• 產(chǎn)品描述： JNK Inhibitor VIII (TCS JNK 6o) 是一種 c-Jun N-terminal kinases 的抑制劑，對(duì)JNK-1和JNK-2的IC50值分別為45 nM和160 nM。JNK Inhibitor VIII (TCS JNK 6o) 可抑制JNK-1、JNK-2和JNK-3，對(duì)應(yīng)的Ki值分別為2 nM、4 nM和52 nM

• 靶點(diǎn)： JNK1(Cell-free assay):2 nM(Ki); JNK2(Cell-free assay):4 nM(Ki); JNK1(Cell-free assay):45 nM; JNK3(Cell-free assay):52 nM(Ki); JNK2(Cell-free assay):160 nM;JNK

• 體內(nèi)研究：
  Pharmacokinetic profiles are determined for JNK Inhibitor VIII (TCS-JNK-6o) in Sprague-Dawley rats. JNK Inhibitor VIII (TCS-JNK-6o) showes a short half-life of roughly 1 h, with rapid clearance and barely measurable bioavailability. Microsomal incubation studies revealed that oxidative metabolism is very rapid with this compound

• 細(xì)胞實(shí)驗(yàn)： Cell lines: hepG2 cells Concentrations: Serial concentrations Incubation Time: 1 h Method: HepG2 human hepatoma cells (ATCC) are cultured in low glucose MEM supplemented with 1×NEAA, 1×sodium pyruvate, and 10% FBS. For P-c-Jun assays, cells are plated at 5×104 cells/well in 500 μL of complete media on 24-well collagen-coated plates and incubated overnight. Serial compound dilutions are made in DMSO at 100×, and then 5 μL is added directly to the media on the cells to provide the final inhibitor concentrations. After 1 h, cells are stimulated with vehicle control or TNFR for 30 min and harvested in 70μL of lysis buffer (TBS (54 mM Tris-HCl, pH 7.6, 150 mM NaCl), 1% TritonX-100,0.5% Nonidet P-40, 0.25% sodium deoxycholate, 1 mM EDTA, 1 mM EGTA, 0.5 mM sodium fluoride, 1 mM pervanadate, 1 μM microcystin, 1 mM AEBSF, 1 tablet of complete EDTA Free-Mini inhibitor cocktail) and frozen at -80 °C prior to use in the P-c-Jun assay.

• 動(dòng)物實(shí)驗(yàn)： Animal Models: Sprague-Dawley rat Dosages: 5 mg/kg Administration: IV, Oral gavage

• 參考文獻(xiàn)：
  1. Bruce G Szczepankiewicz, et al. J Med Chem. 2006 Jun 15;49(12):3563-80.

• 溶解性： Soluble  in  DMSO

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	2.806 ml	14.03 ml	28.06 ml
  5 mM	0.561 ml	2.806 ml	5.612 ml
  10 mM	0.281 ml	1.403 ml	2.806 ml
  50 mM	0.056 ml	0.281 ml	0.561 ml

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *