PD-L1/HDAC6-IN-1
PD-L1/HDAC6-IN-1 is an orally active dual inhibitor of PD-L1 and HDAC6, with IC50 values of 26.8 nM and 78 nM, respectively. PD-L1/HDAC6-IN-1 binds to human and murine PD-L1 proteins with high affinity, while it reduces STAT3 phosphorylation and downregulates PD-L1 expression by inhibiting HDAC6, thus blocking the PD-1/PD-L1 interaction. PD-L1/HDAC6-IN-1 exhibits potent anti-tumor activity in a mouse melanoma model. PD-L1/HDAC6-IN-1 is suitable for research on tumor immune regulation related to melanoma.
For research use only. We do not sell to patients.
- CAS No.: 2834094-36-7
- Formula: C27H33N3O3
- Molecular Weight:447.57
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HDAC6 69 nM (IC50) |
HDAC1 9.08 μM (IC50) |
PD-L1/HDAC6-IN-1 (HP29) (0.1-2.0 μM; 12 h) upregulates the level of acetylated α-tubulin in B16-F10 cells and Jurkat cells[1].
PD-L1/HDAC6-IN-1 (0.1-2.0 μM; 24 h) downregulates the expression of p-STAT3 and PD-L1 in B16-F10 cells[1].
PD-L1/HDAC6-IN-1 shows negligible cytotoxicity against B16-F10, HepG2, MCF-7 and Jurkat cells[1].
PD-L1/HDAC6-IN-1 (0.01-10 μM; 48 h) shows negligible cytotoxicity against HepG2 cells and Jurkat T cells, while dose-dependently increasing the mortality of HepG2 cells co-cultured with Jurkat T cells with an IC50 of 3.4 μM[1].
PD-L1/HDAC6-IN-1 dose-dependently activates luciferase activity in PD-1/PD-L1 NFAT reporter assay (EC50 = 3.15 μM)[1].
PD-L1/HDAC6-IN-1 binds to human PD-L1 and murine PD-L1 with KD values of 179 nM and 73 nM in the ITC assay, and 464 nM and 55.3 nM in the SPR assay, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | T1/2α | Tmax | Vz/F | CLz/F | Cmax | F |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 871.62 μg/L·h | 1076.36 μg/L·h | 15.32 h | 19.29 h | 13.19 h | 5.55 h | 31.91 L/kg | 1.5 L/h/kg | 193.69 μg/L | 15.3 % |
| Mice[1] | 2 mg/kg | i.v. | 1135.33 μg/L·h | 1291.42 μg/L·h | 7.06 h | 7.12 h | 6.9 h | 0.08 h | 8.99 L/kg | 0.97 L/h/kg | 638.14 μg/L | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2834094-36-7
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Molecular Weight 447.57
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Formula C27H33N3O3
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SMILES
CC1=C(C=CC=C1C2=CC=CC=C2)C3=NC(OC)=C(C=C3)CNCCCCCCC(NO)=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)
PD-L1/HDAC6-IN-1 Related Classifications
HY-172200 Related Classifications
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