2. PROTAC Cell Cycle/DNA Damage Apoptosis
  3. Ligands for Target Protein for PROTAC CDK c-Myc
  4. KI-ARv-03

KI-ARv-03 is a potent and selective ATP-competitive CDK9 inhibitor with an IC₅₀ of 0.15 μM (at 45 μM ATP), exhibiting over 130-fold selectivity against other CDKs (including CDK1-7). KI-ARv-03 reduces androgen receptor (AR)-driven transcription and proliferation in prostate cancer cells. KI-ARv-03 can be used for leukemia, pancreatic cancer, alveolar rhabdomyosarcoma (ARMS) and castration-resistant prostate cancer (CRPC) research. KI-ARv-03 is a ligand for target protein for PROTAC. KI-ARv-03 can be used to synthesize PROTAC KI-CDK9d-32 (HY-173523)[1][2].

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KI-ARv-03

KI-ARv-03 Chemical Structure

CAS No. : 2416873-72-6

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KI-ARv-03 Related Antibodies

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Description

KI-ARv-03 is a potent and selective ATP-competitive CDK9 inhibitor with an IC₅₀ of 0.15 μM (at 45 μM ATP), exhibiting over 130-fold selectivity against other CDKs (including CDK1-7). KI-ARv-03 reduces androgen receptor (AR)-driven transcription and proliferation in prostate cancer cells. KI-ARv-03 can be used for leukemia, pancreatic cancer, alveolar rhabdomyosarcoma (ARMS) and castration-resistant prostate cancer (CRPC) research. KI-ARv-03 is a ligand for target protein for PROTAC. KI-ARv-03 can be used to synthesize PROTAC KI-CDK9d-32 (HY-173523)[1][2].

IC50 & Target[1]

CDK9

0.15 μM (IC50)

In Vitro

KI-ARv-03 binds in the ATP-pocket of CDK9, forming critical interactions with hinge residues Glu107, His108, and the DFG-motif's Asp109[1].
KI-ARv-03 (5 μM, 18 h) selectively suppressed AR-V7 transcripts in both VCaP-16 and 22Rv1 cells, an effect that translated to KLK3 downregulation only in VCaP-16 cells, with no impact on AR-FL[1].
KI-ARv-03 (0-10 μM, 48-72 h) exhibits dose-dependent anti-proliferative activity (GR₅₀ = 1.52 μM in MV-4-11; GR₅₀ = 3.26 μM in 22Rv1) and induces more robust apoptosis in MV-4-11 AML cells, suggesting a heightened susceptibility of hematological cancers to CDK9 inhibition[1].
KI-ARv-03 (0-40 μM, 1 h) directly engages CDK9 but not AR species, indicating it affects AR levels through impaired CDK9 enzymatic activity[1].
KI-ARv-03 (0.5-10 μM, 1-48 h) dose-dependently reduces RNA Pol II (pSer2/pSer7), and time-dependently depletes AR-FL, AR-V7 and AR (pSer81) levels in 22Rv1 cells, consistent with its role in CDK9-mediated transcriptional regulation of the AR locus[1].
KI-ARv-03 (5 μM, 6-24 h) triggers the depletion of AR protein through a proteasome-dependent pathway, as evidenced by rescue with MG132 (HY-13259), thereby linking CDK9 inhibition to AR protein stability[1].
KI-ARv-03 (0-10 μM, 72-120 h) dose-dependently inhibits the proliferation of MOLT-4, PSN-1, and RH-4 cells, with IC₅₀ values ranging from 279.2 nM to 9.99 μM[2].

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

KI-ARv-03 Related Antibodies

Real Time qPCR[1]

Cell Line: VCaP-16 and 22Rv1 cells
Concentration: 5 μM
Incubation Time: 18 h
Result: Dramatically decreased transcript levels of KLK3 (PSA) and AR-V7 in VCaP-16 cells.
Decreased AR-V7 transcript, while KLK3 transcript levels showed no significant reduction in 22Rv1 cells.
Transcript levels of AR-FL remained unchanged in both cell lines.

Apoptosis Analysis[1]

Cell Line: MV-4-11 and 22Rv1 cells
Concentration: 10 μM top, 3.16-fold dilution
Incubation Time: 48 h for MV-4-11, and 72 h for 22Rv1
Result: Moderately increased apoptotic cell counts at high doses (10 and 3 μM), while no apoptotic cells were produced at submicromolar doses.

Cell Proliferation Assay[1]

Cell Line: MV-4-11 and 22Rv1 cells
Concentration: 10 μM top, 3.16-fold dilution
Incubation Time: 48 h for MV-4-11, and 72 h for 22Rv1
Result: Inhibited cell proliferation in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 0.5, 2.5, 5 and 10 μM
Incubation Time: 1, 2, 4, 6, 8, 24, and 48 h
Result: Significantly reduced phosphorylation of RNA Pol II at Ser2 and Ser7, even at low doses.
Significantly reduced AR-FL, AR-V7 protein levels and AR phosphorylation at Ser81 starting at 6 h, with complete depletion achieved after 16 h.
The depletion of AR protein was rescued by co-treatment with the proteasome inhibitor MG132 (10 μM).
Molecular Weight

259.35

Formula

C14H21N5
CAS No.
SMILES

CCCC1=NC2=CC=NN2C(N[C@H]3C[C@@H](CC3)N)=C1
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Purity & Documentation
References
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KI-ARv-03 Related Classifications

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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.

Keywords:

KI-ARv-032416873-72-6Ligands for Target Protein for PROTACCDKc-MycTarget Protein-binding MoietyCyclin dependent kinaseMycCDK9AR-drivenprostate cancerCRPCMV-4-11AMLVCaP-1622Rv1 cellsMOLT-4PSN-1RH-4Inhibitorinhibitorinhibit

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