HSP Inhibitor

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.

EGFR-IN-182 (Compound 4) is an EGFR inhibitor with an IC₅₀ value of 199 nM. EGFR-IN-182 inhibits HSP90 and PI3K, with IC₅₀ values of 5.007 and 13.596 μM respectively. EGFR-IN-182 exhibits strong anti-proliferative activity against MCF-7 and MDA-MB-231 cells. EGFR-IN-182 downregulates Cyclin D1, inducing cell cycle arrest; it enhances the activity of caspase-9, inducing cell apoptosis. EGFR-IN-182 downregulates the expressions of ERK and AKT. EGFR-IN-182 can be used for research on breast cancer.

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.

HSP90-IN-9 is a potent and selective HSP90 inhibitor. HSP90-IN-9 displays a fungicidal effect in a dose-dependent manner. HSP90-IN-9 inhibits fungal biofilm formation and fungal morphological changes after being combined with FLC. HSP90-IN-9 recovers FLC resistance by down-regulating the expression of related genes (ERG11, CDR1 and CDR2).

Hsp110-STAT3 PPI-IN-2 (compound 10b) is a Hsp110-STAT3 interaction disruptor. Hsp110-STAT3 PPI-IN-2 can be used in pulmonary arterial hypertension (PAH) related research.

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

MAO A/HSP90-IN-2 (compound 4-C) is a dual inhibitor of HSP90and MAO A with the IC₅₀ values of 0.016 and 4.58 μM, respectively. MAO A/HSP90-IN-2 increases HSP70 expression and reduces HER2 and phospho-Akt expression, and decreases IFN-γ induced PD-L1 expression in GL26 cells. MAO A/HSP90-IN-2 inhibits the growth of Temozolomide (HY-17364) -sensitive and -resistant GBM cells, colon cancer, leukemia, non-small cell lung and other cancers, and has potential to inhibit tumor immune escape^[1].

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.

Hsp90-IN-41 (Compound C1) is an inhibitor of Hsp90 (IC₅₀ = 0.044 μM). Hsp90-IN-41 exhibits antifungal and antitumor (IC₅₀ = 0.049 μM) activities in vitro.

HDAC/HSP90-IN-3 (compound J5) is a potent and selective fungal Hsp90 and HDAC dual inhibitor, with IC₅₀ values of 0.83 and 0.91 μM, respectively. HDAC/HSP90-IN-3 shows antifungal activity against azole resistant C. albicans. HDAC/HSP90-IN-3 can suppress important virulence factors and down-regulate drug-resistant genes ERG11 and CDR1.

Hsp90-IN-44 (compound 16) is a Hsp90 inhibitor with an IC₅₀ of 9.8 µM. Hsp90-IN-44 can be used for cancer research.

17-AEP-GA, an HSP90 antagonist, is a potent inhibitor of glioblastoma cell proliferation, survival, migration and invasion. ADCs Toxin.

GRP78-IN-1 exhibits several interactions with GRP78 residues with binding energy of -8.07 kcal/mol. GRP78-IN-1 shows the potent cytotoxic, anti-proliferative in cancer cells. GRP78-IN-1 exhibits promising apoptosis in breast cancer cells and stalls wound healing properties.

HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC₅₀ values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice.

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).