 4.61 µM (MDA-MB-231), and 7.69 µM (PC-3).
Showed higher potency than doxorubicin in MCF-7 and PC-3 cells, with selectivity indices (SI) of 6.85 (MCF-7), 4.23 (MDA-MB-231), and 2.54 (PC-3) relative to normal WI-38 cells.
Molecular Weight

533.43

Formula

C27H18Cl2N4O2S

SMILES

O=C(NC1=CC=C(/N=C/C2=CC(C3=CC=CS3)=NN2C4=CC=CC=C4)C=C1Cl)C5=CC(Cl)=CC=C5O

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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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  • 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.

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Product Name:
JAK1/CDK7-IN-1
Cat. No.:
HY-181528
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