貨號	規格	價格	上海	北京	武漢	南京
S89992-1mg	99.1%	￥150.00 S89992-1mg ￥150.00 現貨	9 9	-	-	-
S89992-5mg	99.1%	￥250.00 S89992-5mg ￥250.00 現貨	8 8	-	-	-
S89992-25mg	99.1%	￥530.00 S89992-25mg ￥530.00 現貨	6 6	-	-	-
S89992-100mg	99.1%	￥1640.00 S89992-100mg ￥1640.00 現貨	1 1	-	-	-

產品介紹

JNK Inhibitor VIII (TCS JNK 6o) 是一種 c-Jun N-terminal kinases 的抑制劑，對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，對應的Ki值分別為2 nM、4 nM和52 nM

產品描述：

靶點：

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

細胞實驗：

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.

動物實驗：

Animal Models: Sprague-Dawley rat Dosages: 5 mg/kg Administration: IV, Oral gavage

參考文獻：

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：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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