Retaspimycin Hydrochloride is a potent Hsp90 inhibitor with an EC50 of 119 nM.

 

Brand: BCM

 

Target: HSP90:119 nM （EC50）, Grp94:119 nM （EC50）

 

In Vitro: Retaspimycin is an inhibitor of Hsp90. Retaspimycin can abrogate both the unfolded protein response element (UPRE) and ERSE-driven luciferase activity in non-treated U266 and MM.1s cells as well as in Tunicamycin (Tm)-treated cells. Incubation of Retaspimycin potently suppresses both Akt and MAPKs phosphorylation in both sensitive and Trastuzumab-resistant cells. Total levels of Akt decreased in all 4 cell lines (BT474, SKBR-3, HCC1569, and HCC1569) in a dose-dependent manner. However, levels of total MAPKs are not significantly altered with Retaspimycin treatment

 

Solubility: Soluble in DMSO. Insoluble in Water.

 

Isomeric SMILES: C[C@H]1C[C@@H]([C@@H]([C@H](/C=C(/[C@@H]([C@H](/C=C\C=C(\C(=O)NC2=CC(=C(C(=C2O)C1)NCC=C)O)/C)OC)OC(=O)N)\C)C)O)OC.Cl  

 

InChIKey: OIRUWDYJGMHDHJ-AFXVCOSJSA-N  

 

InChI: InChI=1S/C31H45N3O8.ClH/c1-8-12-33-26-21-13-17(2)14-25(41-7)27(36)19(4)15-20(5)29(42-31(32)39)24(40-6)11-9-10-18(3)30(38)34-22(28(21)37)16-23(26)35;/h8-11,15-17,19,24-25,27,29,33,35-37H,1,12-14H2,2-7H3,(H2,32,39)(H,34,38);1H/b11-9-,18-10+,20-15+;/t17-,19+,24+,25+,27-,29+;/m1./s1 

 

Attribute
[Chem Name]	[(4E,6Z,8S,9S,10E,12S,13R,14S,16R)-13,20,22-trihydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3-oxo-19-(prop-2-enylamino)-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18(22),19-hexaen-9-yl] carbamate;hydrochloride
[Synonym]	IPI-504; Retaspimycin Hydrochloride; Retaspimycin HCl
[CAS No.]	857402-63-2
[EINECS]	200-258-5
[Formula]	C31H47N3O8.ClH
[Molecular]	626.186
[Form]	Off-white to pink solid
[Storage]	-20°C, sealed storage, away from moisture

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