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。

NVS-PAK1-1

CAS No. : 1783816-74-9

MCE 站：NVS-PAK1-1

产品活性：NVS-PAK1-1是有效，选择性的 PAK1 变构抑制剂，IC₅₀值为5 nM。

研究领域：Cell Cycle/DNA Damage  |  Cytoskeleton

作用靶点：PAK

In Vitro: NVS-PAK1-1 demonstrates high selectivity for inhibition of PAK1 over other PAK isoforms and the kinome in general. NVS-PAK1-1 has a biochemical PAK1 K_d of 7 nM and a PAK2 K_d of 400 nM. NVS-PAK1-1 shows excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases. NVS-PAK1-1 at 6-20 μM inhibits the phosphorylation of the downstream substrate MEK1 Ser289. Consistent with the observation, NVS-PAK1-1 inhibits proliferation of Su86.86 cell line only above a concentration of 2 μM. In contrast, by applying a mixture of NVS-PAK1-1 and PAK2 shRNA, inhibition of downstream signaling and cell proliferation at a significantly lower 0.21 μM concentration are achieved.

In Vivo: NVS-PAK1-1 shows a relatively poor stability in rat liver microsomes (RLM) and this would limit its application for in vivo studies (t_1/2 in RLM 3.5 min).

相关产品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Cytoskeleton Compound Library  |  Chemical Probe Library  |  Fingolimod hydrochloride  |  IPA-3  |  5-Aminosalicylic Acid  |  FRAX597  |  FRAX486  |  G-5555  |  GNE 2861  |  FRAX1036  |  LCH-7749944  |  Mesalamine impurity P  |  NVS-PAK1-C

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。