MCE 的所有产品仅用作科学研究，我们不为任何个人用途提供产品和服务。

KG-501

CAS No. : 18228-17-6

MCE 站：KG-501

产品活性：KG-501 是 CREB 的抑制剂，其 IC₅₀ 值为 6.89 μM。

研究领域：Epigenetics

作用靶点：Epigenetic Reader Domain

In Vitro: KG-501, which directly targets the KIX domain of CBP, results in a disrupted CREB-CBP complex, inhibits CREB-target gene induction, and inhibits IL-1β-mediated angiogenic activity in NSCLC. KG-501 disrupts phospho (Ser-133) CREB binding to KIX with a K_i of ~90 μM, using concentrations of CREB that are within the linear range of the binding assay. Treatment of HEK293T cells with KG-501 also blocks induction of endogenous CREB target genes (NR4A2, αCG, c-fos, and RGS2) by forskolin, indicating that KG-501 likely exerts a general effect on CREB activity. KG-501 can also inhibit NF-κB transcription activity because NF-κB also uses CBP as a cofactor to regulate gene expression. The migration of HUVECs induced by CM from A549 cells treated with IL-1β plus 10 μM of KG-501 is significantly lower than that induced by CM from A549 cells treated with IL-1β alone. At 10 μM, KG-501 suppresses the expression of all of the IL-1β–induced CXC chemokine genes except CXCL8. For the protein level, KG-501 significantly suppresses IL-1β–induced CXCL5 protein secretion. Similar effects of KG-501 are also observed in the H1734 cell line.

相关产品：Reprogramming Compound Library  |  Epigenetics Compound Library  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Histone Modification Research Compound Library  |  (+)-JQ-1  |  A-485  |  Curcumin  |  Birabresib  |  ARV-771  |  ARV-825  |  dBET6  |  dBET1  |  Molibresib  |  C646  |  BI 2536  |  666-15  |  MZ 1  |  I-BET151  |  ABBV-744  |  CPI-637  |  Anacardic Acid  |  MI-503  |  Mivebresib  |  BETd-260  |  SGC-CBP30  |  AZD5153 6-Hydroxy-2-naphthoic acid  |  GNE-781  |  MG 149  |  PLX51107  |  CPI-0610  |  Apabetalone  |  CPI-203

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。