CeMMEC1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CeMMEC1 是一种有效的、选择性的 TAF1 第二溴结构域抑制剂，Kd 为 1.8 uM。

CeMMEC1 is a potent, selective second bromodomain of TAF1 inhibitor with Kd of 1.8 uM; shows high selectivity for the TAF1 (2) bromodomain over BRD4 (1), BRD9, CREBBP, EP300 and TAF1 (2) bromodomains (IC50>10 uM; impaires cell viability in TAF1 downregulated cells; synergizes with (+)-JQ1 to inhibit the proliferation of THP-1 and H23 lung adenocarcinoma cells.

CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC50 of 0.9 μM for TAF1, and a Kd of 1.8 μM for TAF1 (2) and slso shows high affinity for the bromodomains of CREBBP, EP300, BRD9. CeMMEC1 (1, 10, 20 μM) decreases the number of THP1 cells in S phase in a dose manner. CeMMEC1 also induces apoptosis. CeMMEC1 in combination with (S)-JQ1 displays potently impaired cell viability than treatment alone.

——

CeMMEC 1

Chromatin/Epigenetic

Bromodomain

BRD4|TAF1

——

——

440662-09-9

336.3

C19H16N2O4

>98% (HPLC)

DMSO: 21 mg/mL (62.4 mM) （ < 1 mg/ml refers to the product slightly soluble or insoluble )

CN1C=C(C2=CC=CC=C2C1=O)C(=O)NC3=CC4=C(C=C3)OCCO4

N-(2,3-dihydro-1,4-benzodioxin-6-yl)-1,2-dihydro-2-methyl-1-oxo-4-isoquinolinecarboxamide

(-20℃)

With Ice Pack

≥ 2 years