"目录号: HY-15230
Cell Cycle/DNA DamageMetabolic Enzyme/Protease-
Geldanamycin 是一种特异性的干扰素调节因子3 (IRF3) 抑制剂，抑制IRF3磷酸化分子伴侣Hsp90。
HSP
相关产品
17-AAG-Triptolide-NVP-AUY922-Ganetespib-Teprenone-Rocaglamide-VER-155008-AT13387-Retaspimycin Hydrochloride-Alvespimycin hydrochloride-Debio 0932-BIIB021-PU-H71-NVP-HSP990-Apoptozole-
生物活性
Description
Geldanamycin is a specific inhibitor of interferon regulatory factor 3 (IRF3) (by inhibitingHsp90of the IRF3 phosphorylation chaperone).
IC50& Target
Hsp90[1]
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].
References
[1].Tang HB, et al. Viperin inhibits rabies virus replication via reduced cholesterol and sphingomyelin and is regulated upstream by TLR4. Sci Rep. 2016 Jul 26;6:30529.
[2].Chen WW, et al. RIP1 mediates the protection of Geldanamycin on neuronal injury induced by oxygen-glucosedeprivation combined with zVAD in primary cortical neurons. J Neurochem. 2012 Jan;120(1):70-7.
[3].Lin Z, et al. 17-ABAG, a novel Geldanamycin derivative, inhibits LNCaP-cell proliferation through heat shock protein 90 inhibition. Int J Mol Med. 2015 Aug;36(2):424-32.