Hsp70TAC PD-1 Degrader-2 

Hsp70TAC PD-1 Degrader-2 is a PD-L1 Hsp70TAC (Hsp70-targeting Chimeras) degrader with K_d values of 0.36 μM. Hsp70TAC PD-1 Degrader-2 forms a ternary complex with Hsp70 and PD-L1 to drive PD-L1 degradation. Hsp70TAC PD-1 Degrader-2 induces degradation of mature membrane-bound PD-L1 in an Hsp70-dependent manner and via caveolin-mediated endocytosis and lysosomal trafficking. Hsp70TAC PD-1 Degrader-2 accumulates preferentially in tumor cells with elevated Hsp70 expression for tumor-selective PD-L1 degradation. Hsp70TAC PD-1 Degrader-2 can be used for the research of cancer, such as breast invasive carcinoma, glioblastoma multiforme, diffuse large b-cell lymphoma^[1]. (Pink: PD-1/PD-L1 ligand (HY-19745A); Blue: Hsp70 ligand (HY-182979); Black: linker (HY-182982)).

Hsp70TAC PD-1 Degrader-2 (Compound SP-2) (6.25-100 μM) binds to purified Hsp70 with a K_D of 4.18 μM and to purified PD-L1 with a K_D of 0.36 μM^[1].
Hsp70TAC PD-1 Degrader-2 (0.1-10 μM; 4-24 h) induces time- and dose-dependent degradation of PD-L1 in MDA-MB-231 cells (DC₅₀ = 0.84 μM) and U-87 MG cells (DC₅₀ = 1.23 μM)^[1].
Hsp70TAC PD-1 Degrader-2 (1-5 μM; 24 h) effectively degrades mature membrane-bound PD-L1 in MDA-MB-231 cells^[1].
Hsp70TAC PD-1 Degrader-2 (1 μM; 2-12 h) induces PD-L1 degradation in MDA-MB-231 cells via a lysosome-dependent pathway, which requires formation of a PD-L1-SP-2-Hsp70 ternary complex^[1].
Hsp70TAC PD-1 Degrader-2 (1 μM; 12 h)-mediated PD-L1 degradation in MDA-MB-231 cells is dependent on Hsp70 expression and caveolin-mediated endocytosis^[1].
Hsp70TAC PD-1 Degrader-2 (1-5 μM; 12 h) selectively induces PD-L1 degradation in Hsp70-overexpressing tumor cells (MDA-MB-231, U-87 MG, MCF-7, U937), but not in low Hsp70-expressing normal cells (HEK293T, MEF) or TE-1 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

950.24

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• [1]. Wang Z, et al. Hsp70-Targeting Chimeras Enable Dual Proteasomal and Lysosomal Degradation of Intracellular and Extracellular Proteins. J Med Chem. 2026;69(7):8417-8432.  [Content Brief]