tcsc0628 Geldanamycin

Geldanamycin is a specific inhibitor of interferon regulatory factor 3 (IRF3) (by inhibiting Hsp90 of the IRF3 phosphorylation chaperone, with a K_d of 1.2 μM.).

IC50 & Target: Kd: 1.2 μM (Hsp90)^[4]

In Vitro: Geldanamycin significantly delays and reduces viperin expression, indicating that IRF3 is involved in viperin induction in RAW264.7 cells^[1]. Geldanamycin (GA), a benzoquinone ansamycin, protected against neuronal injury induced by oxygen-glucose deprivation (OGD)/zVAD treatment in cultured primary neurons. More importantly, Geldanamycin decreases RIP1 protein level in a time and concentration-dependent manner. Geldanamycin also decreases the Hsp90 protein level, which causes instability of RIP1 protein, resulting in decreased RIP1 protein level but not RIP1 mRNA level after Geldanamycin treatment^[2]. Geldanamycin (GA) is identified as the first natural product inhibitor of Hsp90 that binds to the N-terminal ATPase domain of Hsp90 to inhibit its chaperone function, and significantly induces tumor cell death via an apoptotic mechanism^[3].