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.

HSP70 ligand 1 is an HSP70 ligand and acts as a ligand for the PROTAC target protein. It is utilized in the synthesis of PROTACHSP70 Degrader-1.

PROTAC HSP70 Degrader-1 (compound C4) is an intracellular HSP70 and CRBN ligand that forms a ternary complex by binding to CRBN. This compound facilitates the ubiquitination and proteasomal degradation of cytoplasmic HSP70. It exhibits cytotoxic activity against cancer cells, inhibiting tumor cell proliferation and inducing apoptosis when used in combination with DTHIB. PROTAC HSP70 Degrader-1 is applicable in research on colon cancer and leukemia.

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].

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].