HSP Inhibitor

Kongensin A is a natural product isolated from Croton kongensis. Kongensin A is an effective, covalent HSP90 inhibitor that blocks RIP3-dependent necroptosishas. Kongensin A is a potent necroptosis inhibitor and an apoptosis inducer. Kongensin A has potential anti-necroptosis and anti-inflammation applications.

Tanespimycin (Standard) is the analytical standard of Tanespimycin. This product is intended for research and analytical applications. Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC₅₀ of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression.

Apatorsen is a 2'-methoxyethyl-modified antisense oligonucleotide and also a Hsp27 inhibitor. Apatorsen reduces Hsp27 mRNA and protein levels, impairs stress-induced cytoprotective functions, induces cell apoptosis, inhibits tumor growth and prevents metastasis. Apatorsen is applicable to research related to non-small cell lung cancer, castration-resistant prostate cancer, breast cancer, ovarian cancer and bladder cancer.

KUNG65 is a selective inhibitor of Grp94, with a target K_d of 540 nM and at least 73 fold selectivity vs. the other Hsp90 isoforms.

2-Chloro-ADP (2-Chloroadenosine 5′-diphosphate) sodium (10 mM) is a Adenosine 5'-diphosphate (ADP; HY-W010918) derivative that induces human platelet aggregation and inhibits stimulated adenylate cyclase. 2-Chloro-ADP sodium (10 mM) inhibits mortalin nucleotide-binding domain (NBD) with a K_i of 45.05 μM.

Geldanamycin (Standard) is the analytical standard of Geldanamycin. This product is intended for research and analytical applications. Geldanamycin is a Hsp90 inhibitor with antimicrobial activity against many Gram-positive and some Gram-negative bacteria. Geldanamycin has anti-influenza virus H5N1 activities.

[Au(TPP)]Cl inhibits the refolding activity of the Hsp60-Hsp10 complex with significant anticancer activities.

Anti-Human/Mouse GRP78 Antibody (C38) is a kind of mouse IgG2b antibody inhibitor, targeting to GRP78. Anti-Human/Mouse GRP78 Antibody (C38) inhibits RhoA, ROCK and AKT activation. Anti-Human/Mouse GRP78 Antibody (C38) can be used for the researches of cancer and metabolic disease, such as melanoma and diabetes.

Apidaecin IA is a basic peptide. Apidaecin IA inhibits the enzymatic activity of DnaK. Apidaecin IA induces bacterial cell death. Apidaecin IA can be used in research related to peritonitis and bacterial infections.

1,6-Dimethoxyhexane is an aliphatic ether that serves as a PROTAC linker and fuel additive. 1,6-Dimethoxyhexane is an orally active testicular toxicant. It has no direct toxicity on its own, but exerts toxicity after oxidative metabolism by liver/testicular microsomes to produce 2-Methoxyacetic Acid (MAA). 1,6-Dimethoxyhexane induces apoptosis/necrosis of pachytene spermatocytes, downregulates the expression of HSP70.2, HSP60 and ERp60/PDI A3, and causes spermatogenic tubule degeneration, testicular/thymic atrophy, a sharp decline in epididymal sperm density, and other effects. 1,6-Dimethoxyhexane can be used in studies related to testicular toxicity.

NDNA4 (compound 17) is a selective inhibitor of Hsp90α (IC₅₀: 0.34 μM). NDNA4 is a permanently charged analog with low membrane permeability and low cytotoxicity against Ovcar-8 and MCF-10A ((IC₅₀ >100 μM)). NDNA4 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins.

KHS101 is a blood-brain barrier-penetrant anticancer agent that primarily functions by inhibiting HSPD1 (IC₅₀ = 14.4 μM) and TACC3 across different cellular backgrounds. KHS101 promotes the aggregation of HSPD1 with client proteins, destabilizes TACC3, and reduces the levels of TACC3, Aurora A and PLK1. KHS101 induces autophagy, apoptosis, cell cycle exit and neuronal differentiation; it suppresses cancer cell growth, motility, EMT and stemness; it also impairs mitochondrial bioenergetics and glycolysis in glioblastoma cells. KHS101 can be used in research related to glioblastoma multiforme and breast cancer.

AR/AR-V7 degrader-1 is an orally active AR and AR-V7 degrader. AR/AR-V7 degrader-1 disrupts the interaction between AR/AR-V7 and HSP90, leading to their ubiquitination and degradation in castration-resistant prostate cancer cells. AR/AR-V7 degrader-1 regulates the expression of cell cycle-related proteins in prostate cancer cells (downregulates CDK4, CDK6, Cyclin D1, Cyclin E1; upregulates P21) and induces G0/G1 phase arrest. AR/AR-V7 degrader-1 inhibits the proliferation and migration of prostate cancer cells. AR/AR-V7 degrader-1 suppresses the growth of castration-resistant prostate cancer tumors in nude mice and induces the degradation of AR and AR-V7 in tumor tissues. AR/AR-V7 degrader-1 is applicable to the research of castration-resistant prostate cancer.

Apidaecin IA acetate is a basic peptide. Apidaecin IA acetate inhibits the enzymatic activity of DnaK. Apidaecin IA acetate induces bacterial cell death. Apidaecin IA acetate can be used in research related to peritonitis and bacterial infections.

Hsp90-Cdc37-IN-2 (Compound 41) is an inhibitor for the interaction between heat shock protein 90 (Hsp90) and cyclin 37 (Cdc37). Hsp90-Cdc37-IN-2 inhibits the proliferation of cancer cell A549, MCF-7, HOS and HepG2 with IC₅₀ of 0.41-0.94 μM. Hsp90-Cdc37-IN-2 decreases the mitochondrial membrane potential, induces apoptosis, and arrest cell cycle at G0/G1 phase in A549.

CH5164840 (16) shows high binding affinity for N-terminal Hsp90a (K_d = 0.52 nM) and strong anti-proliferative activity against human cancer cell lines (HCT116 IC₅₀ = 0.15 μM, NCI-N87 IC₅₀ = 0.066 μM). CH5164840 (16) is orally active (t_1/2 = 2.64 h) with potent antitumor efficacy.

HA15-Biotin is a chemical probe that consists of HA15 and biotin attached on the amide part of HA15. HA15-Biotin exhibits similar levels of activity to HA15. HA15-Biotin can be used for proteomic analysis.

17-Demethoxy-reblastatin (17-DR) is an inhibitor for heat shock protein 90 (Hsp90), with an IC₅₀ of 1.82 μM for yeast Hsp90 ATPase. 17-Demethoxy-reblastatin inhibits the proliferation of cancer cell HepG2 and SMMC7721, reduces the colony formation, and induces apoptosis through mitochondria and caspase mediated pathway.

NDNA3 (compound 14) is a selective inhibitor of Hsp90α (IC₅₀: 0.51 μM). NDNA3 is a permanently charged analog with low membrane permeability and low toxicity to Ovcar-8 (IC₅₀: 12.66 μM) and MCF-10A (IC₅₀: 11.72 μM) cells. NDNA3 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins.

HSP90-IN-19 is an effective heat shock protein 90 (Hsp90) inhibitor. HSP90-IN-19 has effective Hsp90 inhibitory activity with an IC₅₀ value of 0.27 μM. HSP90-IN-19 can be used for the research of viral infection, neurodegenerative disease, and inflammation.