HSP

NVP-BEP800 is a novel, fully synthetic, orally bioavailable inhibitor that binds to the NH2-terminal ATP-binding pocket of Hsp90.

PF-04929113 (SNX-5422) is orally bioavailable heat shock protein 90 (Hsp90) inhibitor.

MPC-3100 is an orally bioavailable, synthetic, second-generation small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.

SNX-2112 is a heat shock protein 90 (Hsp90) inhibitor with anticancer properties currently in clinical trials. SNX-2112 induced autophagy in a time- and dose-dependent manner via Akt/mTOR/p70S6K inhibition. SNX-2112 induces significant apoptosis and autophagy in human melanoma A-375 cells, and may be an effective targeted therapy agent

KW-2478 is an agent that targets the human heat-shock protein 90 (Hsp90) with potential antineoplastic activity.

XL888 is an orally bioavailable, ATP-competitive, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.

IPI-504 is a novel, water-soluble, potent inhibitor of heat-shock protein 90 (Hsp90).

IPI-493 is a potent and orally bioavailable HSP90 inhibitor with Ki of 21 nM.

Occupies mortalin-2 (mot-2), a member of the Hsp70 family, at its p53 binding site and enables p53 translocation to the nucleus. Selectively cytotoxic; causes growth arrest of cancer cells in culture. Also inhibits telomerase activity and cross-links F-actin.

CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC50 of 19 nM for inhibition of HSF1-mediated HSP72 induction.

Debio 0932 is a novel heat shock protein 90 (HSP90) inhibitor with strong affinity for HSP90 alpha/beta, high oral bioavailability and potent anti-proliferative activity against a broad range of cancer cell lines (with a mean IC50 of 220 nmol/L), including many non-small cell lung cancer (NSCLC) cell lines which are resistant to standard-of-care (SOC) agents.

Rocaglamide (Rocaglamide A) is isolated from the genus Aglaia and can be used to treat coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia.

VER-49009 is a pyrazole compound that inhibits Hsp90 with an IC50 value of 47 nM.

VER-50589 is an isoxazole compound that inhibits Hsp90 with an IC50 value of 21 nM.

CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.

Gedunin, a naturally occurring Hsp90 inhibitor, is tetranortriterpenoid isolated from the Indian neem tree (Azadirachta indica).

Macbecin I is an ansamycin antibiotic compound that inhibits Hsp90 activity with IC50 value of μM by binding to the ATP-binding site.

TRC 051384, belonging to substituted 2-propen-1-one class, is a potent inducer of heat shock protein 70 (HSP70) [1]. Induction of HSP70 is a natural response of stressed cells that protects neuronal cells from a variety of insults including acute ischemia.

EC 144 is a potent inhibitor of the heat shock protein 90 and was found to be effective in tumor growth suppression.

HSF1A is a cell-permeable activator of heat shock transcription factor 1 (HSF1).

Col003 is a potent inhibitor of Hsp47, competitively binds to the collagen binding site on Hsp47 (IC50, 1.8 μM), and inhibits collagen secretion by destabilizing the collagen triple helix.

HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof.

SNX-5422 Mesylate (PF-04929113 Mesylate), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37?nM.

HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.