Hsp70TAC PD-1 Degrader-2
Hsp70TAC PD-1 Degrader-2 is a PD-L1 Hsp70TAC (Hsp70-targeting Chimeras) degrader with Kd 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. (Pink: PD-1/PD-L1 ligand (HY-19745A); Blue: Hsp70 ligand (HY-182979); Black: linker (HY-182982)).
For research use only. We do not sell to patients.
- Formula: C56H67N7O5S
- Molecular Weight:950.24
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
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HSP70 4.18 μM (Kd) |
Hsp70TAC PD-1 Degrader-2 (Compound SP-2) (6.25-100 μM) binds to purified Hsp70 with a KD of 4.18 μM and to purified PD-L1 with a KD 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.
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Cell Line:MDA-MB-231 (triple-negative breast cancer), U-87 MG (glioblastoma multiforme)
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Concentration:0.1, 0.5, 1, 5, 10 μM
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Incubation Time:4, 8, 12, 24 h
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Result:Induced time-dependent PD-L1 degradation starting at 8 h, with >80% depletion achieved at 24 h in both cell lines.
Yielded dose-dependent degradation with DC50 values of 0.84 μM in MDA-MB-231 cells and 1.23 μM in U-87 MG cells, with no observed "hook effect" at high concentrations.
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Cell Line:MDA-MB-231
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Concentration:1, 5 μM
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Incubation Time:24 h
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Result:Reduced cell surface PD-L1 fluorescence signal as shown by immunofluorescence.
Confirmed a significant reduction in PD-L1-positive cells after treatment with 1 μM SP-2 for 24 h, compared to the DMSO control via flow cytometry.
Chemical Information
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Molecular Weight 950.24
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Formula C56H67N7O5S
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SMILES
COC1=NC(OCC2=C(C(C3=CC=CC=C3)=CC=C2)C)=CC=C1CNCCNC(CCCCCCC(NCCN(CCNC4=C(C(C5=C6C(C(SC7CCCCC7)=CC=C46)=CC=C5)=O)C#N)C)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Hsp70TAC PD-1 Degrader-2 Related Classifications
HY-182959 Related Classifications
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