HSP Inhibitor

HA15 (Standard) is the analytical standard of HA15 (HY-100437). This product is intended for research and analytical applications. HA15 is a potent and specific inhibitor of ER chaperone BiP/GRP78/HSPA5, inhibits the ATPase activity of BiP, with anti-cancerous activity.

2-Chloro-ADP (2-Chloroadenosine 5′-diphosphate) sis a Adenosine 5'-diphosphate (ADP; HY-W010918) derivative that induces human platelet aggregation and inhibits stimulated adenylate cyclase. 2-Chloro-ADP inhibits mortalin nucleotide-binding domain (NBD) with a K_i of 45.05 μM.

VER-82576 (Standard) is the analytical standard of VER-82576 (HY-10942). This product is intended for research and analytical applications. VER-82576 (NVP-BEP800) is a potent, orally available and selective Hsp90 inhibitor, with an IC₅₀ of 58 nM for Hsp90β; VER-82576 also slightly blocks Grp94 and Trap-1, with IC₅₀s of 4.1 and 5.5 μM, respectively.

C086, a novel potent Hsp90 inhibitor, could inhibit cell cycle progression and induce cell apoptosis and anti-metastasis by regulating various mechanisms in different cell types.

Ganetespib (Standard) is the analytical standard of Ganetespib. This product is intended for research and analytical applications. Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3.

SU086 is a chalcone-derived HSP90 inhibitor. SU086 interacts with HSP90, reduces HSP90 protein levels, and suppresses glycolysis in prostate cancer cells. SU086 can be used in research related to advanced prostate cancer and castration-resistant prostate cancer (CRPC).

Pifithrin-μ (Standard) is the analytical standard of Pifithrin-μ. This product is intended for research and analytical applications. Pifithrin-μ is an inhibitor of p53 and HSP70, with antitumor and neuroprotective activity.

Pochonin D ((+)-Pochonin D) is an inhibitor of heat shock protein 90 (Hsp90) with antiviral and anti-inflammatory activities. Pochonin D inhibits Hsp90, affects the homeostasis, folding and assembly processes of viral proteins, and reduces the replication capacity of viruses. Pochonin D is a copper ion carrier that can induce cuproptosis in triple-negative breast cancer cells by targeting PRDX1. Pochonin D reduces the infiltration of inflammatory cells, decreases the secretion of inflammatory cytokines such as TNF-α and IL-1β, and alleviates inflammatory responses. Pochonin D is a promising candidate for research on human rhinovirus (HRV) infection and cancer.

19-epi-Scholaricine is an orally active indole alkaloid. 19-epi-Scholaricine downregulates the expression of profibrotic/apoptotic proteins (HRAS, HSP90AA1, KDR) and upregulates the expression of cell cycle-related protein (CDK2). 19-epi-Scholaricine suppresses ROS production and reduces the release of inflammatory mediators, thereby attenuating podocyte apoptosis, renal inflammation and oxidative stress by inhibiting AKT/mTOR. 19-epi-Scholaricine can be used in the research of chronic glomerulonephritis and membranous nephropathy.

Caesappanin C, a biphenyl dimer from the ethanolic extract of the heartwood of Indonesian Caesalpinia sappan L., shows strong proliferation stimulating activity against the primary osteoblastic cells in vitro. Caesappanin C has the potential to stimulate bone formation and regeneration. Caesappanin C can effectively deactivate HSV particles and bind HSV surface glycoprotein B (gB) to inhibit membrane fusion.

Hsp90-IN-34 (compound HAM-1) is a compound that inhibits the Aha1-Hsp90 chaperone complex with a high affinity for Hsp90/Aha1 (K_Dapp=23.5 µM). Hsp90-IN-34 modulates the ATPase activity of Hsp90 by affecting the interaction between Hsp90 and Aha1.

Derrubone is a prenylated isoflavone Hsp90 inhibitor that binds to the C-terminal ATP site of Hsp90α, stabilizes the Hsp90-client protein co-chaperone complex, and induces client protein degradation, thereby inhibiting cancer cell proliferation. Derrubone can be used for research on breast cancer, colon cancer, Alzheimer's disease, and type 2 diabetes.

SNX-2112 (Standard) is the analytical standard of SNX-2112 (HY-10214). This product is intended for research and analytical applications. SNX-2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a K_d of 16 nM for Hsp90 and IC₅₀s of 30 nM, 30 nM for Hsp90 α and Hsp90 β, also induces Her-2 degradation, and inhibits Grp94 and Trap-1, with IC₅₀s of 10 nM, 4.275 μM and 0.862 μM, respectively. SNX-2112 (PF 04928473) binds Hsp90 isoforms Hsp90α, Hsp90β and Hsp90b1/Grp94 with Kds of 4 nM, 6 nM and 484 nM, respectively.

BIIB021 (Standard) is the analytical standard of BIIB021. This product is intended for research and analytical applications. BIIB021 (CNF2024) is an orally active, fully synthetic inhibitor of HSP90 with a Ki and an EC50 of 1.7 nM and 38 nM, respectively.

KNK437 (Standard) is the analytical standard of KNK437 (HY-100110). This product is intended for research and analytical applications. KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.

Hsp90-Cdc37-IN-1 (Standard) is the analytical standard of Hsp90-Cdc37-IN-1 (HY-111414). This product is intended for research and analytical applications. Hsp90-Cdc37-IN-1 is an Hsp90-Cdc37 interaction disruptor that inhibit cell migration and reverse agent resistance, with an IC₅₀ of 140 nM.

Gamitrinib TPP hexafluorophosphate (Standard) is the analytical standard of Gamitrinib TPP hexafluorophosphate (HY-102007A). This product is intended for research and analytical applications. Gamitrinib TPP hexafluorophosphate is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP hexafluorophosphate is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.

Displurigen (Standard) is the analytical standard of Displurigen (HY-111002). This product is intended for research and analytical applications. Displurigen (NSC375009) disrupts human embryonic stem cell pluripotency by targeting HSPA8. Displurigen inhibits ATPase activity of HSP70 (IC₅₀ = 225 μM).

PF-4942847 is an orally active HSP90 inhibitor with an IC₅₀ of approximately 50 nM. PF-4942847 induces apoptosis in osteosarcoma cells, increases the proportion of cells in the sub-G1 phase and PARP cleavage, reduces the expression of Akt, Erk, MYC, c-MET and STAT-3, and regulates HSP expression. PF-4942847 can be used in studies related to osteosarcoma and HSP90.

BIIB-028 is an orally active inhibitor for heat shock protein 90 (Hsp90). BIIB-028 targets the ATP-binding site of Hsp90, disrupts the function of Hsp90, leads to the degradation of client proteins, that are crucial for cancer cell survival and proliferation.