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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Matrix Metalloproteinase (MMP)-GI254023X
GI254023X

Chemical Structure : GI254023X

CAS No.: 260264-93-5

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GI254023X (GI 254023X, GI4023, SRI028594)

货号: PC-73195Not For Human Use, Lab Use Only.

GI 254023X (GI4023, SRI028594) is a potent, preferential ADAM10 inhibitor with IC50 of 5.3 nM, also inhibits MMP9 (IC50=2.5 nM), preferentially blocking ADAM10 but not TACE.

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5 mg ￥1280 In stock
10 mg ￥1980 In stock
25 mg ￥3580 In stock
50 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GI 254023X (GI4023, SRI028594) is a potent, preferential ADAM10 inhibitor with IC50 of 5.3 nM, also inhibits MMP9 (IC50=2.5 nM), preferentially blocking ADAM10 but not TACE.
GI 254023X displays >100-fold selectivity for ADAM10 over ADAM17 (TACE).
GI 254023X bolcks antibody-induced shedding of target antigens, increases specificity of targeted immunotherapy in vitro.
GI 254023X inhibits PACAP-induced shedding of RAGE in PAC1/RAGE cells.
GI 254023X remarkably inhibits the proliferation and induce the apoptosis of H929 cells.

物理化学性质&存储条件

分子量 391.51
分子式 C21H33N3O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(R)-N-((S)-3,3-Dimethyl-1-(methylamino)-1-oxobutan-2-yl)-2-((S)-1-(N-hydroxyformamido)ethyl)-5-phenylpentanamide

参考文献

1. Hundhausen C, et al. Blood. 2003 Aug 15;102(4):1186-95.

2. Budagian V, et al. J Biol Chem. 2004 Sep 24;279(39):40368-75.

3. Verena V Metz, et al. PLoS One.2012;7(7):e41823.

4. Eichenauer DA, et al. Cancer Res. 2007 Jan 1;67(1):332-8.

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