85-2076-35　Rho Inhibitor II, Y16 (PDZ Rho-Binding Domain Blocker, LARG Rho-Binding Domain Blocker, (E)-4-(3-(3-Methylbenzyloxy)benzylidene)-1-phenylpyrazolidine-3,5-dione, (4E)-4-(3-(3-Methylbenzyloxy)benzylidene)-1-phenyl-3,5-pyrazolidinedione, p115 Rho-Binding Domain Blocker) 10mg　217743

特徴

• A cell-permeable pyrazolidinedione compound that is shown to target RhoGEF DH-PH domain junction with high affinity (Kd = 65nM) and effetively prevent RhoGEFs LARG, p115, and PDZ from interacting with RhoA, while displaying little potency against DBL-RhoA, LBC-RhoA, intersectin-Cdc42, or TrioN-Cdc42 interaction. Shown to completely prevent serum-induced activation of cellular RhoA, but not Cdc42 or Rac1, in NIH-3T3 cultures (10uM) and RhoA downstream signaling events. Greatly synergizes with Rho GEF-binding domain blocker Rhosin in blocking RhoA-LARG interaction and in preventing cellular RhoA activation (both drug at 5uM).
• Synonyms:LARG Rho-Binding Domain Blocker, (E)-4-(3-(3-Methylbenzyloxy)benzylidene)-1-phenylpyrazolidine-3,5-dione, (4E)-4-(3-(3-Methylbenzyloxy)benzylidene)-1-phenyl-3,5-pyrazolidinedione, p115 Rho-Binding Domain Blocker, PDZ Rho-Binding Domain Blocker
• Molecular Formula:C₂₄H₂₀N₂O₃
• Primary Target:RhoGEF
• Molar Mass:384.4
• Solubility:DMSO
• Storage and Stability:Store at 4°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.