Hsp90-Cdc37-IN-4
Hsp90-Cdc37-IN-4, a 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.
For research use only. We do not sell to patients.
- CAS No.: 2758818-41-4
- Formula: C40H50N2O5
- Molecular Weight:638.84
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
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Cell Line:MDA-MB-231 cells
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Concentration:0.15, 0.3 and 0.6 μM
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Incubation Time:24h
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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.
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Cell Line:MDA-MB-231 cells
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Concentration:MDA-MB-231 cells
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Incubation Time:24h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MDA-MB-231 xenograft model established in BALB/C nude female mice (4 weeks) [1]
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Dosage:1 mg/kg
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Administration:Daily intraperitoneal injection (i.p.), at the corresponding doses for 21 days.
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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.
Chemical Information
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CAS No. 2758818-41-4
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Molecular Weight 638.84
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Formula C40H50N2O5
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Hsp90-Cdc37-IN-4 Related Classifications
HY-174347 Related Classifications
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