ZXH-4-137
ZXH-4-137 is a CRBN PROTAC degrader. ZXH-4-137 brings CRBN and VHL E3 ligase into proximity, induces CRBN ubiquitination and proteasomal degradation, and exhibits high selectivity for CRBN. ZXH-4-137 blocks the degradation of CRBN-dependent target proteins such as GSPT1 and CDK9. ZXH-4-137 serves as a chemical knockdown tool compound for investigating CRBN-dependent biological processes.
(Pink: Cereblon ligand (HY-103596); Blue: VHL ligand (HY-112078); Black: linker (HY-132859)).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2711006-74-3
- 分子式: C47H60N6O9S
- 分子量:885.08
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
Cereblon |
VHL |
体外実験
ZXH-4-137 (10-500 nM; 1-24 h) potently and selectively induces CRBN degradation in MM1.S cells[1].
ZXH-4-137 (50 nM; 2 h pre-treatment) mediates the knockdown of CRBN in MM1.S cells, and this effect blocks the CRBN-dependent degradation of GSPT1 by CC-885 (HY-101488)[1].
Knockdown of CRBN in MOLT-4 cells mediated by ZXH-4-137 (0.1 μM; 2 h pre-treatment) partially blocks the CRBN-dependent degradation of CDK9 induced by THAL-SNS-032 (HY-123937)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MM1.S multiple myeloma cells
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Concentration:10 nM, 50 nM, 100 nM, 500 nM
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Incubation Time:4 h
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Result:Reduced CRBN levels to 44% of DMSO control at 10 nM, 31% at 50 nM, 16% at 100 nM, and 17% at 500 nM after 4 hours.
Did not significantly alter levels of Ikaros, Aiolos, CK1α, pVHL30, or pVHL19 at any tested concentration.
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Cell Line:MM1.S multiple myeloma cells
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Concentration:50 nM
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Incubation Time:1 h, 2 h, 4 h, 8 h, 16 h, 24 h
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Result:Reduced CRBN levels to 58% of DMSO control at 1 h, 41% at 2 h, 23% at 4 h, 17% at 8 h, 13% at 16 h, and 31% at 24 h.
Left levels of Ikaros, pVHL30, and pVHL19 largely unchanged across all time points.
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Cell Line:MM1.S multiple myeloma cells
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Concentration:50 nM (ZXH-4-137 pre-treatment); 0.1 μM (CC-885)
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Incubation Time:2 h (ZXH-4-137 pre-treatment); 4 h (CC-885 incubation)
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Result:Rescued CC-885-induced GSPT1 degradation, maintaining GSPT1 levels comparable to DMSO control.
Induced nearly complete CRBN degradation.
Achieved rescue comparable to that seen with proteasome inhibitor carfilzomib pre-treatment.
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Cell Line:MOLT-4 leukemia cells
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Concentration:0.1 μM (ZXH-4-137 pre-treatment); 0.25 μM (THAL-SNS-032)
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Incubation Time:2 h (ZXH-4-137 pre-treatment); 6 h (THAL-SNS-032 incubation)
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Result:Partially prevented THAL-SNS-032-induced CDK9 degradation.
Induced nearly complete CRBN degradation.
Achieved partial rescue more effective than pre-treatment with 0.1 μM Pomalidomide.
化学情報
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CAS 番号 2711006-74-3
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分子量 885.08
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分子式 C47H60N6O9S
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SMILES
O=C1C2=C(OCCCCCCCCCCC(N[C@@H](C(C)(C)C)C(N3[C@@H](C[C@H](C3)O)C(N[C@H](C4=CC=C(C5=C(N=CS5)C)C=C4)C)=O)=O)=O)C=CC=C2C(N1C6C(NC(CC6)=O)=O)=O
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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.
プロトコル
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RNA interference technology
RNA interference (RNAi) is a cellular mechanism that inhibits gene expression by suppressing gene transcription or activating RNA degradation. This mechanism was discovered in plants in 1998 by Andrew Fire and Craig Mello. Today, this phenomenon can be observed in almost all eukaryotes, including protozoa, flies, nematodes, insects, parasites, and mammals.
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)
ZXH-4-137 関連分類
HY-132862 関連分類
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