HSP Inhibitor

HSP90-IN-32 is a Hsp90 C-terminal inhibitor that displays anti-proliferative activities against SKMel173, SKMel103, SKMel19 and A375 cells with IC₅₀ values of 1.01 μM, 0.782 μM, 0.607 μM and 1.413 μM , respectively. HSP90-IN-32 is promising for research of anti-cancer agents.

HSP90-IN-25 (compound 4a) is an HSP90 inhibitor that specifically inhibits the ATPase activity of HSP90.

HSF1 Human Pre-designed siRNA Set A contains three designed siRNAs for HSF1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

TCI 18 is a ligand of HSP72 with a K_i value of 4.7 μM. TCI 18 forms a covalent bond with Lys56 residue of HSP72 via a process involving initial reversible binding, conversion to a pre-covalent complex, and subsequent covalent bond formation. TCI 18 addresses the undruggable target HSP72.

Hsp90-IN-39 (Compound 16t) is a HSP90 inhibitor with notable selectivity for the HSP90α isoform. Hsp90-IN-39 demonstrates significant antiproliferative activity in various cancer cell lines, including MCF-7, HCT116, SKBr3, K562, and A549. Hsp90-IN-39 holds potential for cancer research.

HSF1-IN-1 (page 71, compound 1) is a heat shock factor 1 (HSF1) inhibitor. HSF1-IN-1 inhibit stress-induced expression from heat shock gene promoters. HSF1-IN-1 can be used for the study of cancer.

Alvespimycin (17-DMAG) TFA is a potent inhibitor of Hsp90, binding to Hsp90 with an EC₅₀ of 62 nM.

GR-25 is an orally active, selective Hsp90p inhibitor.

TRAP1-IN-2 is a TRAP1-selective inhibitor, with a K_d value of 0.04 μM against human TRAP1. TRAP1-IN-2 exhibits more than 250-fold selectivity for Grp94 and shows no detectable affinity for cytosolic Hsp90α/β. TRAP1-IN-2 selectively induces the degradation of TRAP1 client proteins by inhibiting its ATPase activity, without triggering the heat shock response or affecting cytosolic Hsp90 client proteins. TRAP1-IN-2 suppresses oxidative phosphorylation, shifts cellular metabolism toward glycolysis, disrupts the stability of the TRAP1 tetramer and the mitochondrial membrane potential. TRAP1-IN-2 can be used in studies related to prostate cancer, cervical cancer, and ovarian cancer.

KU-32 is a novel, novobiocin-based Hsp90 inhibitor that can protect against neuronal cell death.

Apatorsen sodium scrambled negative control is the sequence scrambled negative control of Apatorsen sodium.

Hsf1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Hsf1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

HSP90i is a HSP90 inhibitor. HSP90i can be used as a drug intermediate to synthesize LYTACs, such as dPDL1-4 (HY-174468).

KW-2478 hydrochloride is an HSP90 inhibitor (IC₅₀ = 3.8 nM). KW-2478 hydrochloride inhibits the growth and induces apoptosis in chronic myeloid leukemia (CML) cells and liver cancer cells. KW-2478 hydrochloride weakens the BCR/ABL and MAPK signaling pathways, leading to increased p27 and p21 expression and decreased cyclin B1 expression. KW-2478 hydrochloride downregulates STAT3 expression. KW-2478 hydrochloride may be used in research on cancers such as CML and liver cancer.

STA-2842 is an inhibitor of heat shock protein HSP90 with potential to inhibit autosomal dominant polycystic kidney disease (ADPKD). ADPKD is caused by inherited mutations in the PKD1 or PKD2 genes that abnormally activate multiple signaling proteins and pathways that regulate cell proliferation. STA-2842 can significantly reduce initial renal cyst formation and kidney growth in mice, and slow disease progression in mice with existing cysts.

Hsp90β-IN-1 (Compound 7b) is a selective biotinylated inhibitor of heat shock protein 90β (HSP90β) with an IC₅₀ = 0.33 μM.

SST0116CL1 is a HSP90 inhibitor (IC₅₀: 0.21 μM). SST0116CL1 binds to the ATP binding pocket of Hsp90, and interferes with Hsp90 chaperone function thus resulting in client protein (EGFR, CDK4 and AKT) degradation. SST0116CL1 induces degradation of Her2 in BT-474 cell (IC₅₀: 0.2 μM). SST0116CL1 has antiproliferative activity and inhibits tumor growth. SST0116CL1 can be used for the study of leukemia, gastric and ovarian carcinoma.

HSP90-IN-10 (Compound 16s) is a potent inhibitor of HSP90. HSP90-IN-10 exhibits high antiproliferative potency against HCC1954 breast cancer cells with the IC₅₀ value of 6 µM. HSP90-IN-10 does not inhibit the growth of normal epithelial cells. HSP90-IN-10 also induces apoptosis.

HSP70-IN-3 is a potent HSP70 inhibitor (IC₅₀s of 1.1 and 1.9 μM in ASZ001 and C3H10T1/2, respectively). HSP70-IN-3 has anti-Hh (Hedgehog signaling) activity and anti-proliferative activity and reduces expression of the oncogenic transcription factor GLI1.

Androgen receptor degrader-6 is a blood-brain barrier-permeable AR degrader. Androgen receptor degrader-6 inhibits the chaperone activity of HSP27 and disrupts the HSP27-AR complex. Androgen receptor degrader-6 promotes the degradation of wild-type and mutant AR, reduces AR protein levels, and inhibits the growth of glioblastoma cells. Androgen receptor degrader-6 can be used in glioblastoma research.