RN193
RN193 is a type II kinase inhibitor with a human PAK1 IC50 of 4.28 μM. RN193 functionally inhibits kinase activity of PAK1, PAK2, and PAK3, and engages with their kinase domains in live cells. RN193 induces thermal shifts in CLK1, GSK3B, ULK1, MELK, MAPK13, BRAF, and STK10, indicating binding and stabilization of these proteins. RN193 induces formation of PAK3:PAK2 heterodimers and displaces PAK2 homodimers in live cells. RN193 acts as a tool compound for studying group I PAK conformational states.
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- CAS 番号: 3091508-49-2
- 分子式: C30H32N6O3
- 分子量:524.61
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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PAK1M248-H545 4.25 μM (IC50) |
PAK2 |
PAK3 |
RN193 (2 h) potently and selectively binds to the truncated kinase domains of group I PAK1, PAK2, and PAK3 in 293T cells, with IC50 values ranging from 0.14 to 0.16 μM[1].
RN193 (2 h) inhibits the kinase activity of purified PAK1M248-H545 with an IC50 of 4.28 μM in an in vitro ADP-Glo assay[1].
RN193 (2 h) induces the formation of PAK3:PAK2 heterodimers in live HEK293T cells with an IC50 of 0.38 μM; it also disrupts PAK2:PAK2 homodimers with an IC50 of 0.42 μM[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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CAS 番号 3091508-49-2
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分子量 524.61
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分子式 C30H32N6O3
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SMILES
O=C(C1(CC1)C(NC2=CC(C(C)C)=CC=C2)=O)NC3=CC(C4=CNC5=NC=NC(N6CCOCC6)=C54)=CC=C3
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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)