PCC16 chloride
PCC16 chloride is a dual PROTAC degrader targeting DHHC3 and PD-L1, with a DC50 of 0.103 μM for PD-L1 degradation. PCC16 chloride induces DHHC3 degradation via the ubiquitin-proteasome pathway by recruiting the CRBN E3 ubiquitin ligase (E3 ubiquitin ligase). By targeting DHHC3-which is essential for PD-L1 palmitoylation and membrane stability-PCC16 chloride reduces PD-L1 levels, decreases PD-L1 membrane retention time, and impairs its immunosuppressive function. PCC16 chloride enhances anti-tumor immunity by disrupting PD-L1-mediated immunosuppression. PCC16 chloride can be used in the research of immune checkpoint blockade-resistant cancers.
(Pink: DHHC3 ligand (HY-169235); Blue: Cereblon ligand (HY-10984); Black: linker (HY-169236)).
For research use only. We do not sell to patients.
- Formula: C206H322ClN67O60S
- Molecular Weight:4764.69
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
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DHHC3 |
PD-L1 0.103 μM (DC50) |
PCC16 (0.1-50 μM; 6 h) chloride degrades DHHC3 and PD-L1 in C33A cells with a DC50 of 0.103 μM for PD-L1 degradation, showing potent activity even at 0.1 μM after 6-hour incubation[1].
PCC16 (1 μM; 1-24 h) chloride induces significant degradation of DHHC3 and PD-L1 in C33A cells after 4-hour incubation, with greater degradation observed at extended incubation times up to 24 h[1].
PCC16(0.1-50 μM) chloride reduces PD-L1 protein levels in a concentration-dependent manner in U14, CT26, and B16F10 cells[1].
PCC16 (2.5 μM; 6 h) chloride colocalizes with DHHC3 protein in C33A cells, demonstrating stable binding affinity to the target[1].
PCC16 (0.5 μM) chloride binds to DHHC3 in C33A cells, increasing the protein's thermal stability and shifting its degradation temperature from 49 °C to 55 °C[1].
PCC16 (0.1-50 μM; 24 h and 1 μM; 1-24 h) chloride exhibits low cytotoxicity in C33A cells, with no significant reduction in cell viability observed at concentrations up to 50 μM (24-hour incubation) or over incubation times up to 24 h (1 μM concentration)[1].
PCC16 chloride enhances the sensitivity of C33A cells to cisplatin, significantly reducing cell proliferation and increasing apoptosis when combined with cisplatin treatment[1].
PCC16 (1-10 μM; 6 h) chloride increases IFN-γ and TNF-α secretion and enhances T-cell-mediated killing of C33A cells in a concentration-dependent manner in a T-cell-C33A co-culture system[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human cervical cancer (C33A) cells
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Concentration:0.1 μM; 0.5 μM; 5 μM; 10 μM; 50 μM
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Incubation Time:6 h
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Result:Induced significant degradation of DHHC3 and PD-L1 proteins at concentrations as low as 0.1 μM.
Achieved a DC50 value of 0.103 μM for PD-L1 degradation, representing the highest degradation activity among tested cp-PCCs.
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Cell Line:Human cervical cancer (C33A) cells
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Concentration:1 μM
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Incubation Time:1 h; 2 h; 4 h; 8 h; 12 h; 24 h
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Result:Required a minimum incubation period of 4 h to achieve statistically significant degradation of DHHC3 and PD-L1 proteins.
Increased degradation of both proteins with longer incubation times up to 24 h.
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Cell Line:Human cervical cancer (C33A) cells
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Concentration:2.5 μM
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Incubation Time:6 h
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Result:Colocalized with DHHC3 protein in C33A cells.
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Cell Line:Human cervical cancer (C33A) cells
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Concentration:0.1-50 μM (24 h incubation); 1 μM (1-24 h incubation)
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Incubation Time:24 h (0.1-50 μM); 1-24 h (1 μM)
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Result:Showed no significant differences in cell viability between PCC16 chloride-treated groups and the control group, even at concentrations up to 50 μM or incubation times up to 24 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 4764.69
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Formula C206H322ClN67O60S
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Sequence
{Rhodmine B}-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Cys-Gly-Ile-Gln-Asp-Thr-Asn-Ser-Lys-Lys-Gln-Ser-Asp-Thr-His-Leu-Glu-Glu-Thr-{Lys(pomalidomide-Suc-PEG2)}-NH2
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Sequence Shortening
{Rhodmine B}-YGRKKRRQRRRCGIQDTNSKKQSDTHLEET-{Lys(pomalidomide-Suc-PEG2)}-NH2
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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)