hsp70-in-1

HSP70-IN-1 is a heat shock protein (HSP) inhibitor that suppresses the growth of Kasumi-1 cells with an IC50 of 2.3 μM.

USP1-IN-11 (compound 38-P2) is a selective, reversible, and non-competitive inhibitor of USP1 (Ubiquitin-specific protease 1). It activates the DDR (DNA damage repair) pathway, leading to cell cycle arrest and apoptosis, thereby inhibiting cell survival. USP1-IN-11 increases sensitivity to Olaparib in drug-resistant cells and works synergistically with Andrographolide in cancer cells with functional BRCA. In the MDA-MB-436 xenograft model, USP1-IN-11 demonstrates significant dose-dependent antitumor activity.

TRC051384 is a heat shock protein 70 (HSP70) inducer that reduces stroke-associated neuronal damage and increases survival in a rat model of transient ischemic stroke, activates heat shock factor-1 and leads to elevated molecular chaperone and anti-inflammatory activity, and enhances Hsp72 expression in neurons and glial cells.

HDAC/HSP90-IN-1 (compound 20) is a potent dual inhibitor targeting HDAC (IC50 = 194 nM) and HSP90 (HSP90α IC50 = 153 nM). It induces the expression of HSP70, downregulates HSP90 substrate proteins, and enhances the acetylation of α-tubulin and histone H3 in cancer cells. Additionally, HDAC/HSP90-IN-1 reduces PD-L1 expression in IFN-γ-treated H1975 cells. This compound is applicable in research on cancers such as lung and colon cancer.

TRC051384 is an inducer of heat shock protein Hsp70, activating heat shock factor-1 and enhancing Hsp72 expression in neurons and glial cells.

DL-Sulforaphane N-acetyl-L-cysteine (SFN-NAC), a metabolite of sulforaphane, induces apoptosis through down-regulation of α-microtubulin and phosphorylation of ERK1/2-mediated Stathmin-1, and up-regulation of Hsp70 through phosphorylation of ERK1/2 in non-small-cell lung cancer (NSCLC).

YM-1 is an HSP70 modulator and an allosteric inhibitor. It promotes the degradation of client proteins (e.g., Akt, Raf-1), used for cancer and antiviral research.

HSP70-IN-3, a potent inhibitor of HSP70 with IC50 values of 1.1 μM in ASZ001 cells and 1.9 μM in C3H10T1/2 cells, exhibits anti-Hedgehog (Hh) signaling and anti-proliferative activities. Furthermore, it reduces the expression of the oncogenic transcription factor GLI1 [1].

MAO A/HSP90-IN-2 (compound 4-C), a dual inhibitor of HSP90 and MAO A, exhibits IC50 values of 0.016 μM for MAO A and 4.58 μM for HSP90. This compound enhances HSP70 expression, diminishes HER2 and phospho-Akt levels, downregulates IFN-γ-induced PD-L1 expression in GL26 cells, and demonstrates efficacy against Temozolomide-sensitive and -resistant GBM cells, colon cancer, leukemia, and non-small cell lung cancer, possibly impeding tumor immune evasion [1].

HSP70/SIRT2-IN-2 (Compounds 1a), a dual inhibitor of SIRT2 and HSP70, exhibits an IC50 of 45.1±5.0 μM against SIRT2 and demonstrates antitumor activity [1].

HSP70/SIRT2-IN-1 (Compound 2a) serves as a dual inhibitor targeting both SIRT2 and HSP70, exhibiting an IC50 of 17.3±2.0 μM against SIRT2. This compound possesses antitumor activity [1].