TP1L
TP1L is a potent and selective T-cell protein tyrosine phosphatase (TC-PTP) PROTAC degrader, with a DC50 value of 35.8 nM. TP1L elevates the phosphorylation level of TC-PTP substrates including pSTAT1 and pJAK1. TP1L selectively enhances IFN-γ signaling and increases MHC-I expression. TP1L activates TCR signaling through increases phosphorylation of LCK. TP1L enhances CAR-T cell mediated tumor killing efficacy through activation of the CAR-T cells. TP1L can be used for the study of cancer. (Pink: TC-PTP ligand: (HY-138964), Blue: E3 ligase CRBN Ligand (HY-A0003), Black: Linker: (HY-140002)).
(Pink: TC-PTP ligand (HY-138964); Blue: Cereblon ligand (HY-A0003); Black: linker (HY-140002)).
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- 화학식: C64H81F2N8O14P
- 분자량:1255.34
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보관:
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
- 순도&문서
- References
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Help & FAQs
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Biological Activity
TP1L (0.5-4000 nM, 3-24 h) selectively degrades TC-PTP depends on the ubiquitination-proteasome pathway (DC50 = 35.8 nM) in HEK293 cells[1].
TP1L (< 10 μM) shows no significant inhibition towards other PTPs even at up to 10 μM TP1L concentration[1].
TP1L (3.9-4000 nM, 16 h) selectively enhances IFN-γ signaling and promotes antigen presentation in HEK293 cells[1].
TP1L (62.5-1000 nM, 16 h) elevates pLCK in Jurkat T-cells and enhances CAR-T cells killing efficiency in a KB tumor/CAR-T cell coculture system [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells and Jurkat T-cells
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Concentration:0.5, 3.9, 7.8, 15.6, 31.2, 62.5, 125, 250, 500, 1000, 2000, 4000 nM
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Incubation Time:3, 6, 16, 24 h
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Result:Degradated TC-PTP with a DC50 of 35.8 nM in HEK293 cells after 16 hours of treatment.
Showed no signicantly altered on the level of PTP1Bat up to 4 mM concentration.
Degradated TC-PTP completly within 6 hours.
Did not decrease during the entire period of TP1L treatment.
Enhanced the levels of pJAK1 and pSTAT1.
Did not affected the phosphorylation level of JAK2, which is a substrate of PTP1B.
Degraded TC-PTP and promoted phosphorylation of LCK in Jurkat T-cells.
Chemical Information
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분자량 1255.34
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화학식 C64H81F2N8O14P
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SMILES
FC(C1=CC=C(C[C@H](NC([C@@H](NC(CO[C@@H]2[C@@H](C(C)C)CC[C@H](C)C2)=O)CC3=CC=CC=C3)=O)C(N[C@@H](CCCCNC(C4=CC=C(CC)C=C4)=O)C(NCCOCCC(NC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)=O)=O)=O)C=C1)(P(O)(O)=O)F
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TP1L Related Classifications
HY-160151 Related Classifications
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