2. Cell Cycle/DNA Damage
  3. CDK
  4. KB-0742

KB-0742 is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 has potent anti-tumor activity.

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KB-0742 Chemical Structure

KB-0742 Chemical Structure

CAS No. : 2416873-83-9

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Description

KB-0742 is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 has potent anti-tumor activity[1].

IC50 & Target[1]

CDK9/cyclinT1

6 nM (IC50)

In Vitro

KB-0742 (6 hours; 0.1-10 μM; 22Rv1 cells) treatment significant reduction of downstream phosphorylation of RNA Pol II at Ser2 and Ser7, and diminished phosphorylation at Ser5. Global androgen receptor (AR)-FL and AR-V protein levels are significantly reduced starting at 6 h treatment time, which is accompanied by the reduction of phospho-AR levels (Ser81)[1].
KB-0742 (48-72 hours) treatment shows cytostatic effects in prostate cancer and leukemia cell lines. KB-0742 shows antiproliferative activity with GR50s of 0.183 μM and 0.288 μM for 22Rv1 cells and MV-4-11 AML cells, respectively[1].
In 22Rv1 cells, KB-0742 rapidly downregulates nascent transcription, preferentially depleting short half-life transcripts and AR-driven oncogenic programs[1].

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

KB-0742 Related Antibodies

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 0.1 μM, 0.5 μM, 1 μM, 10 μM
Incubation Time: 6 hours
Result: Significant reduction of downstream phosphorylation of RNA Pol II at Ser2 and Ser7, and diminished phosphorylation at Ser5.
In Vivo

KB-0742 (3-30 mg/kg; p.o.; daily; over 21 days) is well tolerated even at high dose, while significantly reducing tumor burden in 22Rv1 human prostate cancer cell line-derived xenograft (CDX) models[1].

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

Animal Model: Male CB17-SCID mice injected with 22Rv1 human prostate cancer cells[1]
Dosage: 3 mg/kg, 10 mg/kg, and 30 mg/kg
Administration: p.o.; daily; over 21 days
Result: Significantly reduced tumor growth in castration-resistant prostate cancer (CRPC).
Molecular Weight

287.40

Formula

C16H25N5
CAS No.
SMILES

N[C@@H]1C[C@@H](NC2=CC(C(CC)CC)=NC3=CC=NN23)CC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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KB-0742 Related Classifications

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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:

KB-07422416873-83-9KB0742KB 0742CDKCyclin dependent kinaseCDK9oralanticancerCRPCSer2Ser7Ser5antiproliferativeInhibitorinhibitorinhibit

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