UNC9036
UNC9036 is a STING PROTAC degrader with a DC50 value of 227 nM. UNC9036 binds to and activates STING, recruits the VHL E3 ligase to target phosphorylated STING for ubiquitination and proteasomal degradation. UNC9036 inhibits downstream innate immune signaling events triggered by cytoplasmic DNA sensing, including IRF3 phosphorylation. UNC9036 reduces the antiviral response of cells infected with HSV-1. UNC9036 can be used in the research of renal cell carcinoma.
(Pink: STING ligand (HY-184545); Blue: VHL ligand (HY-138678B); Black: linker (HY-W105727)).
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- CAS 番号: 3094059-54-5
- 分子式: C73H95N17O11S
- 分子量:1418.71
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
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生物活性
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VHL |
HSV-1 |
UNC9036 (0-31.6 μM; 0-24 h) potently degrades STING in Caki-1 renal cell carcinoma cells with a DC50 of 227 nM and achieves 91.68% maximal degradation after 24 h, with significant degradation detectable within 8 h[1].
UNC9036 (5 μM; 24 h) degrades wild-type, cGAMP binding-deficient (R238A), and TBK1 phosphorylation-deficient (S366A) STING, but does not degrade trafficking-deficient (EDAA) or palmitoylation/activation-deficient (CACA) STING in Caki-1 renal cell carcinoma cells[1].
UNC9036 (0.316 μM; 6 h) dampens STING-mediated DNA sensing signaling in Caki-1 renal cell carcinoma cells by reducing STING protein levels and suppressing ISD90-induced and 2'3'-cGAMP-induced IRF3 phosphorylation, while having minimal effect on poly(I:C)-induced IRF3 phosphorylation[1].
UNC9036 (3 μM; 16 h) treatment significantly reduces the anti-viral response in Caki-1 renal cell carcinoma cells infected with HSV-1, as evidenced by increased viral titers compared to DMSO control[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Caki-1 renal cell carcinoma cells
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Concentration:0-31.6 μM (dose-response); 1 μM (time-course)
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Incubation Time:24 h (dose-response); 0-24 h (time-course)
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Result:Triggered dose-dependent and time-dependent degradation of STING protein.
Achieved a DC50 of 227 nM and a Dmax of 91.68% after 24 h treatment.
Induced significant STING degradation within 8 h of treatment with 1 μM.
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Cell Line:Caki-1 renal cell carcinoma cells (transfected with Flag-tagged wild-type or mutant STING)
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Concentration:5 μM
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Incubation Time:24 h
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Result:Degraded wild-type STING, R238A (2'3'-cGAMP binding-deficient) mutant, and S366A (TBK1 phosphorylation-deficient) mutant.
Failed to degrade EDAA (trafficking-deficient) mutant and CACA (palmitoylation/activation-deficient) mutant.
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Cell Line:Caki-1 renal cell carcinoma cells
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Concentration:0.316 μM UNC9036; 5 μg/mL ISD90, 5 μg/mL 2'3'-cGAMP, 5 μg/mL poly(I:C)
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Incubation Time:6 h pre-incubation; 0-6 h stimulation
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Result:Reduced STING protein abundance.
Suppressed ISD90-induced and 2'3'-cGAMP-induced phosphorylated IRF3 signals.
Minimally affected poly(I:C)-induced phosphorylated IRF3 signals.
化学情報
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CAS 番号 3094059-54-5
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分子量 1418.71
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分子式 C73H95N17O11S
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SMILES
O=C(NCCCCCCCCC(N[C@@H](C(N1[C@H](C(NCC2=CC=C(C=C2)C3=C(C)N=CS3)=O)C[C@H](C1)O)=O)C(C)(C)C)=O)C4=CC5=C(C(OC)=C4)N(C/C=C/CN6C(NC(C7=CC(C)=NN7CC)=O)=NC8=C6C(OCCCN9CCOCC9)=CC(C(N)=O)=C8)C(NC(C%10=CC(C)=NN%10CC)=O)=N5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
UNC9036 関連分類
HY-158048 関連分類
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