An inhibitor of the Hsp90-Cdc37 protein-protein interaction
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CAY10747

Item No. 29915

Technical Information
Formal Name
(9β,13α,14β,20α)-3-hydroxy-9,13-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid, 3-[[(2Z)-3-cyano-3-(4-fluorophenyl)-1-oxo-2-propen-1-yl]oxy]propyl ester
CAS Number
2413849-81-5
Molecular Formula
C42H48FNO6
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 30 mg/mlDMSO: 20 mg/mlEthanol: 1 mg/ml
λmax
298, 422 nm
SMILES
O=C1C=C2C(C(C)=C1O)=CC=C3[C@]2(CC[C@]4([C@]5([H])C[C@@](CC[C@@]5(CC[C@]34C)C)(C(OCCCOC(/C=C(C#N)/C6=CC=C(F)C=C6)=O)=O)C)C)C
InChi Code
InChI=1S/C42H48FNO6/c1-26-30-12-13-33-40(4,31(30)23-32(45)36(26)47)17-19-42(6)34-24-39(3,15-14-38(34,2)16-18-41(33,42)5)37(48)50-21-7-20-49-35(46)22-28(25-44)27-8-10-29(43)11-9-27/h8-13,22-23,34,47H,7,14-21,24H2,1-6H3/b28-22+/t34-,38-,39-,40+,41-,42+/m1/s1
InChi Key
PNQKCDFOTMDGCU-PYZHFFOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    CAY10747 is an inhibitor of the protein-protein interaction between heat shock protein 90 (Hsp90) and cell division cycle 37 (Cdc37) and a derivative of celastrol (Item No. 70950).1 It decreases protein levels of the Hsp90-Cdc37 complex and the Hsp90-Cdc37 clients phosphorylated Akt and Cdk4 in A549 cells when used at a concentration of 5 µM. CAY10747 inhibits proliferation of A549, MCF-7, HOS, and HepG2 cells (IC50s = 0.41, 0.64, 0.9, and 0.94 µM, respectively) and induces apoptosis in A549 cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Li, N., Xu, M., Wang, B., et al. Discovery of novel celastrol derivatives as Hsp90-Cdc37 interaction disruptors with antitumor activity. J. Med. Chem. 62(23), 10798-10815 (2019).