2. PROTAC Immunology/Inflammation Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. LYTACs PD-1/PD-L1 HSP
  4. dPDL1-4

dPDL1-4 is a potent and selective eHSPTAC eHSP90 PD-L1 degrader with DC50s of 7.77μM and 6.52 μM in HeLa and B16F10 cells. dPDL1-4 bridges eHSP90 with the target protein, inducing lysosomal degradation. dPDL1-4 can degrade PD-L1 significantly and inhibits tumor growth. dPDL1-4 can be used for the study of cervical cancer and melanoma. ((Pink: eHSP90 ligand (HY-174476); Blue: PD-L1 ligand (HY-116274); Black: Linker (HY-W021787); HSP ligand + linker: HY-174799)).

For research use only. We do not sell to patients.

dPDL1-4 Chemical Structure

dPDL1-4 Chemical Structure

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dPDL1-4 Related Antibodies

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Description

dPDL1-4 is a potent and selective eHSPTAC eHSP90 PD-L1 degrader with DC50s of 7.77μM and 6.52 μM in HeLa and B16F10 cells. dPDL1-4 bridges eHSP90 with the target protein, inducing lysosomal degradation. dPDL1-4 can degrade PD-L1 significantly and inhibits tumor growth. dPDL1-4 can be used for the study of cervical cancer and melanoma. ((Pink: eHSP90 ligand (HY-174476); Blue: PD-L1 ligand (HY-116274); Black: Linker (HY-W021787); HSP ligand + linker: HY-174799))[1].

In Vitro

dPDL1-4 (0-20 μM, 12-24 h) promotes degradation of membrane PD-L1 in an eHSP90-, ternary complex- and lysosome-dependent manner in HeLa and B16F10 cells[1].

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

dPDL1-4 Related Antibodies

Western Blot Analysissup>[1]

Cell Line: HeLa and B16F10 cells
Concentration: 0, 1, 3, 5, 10, 20 μM
Incubation Time: 12 h
Result: Induced dose- and time-dependent degradation of PD-L1 in HeLa cells (Dmax = 68%) and B16F10 cells (Dmax = 56%).

Western Blot Analysissup>[1]

Cell Line: B16F10 cells
Concentration: 5 μM
Incubation Time: 12 h
Result: Inhibited the degradation of membrane-associated PD-L1 by BMS-8 (HY-116274) or HSP90i-Ac.

Western Blot Analysissup>[1]

Cell Line: HeLa cells
Concentration: 10, 20 μM
Incubation Time: 24 h
Result: Inhibited the degradation of membrane-associated PD-L1 by Bafilomycin A1 (HY-100558) and Monensin (HY-N4302) but not by MG132 (HY-13259).
Parmacokinetics
Species Dose Route Indicator value
Rat 50 mg/kg i.v. AUC0-∞ 27866.1 μg/L·h
Rat 50 mg/kg i.v. T1/2 1.6 h
In Vivo

dPDL1-4 (50 mg/kg, i.p., every 2 days for 6 doses) effectively degrades PD-L1 and potently suppresses tumor growth in the B16F10 melanoma mouse model[1].

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

Animal Model: B16F10 melanoma syngeneic mouse model established by tumor-bearing mice (C57BL/6J, 6-7 weeks, female)[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection(i.p.), every 2 days for 6 doses.
Result: Suppressed tumor growth significantly, without causing notable weight loss.
Induced a remarkable decrease in the PD-L1 level among all the treatments.
Increased the percentage of activated cytotoxic T cells (CD8+cells).
Molecular Weight

1133.17

Formula

C60H74BrN7O10
SMILES

CC(C1=C(C=C(C(C2=NN=C(N2C3=CC=C(C=C3)CN4CCN(CC4)C(CCOCCOCCOCCOCCNC(C5CCCCN5CC6=CC=C(OCC7=C(C(C8=CC=CC=C8)=CC=C7)C)C(Br)=C6)=O)=O)O)=C1)O)O)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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dPDL1-4 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

dPDL1-4LYTACsPD-1/PD-L1HSPLysosome-targeting chimerasPD-1/Programmed death-ligand 1Heat shock proteinsCancereHSPTACsMC38HeLaC57BL/6J miceInhibitorinhibitorinhibit

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