||Rifabutin inhibits bacterial DNA-dependent RNA polymerase, thereby suppressing the initiation of RNA formation and leading to inhibition of RNA synthesis and transcription. Rifabutin is a semisynthetic ansamycin antibiotic with potent antimycobacterial properties.
||AUY922 (NVP-AUY922) is a new-type synthetic resorcinylic isoxazole amide inhibitor of heat shock protein 90 (HSP90). It has been used in trials studying the treatment and basic science of lymphoma, leukemia, T-cell lymphoma, hepatic Impairment, and follicular lymphoma, among others.
||NVP-BEP800, a synthetic HSP90β inhibitor (IC50: 58 nM), exhibits >70-fold selectivity against Hsp90 family members Trap-1 and Grp94.
||Triptolide is a diterpenes trioxide, immunosuppressive agent extracted from the Chinese herb Tripterygium wilfordii.
||VER-50589 is a potent HSP90 inhibitor.
||VER-49009 is an effective HSP90 inhibitor(IC50 =25 nM,Kd=78 nM).
||BIIB021 is an orally-available, fully synthetic inhibitor of HSP90(Ki=1.7nM,EC50=38nM).
||Ganetespib is a synthetic small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.
||KNK437, a pan-HSP inhibitor, suppresses the synthesis of inducible HSPs(HSP105, HSP72, and HSP40).
||Apoptozole is an inhibitor of the ATPase domain of Hsc70 and Hsp70，and can induce apoptosis.
||Inducer of heat shock protein Hsp70; reduces stroke-associated neuronal injury and increases survival in a rat model of transient ischemic stroke. Activates heat shock factor-1 and results in elevated chaperone and anti-inflammatory activity. Enhances Hsp72 expression in neurons and glial cells.
||ML346 is a novel activator of Hsp70.
||NVP-HSP990 (HSP990) is an effective and specific HSP90α/β inhibitor (IC50: 0.6 /0.8 nM).
||Elesclomol (STA-4783) is an effective oxidative stress inducer that elicits pro-apoptosis of tumor cells.
||XL888 is an ATP-competitive inhibitor of Hsp90 ( IC50: 24 nM). Heat shock protein 90 (Hsp90) is a chaperone that maintains the functionality of client proteins involved in cell proliferation, cell cycling, and apoptosis. Through this action, specific client proteins are degraded, resulting in cell c
||Onalespib is a synthetic, orally bioavailable, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity. Onalespib selectively binds to Hsp90, thereby inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in t
||17-AAG (Tanespimycin), an effective HSP90 inhibitor (IC50: 5 nM), has a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells.
||SNX-2112 is an orally active Hsp90 inhibitor, with a Kd of 16 nM.
||SNX-5422 is a synthetic, novel, small molecule Hsp90 Inhibitor. As an oral formulation that demonstrates strong efficacy and tolerability, SNX-5422 is positioned as a breakthrough therapy with broad applicability across a wide range of cancers.
||Geldanamycin, an HSP90 inhibitor (Kd: 1.2 μM), specifically disrupts glucocorticoid receptor (GR)/HSP association.
||CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
||KW-2478 is a non-ansamycin HSP90 inhibitor with IC50 of 3.8 nM.
||NMS-E973 is a potent and selective Hsp90 inhibitor with DC50 of <10 nM for Hsp90 binding, no activiy against a panel of 52 diverse protein kinases.
||HA15 targets specifically BiP/GRP78/HSPA5. HA15 exhibits anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors.
||PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.
||VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, >100-fold selectivity over HSP90.
||HSF1A is a cell-permeable activator of HSF1 that protects mammalian cells against stress-induced apoptosis.
||PF-04929113 Mesylate, a prodrug of SNX-2112, is an orally available Hsp90 inhibitor (Kd: 41 nM) and also induces Her-2 degradation (IC50: 37?nM).