SJ46421
SJ46421 is a BRD3BD2 PROTAC degrader. SJ46421 induces a cooperative ternary complex of KLHDC2 and BRD3BD2 with an IC50 of 7.8 nM. SJ46421 binds to the substrate-binding pocket of KLHDC2, forms cooperative ternary complexes with BRD3BD2, BRD2BD2 and BRD4BD2, disrupts the autoinhibitory tetramer assembly of KLHDC2, drives selective ubiquitination of BRD3BD2, and inhibits the ubiquitination of endogenous KLHDC2 diglycine substrates. SJ46421 can be used in cancer research.
(Pink: BRD3 BD2 ligand (HY-13030); Blue: KLHDC2 ligand (HY-168536); Black: linker (HY-20797)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。
- 分子式: C42H41ClN8O5S2
- 分子量:837.41
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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
- 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]|
BRD3 BD2 987 nM (Kd) |
BRD4 BD2 1020 nM (Kd) |
BRD2 BD2 2090 nM (Kd) |
体外実験
SJ46421 (0.6 μM; 0-60 seconds) promotes efficient polyubiquitylation of BRD2BD2, BRD3BD2, and BRD4BD2 via neddylated CRL2KLHDC2 in vitro[1].
SJ46421 (0.001-10 μM; 15 minutes pre-incubation) forms a high-affinity ternary complex with neddylated CRL2KLHDC2 and BRD3BD2, potently inhibiting KLHDC2 substrate ubiquitylation with a Ki(app) of 7.84 nM[1].
SJ46421 forms a highly positively cooperative ternary complex with KLHDC2SBD and BRD3BD2 (α=16) with a Kd of 19 nM, while forming only moderately cooperative complexes with BRD2BD2 (α=1.4) and BRD4BD2 (α=2.8)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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分子量 837.41
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分子式 C42H41ClN8O5S2
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SMILES
O=C(O)CNC(CC1=CSC(C2=CC=C3C=CC=C(OCCN4CCN(C(C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5)=O)CC4)C3=C2)=N1)=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.
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)
SJ46421 関連分類
HY-168634 関連分類
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