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IC 86621

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Chemical Structure| 404009-40-1 同义名 : -
CAS号 : 404009-40-1
货号 : A745895
分子式 : C12H15NO3
纯度 : 95%
分子量 : 221.252
MDL号 : MFCD07370140
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 IC 86621 is recognized as a strong inhibitor of DNA-dependent protein kinase (DNA-PK), with an IC50 value of 120 nM. It functions as a selective and reversible inhibitor that competes with ATP. IC 86621 impedes the repair of cellular DNA double-strand breaks (DSB) mediated by DNA-PK, with an EC50 of 68 µM. It enhances the antitumor activity induced by DSB without causing cytotoxicity and also shields rheumatoid arthritis (RA) T cells from apoptosis[1][2]. Moreover, IC 86621 is highly selective, showing minimal activity against other kinases including PI3K, Cdk2, Src, PKA, PKC, Chk1, CK1, ATM, and FKBP12[1]. Treatment with IC 86621, ranging from 0 to 100 nM for 24 hours, has been found to prevent apoptosis in T cells of patients with rheumatoid arthritis (RA). This protective effect was observed in CD4+CD45RO- T cells collected from both control individuals and RA patients, with concentrations of 0 nM, 50 nM, and 100 nM, effectively shielding RA T cells from programmed cell death[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.52mL

0.90mL

0.45mL

22.60mL

4.52mL

2.26mL

45.20mL

9.04mL

4.52mL
参考文献

[1]Chandra G, et al. Improved synthesis of a DNA-dependent protein kinase inhibitor IC86621. Arch Pharm Res. 2012 Mar;35(4):639-45.

[2]Shao L, et al. DNA-dependent protein kinase catalytic subunit mediates T-cell loss in rheumatoid arthritis. EMBO Mol Med. 2010 Oct;2(10):415-27.