MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

PRN694

CAS No. : 1575818-46-0

MCE 站：PRN694

产品活性：PRN694 是一种不可逆的，高效选择性的，有效共价结合的白介素 2 诱导细胞激酶 ITK、 静息淋巴细胞激酶 RLK 双重抑制剂，抑制 ITK、RLK 的IC₅₀ 分别为 0.3 nM 和 1.4 nM。PRN694 延长靶向停留时间，使效应细胞在体内外持久衰减。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Itk

In Vitro: PRN694 inhibits TEC, BTK, BMX, BLK, JAK3 with IC₅₀s of 3.3, 17, 17, 125, 30 nM, respectively.
Immunoblot analysis of TCR activation pathways reveales that PRN694 blocks activation or nuclear translocation of NFAT1, JunB, pIκBα, ａnd pERK. Results reveal inhibition of Ca²⁺ signaling with PRN694 at all concentrations above 1 nM. PRN694 significantly attenuates NK cell FcR-induced killing at concentrations exceeding 0.37 μM.
Day 6 flow cytometry analysis reveals that PRN694 significantly inhibits the anti-CD3/CD28-induced proliferation of both CD4 ａnd CD8 T-cells (p<0.01).

In Vivo: The PRN694 occupancy of ITK is 98, 95, ａnd 54% at 1, 6, ａnd 14 h, respectively. The concentrations of PRN694 in the plasma are 2.8, 0.66, ａnd 0.027 μM at 1, 6, ａnd 14 h, respectively. At 14 h, the plasma level of PRN694 is over 10 fold lower than the IC₅₀ in whole blood. RN694 treatment also results in significantly lower weights relative to vehicle (p<0.05).
Colitis studies show reduced numbers of CD4⁺ T cells present in the colonic epithelium of PRN694-treated mice compare with controls.

相关产品：Bioactive Compound Library Plus  |  ITK inhibitor 2  |  GNE-4997

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。