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

KI-ARv-03 是一种强效且选择性的 ATP 竞争性 CDK9 抑制剂，IC50 为 0.15 μM (在 45 μM ATP 浓度下)，对其他 CDK (包括 CDK1-7) 的选择性超过 130 倍。KI-ARv-03 可降低前列腺癌细胞中 AR 驱动的转录和增殖。KI-ARv-03 可用于白血病、胰腺癌、肺泡横纹肌肉瘤 (ARMS) 和去势抵抗性前列腺癌 (CRPC) 的相关研究。KI-ARv-03 是 PROTAC 靶蛋白的配体 (ligand for target protein for PROTAC)。KI-ARv-03 可用于合成 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 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(In Vitro)

KI-ARv-03 结合于 CDK9 的 ATP 口袋，与铰链残基 Glu107、His108 和 DFG 基序的 Asp109 形成关键相互作用[1]。
KI-ARv-03 (5 μM，18 小时) 选择性抑制 VCaP-16 和 22Rv1 细胞中的 AR-V7 转录本，这种效应仅在 VCaP-16 细胞中导致 KLK3 下调，而对 AR-FL 没有影响[1]。
KI-ARv-03 (0-10 μM，48-72 小时) 表现出剂量依赖性抗增殖活性 (MV-4-11 中 GR₅₀ = 1.52 μM；22Rv1 中 GR₅₀ = 3.26 μM)，并在 MV-4-11 AML 细胞中诱导更强烈的细胞凋亡，表明血液系统癌症对 CDK9 抑制的敏感性增强[1]。
KI-ARv-03 (0-40 μM，1 小时) 直接作用于 CDK9，但不作用于 AR 种类，表明它通过削弱 CDK9 酶活性来影响 AR 水平[1]。
KI-ARv-03 (0.5-10 μM，1-48 小时) 剂量依赖性地降低 22Rv1 细胞中的 RNA Pol II (pSer2/pSer7) 水平，并时间依赖性地降低 AR-FL、AR-V7 和 AR (pSer81) 水平，这与其在 CDK9 介导的 AR 基因座转录调控中的作用一致[1]。
KI-ARv-03 (5 μM，6-24 小时) 通过蛋白酶体途径触发 AR 蛋白的耗竭，这一机制经 MG132 (HY-13259) 对其降解的挽救作用证实，从而将CDK9抑制与AR蛋白稳定性联系起来[1]。
KI-ARv-03 (0-10 μM，72-120 小时) 剂量依赖性地抑制 MOLT-4、PSN-1 和 RH-4 细胞的增殖，IC₅₀ 值范围为 279.2 nM 至 9.99 μM[2]。

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

KI-ARv-03 相关抗体:

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).
分子量

259.35

Formula

C14H21N5
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

KI-ARv-03 相关分类

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  • 稀释计算器

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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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