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, 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.

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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 Related Antibodies

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Description

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].

In Vitro

Hsp90-Cdc37-IN-4 (Compound 11) (48 h) inhibits proliferation in five human cancer cell lines with IC50 of 0.21 μM (MBGC-823), 0.27 μM (HOS), 0.33 μM (HCT-116), 0.43 μM (MCF-7) and 0.25 μM (MDA-MB-231)[1].

Hsp90-Cdc37-IN-4 (0.5-8.0 μM, 2 h) shows the strongest inhibitory effect on CK2α1[1].

Hsp90-Cdc37-IN-4 (0.2-0.8 μM, 24 h) down-regulates p-Cdc37 (Ser13) and p-Akt (Ser129) levels in MDA-MB-231 cells, demonstrating concentration-dependent inhibition of intracellular CK2 activity and suppression of Cdc37 phosphorylation[1].

Hsp90-Cdc37-IN-4 (0.15-0.6 μM, 24 h) concentration-dependently induces G0/G1 phase cell cycle arrest in MDA-MB-231 cells[1].

Hsp90-Cdc37-IN-4 (0.2 μM, 24 h) induces apoptosis in MDA-MB-231 cells by inhibiting the Hsp90-Cdc37 chaperone cycle[1].

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

Hsp90-Cdc37-IN-4 Related Antibodies

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.
In Vivo

Hsp90-Cdc37-IN-4 (Compound 11) (1 mg/kg, i.p., daily for 21 days) shows potent antitumor activity in the MDA-MB-231 xenograft mice model[1].

MedChemExpress (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.
Molecular Weight

638.84

Formula

C40H50N2O5
CAS No.
SMILES

O=C1C(O)=C(C)C2=CC=C([C@](CC[C@]3(C)[C@@]4([H])C[C@](C)(C(NCCCOC(/C=C/C5=NC=CC=C5)=O)=O)CC3)(C)[C@@]4(C)CC6)[C@]6(C)C2=C1
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Purity & Documentation
References
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Hsp90-Cdc37-IN-4 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:

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

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