2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Stem Cell/Wnt Apoptosis
  3. HSP Casein Kinase Apoptosis
  4. Hsp90-Cdc37-IN-4

Hsp90-Cdc37-IN-4 是一种新型的雷公藤红素 (HY-13067)衍生物，可抑制 Hsp90-Cdc37 蛋白相互作用 (PPI)。Hsp90-Cdc37-IN-4 选择性抑制酪蛋白激酶 2 (CK 2)，减少其底物 Cdc37 在丝氨酸 13 位点的磷酸化。Hsp90-Cdc37-IN-4 诱导 G0/G1 期细胞周期阻滞，并通过线粒体途径触发细胞凋亡。Hsp90-Cdc37-IN-4 显示出强大的抗乳腺癌活性[1]。

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Hsp90-Cdc37-IN-4 Chemical Structure

Hsp90-Cdc37-IN-4 Chemical Structure

CAS No. : 2758818-41-4

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Hsp90-Cdc37-IN-4 相关抗体

Top Publications Citing Use of Products

查看 HSP 亚型特异性产品:

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

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CK1 CK2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Hsp90-Cdc37-IN-4, a novel Celastrol (HY-13067) derivative, inhibits the Hsp90-Cdc37 protein-protein interaction (PPI). Hsp90-Cdc37-IN-4 selectively inhibits casein kinase 2 (CK2), reducing phosphorylation of its substrate Cdc37 at Serine 13. Hsp90-Cdc37-IN-4 induces G0/G1 cell cycle arrest and triggers apoptosis via the mitochondrial pathway. Hsp90-Cdc37-IN-4 demonstrates potent anti-breast cancer activity[1].

体外研究
(In Vitro)

Hsp90-Cdc37-IN-4 (化合物11) (48 h) 对五种人类癌细胞系显示出抑制细胞系增殖的作用，IC50分别为0.21 μM (MBGC-23)，0.27 μM (HOS)，0.33 μM (HCT-116)，0.43 μM (MCF-7)和0.25 μM (MDA-MB-231)[1]。

Hsp90-Cdc37-IN-4 (0.5-8.0 μM, 2 h)对 CK2α1 表现出强抑制作用[1]。

Hsp90-Cdc37-IN-4 (0.2-0.8 μM, 24 h) 能下调 MDA-MB-231 细胞中p-Cdc37 (丝氨酸 13)和 p-Akt (丝氨酸 129) 水平，表明对细胞内 CK2 活性有抑制作用并以浓度依赖性抑制 Cdc37 磷酸化[1]。

Hsp90-Cdc37-IN-4 (0.15-0.6 μM, 24 h) 以浓度依赖的方式诱导 MDA-MB-231 细胞发生 G0/G1 期细胞周期阻滞[1]。

Hsp90-Cdc37-IN-4 (0.2 μM, 24 h) 通过抑制 Hsp90-Cdc37 循环诱导 MDA-MB-231 细胞凋亡[1]。

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

Hsp90-Cdc37-IN-4 相关抗体:

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 24h
Result: Significantly increased G0/G1-phase cell cycle arrest to 44.54% at 0.6 μM demonstrated superior efficacy versus 1.0 μM Celastrol.
Nearly abolished kinase client protein Cdk4 levels at 0.8 μM.
Mechanistically linked G0/G1 arrest in MDA-MB-231 cells to Cdk4 degradation through dual-targeted disruption of the Hsp90-Cdc37-kinase cycle.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: MDA-MB-231 cells
Incubation Time: 24h
Result: Blocked the Hsp90-Cdc37-kinase cycle through a dual-targeting mechanism, thereby triggering degradation of kinase client proteins and activating the mitochondrial apoptosis pathway.
体内研究
(In Vivo)

Hsp90-Cdc37-IN-4 (1 mg/kg，腹腔注射，每日一次，持续21天) 在 MDA-MB-231 异种移植小鼠模型中显示出强大的抗肿瘤活性[1]。

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

Animal Model: MDA-MB-231 xenograft model established in BALB/C nude female mice (4 weeks) [1]
Dosage: 1 mg/kg
Administration: Daily intraperitoneal injection (i.p.), at the corresponding doses for 21 days.
Result: Achieved 65.3% tumor growth inhibition (TGI) at 1 mg/kg through dual-targeting mechanisms demonstrated significantly superior efficacy versus positive control (1 mg/kg Celastrol, TGI = 38.0%).
Induced no significant body weight loss in treated mice exhibited low systemic toxicity.
Showed no observable histopathological damage in cardiac, hepatic, splenic, pulmonary, or renal tissues at 1.0 mg/kg.
Established an efficacious and low-toxicity antitumor candidate profile.
分子量

638.84

Formula

C40H50N2O5
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

Hsp90-Cdc37-IN-4 相关分类

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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:

Hsp90-Cdc37-IN-42758818-41-4HSPCasein KinaseApoptosisHeat shock proteinsCelastrolCK2Hsp90-Cdc37 PPIAntitumorMDA-MB-231Inhibitorinhibitorinhibit

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