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Cat. No. Product Name CAS No. Information
PC-35293

KBU2046

1143863-69-7

KBU2046 (KBU-2046) is a highly selective inhibitor of metastasis, binds to and stabilizes CDC37/HSP90β heterocomplexes; selectively disrupts heterocomplex function and inhibits cancer cell motility, only binds to HSP90β and CDC37 when both proteins are present, does not bind to either protein alone; decreases phosphorylation of HSP90β, inhibits cancer metastasis and prolongs life in vivo; KBU2046-mediated changes in the signature of client proteins bound to the HSP90β/CDC37 heterocomplex mediate effects upon cell motility.

PC-63191

HSP27 inhibitor J2

2133499-85-9

HSP27 inhibitor J2 is a small molecule functional inhibitor of Hsp27, induces significant abnormal HSP27 dimer formation in cancer cells; enhances cancer cell sensitization with cisplatin, cisplatin-induced lung cancer cell growth inhibition in vitro; significantly inhibits immune cell infiltration in lung tissue, attenuates radiation-induced pulmonary inflammation in mice.

PC-62492

JG-98

1456551-16-8

JG-98 is an allosteric Hsp70 inhibitor, displays >3-fold more active, greater stability than MKT-077 against the breast cancer cell lines MDA-MB-231 and MCF-7 (EC50 of 0.4 uM and 0.7 uM, respectively); strongly affects autophagic flux, increases p62 oligomerization and reduces p62 monomer; destabilizes FoxM1 and relieved suppression of downstream effectors, including p21 and p27.

PC-61250

KW-2478

819812-18-5

KW-2478 (KW2478) is a novel potent Hsp90 inhibitor with IC50 of 3.8 nM (Hsp90α), exhibits antitumor activities both in vitro and in vivo; demonstrates antiproliferative activities against human MM cells, OPM-2/GFP, KMS-11, RPMI 8226, and NCI-H929 with IC50 of 0.30, 0.34, 0.39, and 0.12 uM respectively, associated with degradation of well-known client proteins as well as FGFR3, c-Maf, and cyclin D1; suppresses tumor growth in NCI-H929 models.

Blood Cancer

Phase 2 Discontinued

PC-70347

STA 2842

1046490-67-8

STA 2842 (STA2842) is a highly specific inhibitor of HSP90 (IC50=135 nM, HSP90α) that competitively binds the N-terminal ATP pocket of HSP90; induces the degradation of many ADPKD-relevant HSP90 client proteins in Pkd1(-/-) primary kidney cells and in vivo; significantly reduces initial formation of renal cysts and kidney growth and slows the progression of these phenotypes in mice with preexisting cysts.

PC-60683

SNX-0723

1073969-18-2

SNX-0723 is a selective, brain-permeable, orally acitve small-molecule inhibitor of Hsp90 (IC50=14 nM) that inhibits alpha-synuclein oligomerization with EC50 of 48 nM; induces Hsp70 (IC50=31 nM), and decreases expression of several known Hsp90 client proteins:HER2 (IC50=9.4 nM), ribosomal protein s6 (pS6) (IC50=13 nM), and PERK (IC50=5.5 nM); shows significant brain concentrations along with induction of brain Hsp70 in vivo with promising PK properties.

PC-60497

SM253

1610546-52-5

SM253 (SM 253, SM-253) is a novel potent Hsp90 inhibitor that does not induce heat shock response; demonstrates cytotoxicity to both HCT-116 and MiaPaCa-2 cells lines with IC50 of 5 and 5.5 uM, respectively; also induces apoptosis and significantly increases caspase 3/7 activity compared to 17-AAG (2-fold); binds to the N-middle linker region of Hsp90, resulting in reduced client protein activation and preventing C-terminal co-chaperones and client proteins from binding to Hsp90; exhibits antiproliferative and pro-apoptotic activity in multiple prostate cancer cell lines (LNCaP, 22Rv1, and PC-3) at low micromolar concentrations.

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