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HSP

Heat shock proteins (HSPs) are a family of highly conserved proteins that are expressed, either constitutively or regulated inductively, in response to a wide range of physiological and environmental insults, such as heat shock. According to molecular weight, mammalian HSPs are classified into four subfamilies, including HSP90 (90 kDa), HSP70 (70 kDa), HSP60 (60 kDa) and small HSPs (15 to 30 kDa), among which HSP90 and HSP70 are two of the most studied stress-inducible HSPs. HSP90 is a highly abundant chaperone protein characterized by containing three relevant domains, including the N-terminal domain, the charged middle linker region and the C-terminal dimerization domain; while HSP70 is an ATP-dependent chaperone protein characterized by containing two distinct functional domains, including a peptide binding domain (PBD) and the amino-terminal ATPase domain (ABD). Collectively HSPs play a fundamental role in maintaining the stability of other cellular proteins.

Research Area

  1. Cat.No. Product Name Information
  2. A2213 17-DMAG (Alvespimycin) HCl 17-DMAG is an inhibitor of Hsp90 with IC50 value of 62±29nM .
  3. A4388 XL-888

    XL-888 is a novel and orally-bioavailable inhibitor of heat shock protein 90 (HSP90) that selectively inhibits HSP90α and HSP90β with values of 50% inhibition concentration IC50 of 22 nM and 44 nM respectively.

  4. A4387 VER 155008 VER 155008 is a potent inhibitor of heat shock protein 70 (Hsp70) family of chaperones, which have been shown to contribute to cancer cell survival via anti-apoptotic functions, that inhibits Hsp70 (with the value of 50% inhibition concentration IC50 of 0.5 μM) as well as heat shock cognate 71 kDa protein (Hsc70) and 78 kDa glucose-regulated protein (Grp78) but to a lesser extent.
  5. A4067 Radicicol Radicicol is an inhibitor of the ATPase/kinase with IC50 values of <1μM, 100μM and 400μM, respectively for Hsp90, Topo VI and PDK3 .
  6. A4065 PF-04929113 (SNX-5422) PF-04929113 is an inhibitor of Hsp90 .
  7. A4064 NVP-BEP800 NVP-BEP800 is a fully synthetic, orally bioavailable inhibitor of Hsp90 with IC50 value of 58nM .
  8. A4063 MPC-3100 MPC-3100 is a purine-based inhibitor of Hsp90 with IC50 value of 60nM .
  9. A4061 IPI-504 (Retaspimycin hydrochloride) Retaspimycin hydrochloride (also known as IPI-504), a hydroquinone hydrochloride salt derivative of 17-AAG, is a novel, potent and selective inhibitor of heat shock protein 90(Hsp90) that binds to the amino-terminal ATP/ADP-binding site of Hsp90.
  10. A4058 BIIB021 BIIB021 is a selective inhibitor of Hsp90 with Ki and EC50 values of 1.7 nM and 38 nM, respectively.
  11. A4056 AT13387 AT13387, discovered by a high-throughput x-ray craystallography fragment-based platform, is a non-geldanamycin heat shock proterin 90 (HPS90), a molecule chaperone regulating signal transduction pathways for cell growth and survival, inhibitor reportedly resulting in client protein degradation, suppression of signaling, and inducing cell cycle arrest and apoptosis.

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