Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9194 |
UMB298
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
UMB298 是一种有效的选择性 CBP/P300 溴结构域抑制剂,抑制 BRD4,IC50 为 5193nM。 | |||
T3082 |
SGC0946
|
Histone Methyltransferase | Chromatin/Epigenetic |
SGC0946是一种组蛋白甲基转移酶DOT1L 高选择性抑制剂,IC50值为0.3nM,可选择性地杀死混合谱系白血病细胞。 | |||
T78854 |
WK499
|
||
BCL6-IN-10 (Compound WK499) 是抑制蛋白 BCL6 的化合物。该化合物能干扰 BCL6 与 SMRT 蛋白的结合作用,进而诱导 apoptosis、导致细胞周期阻滞以及 DNA 损伤。针对多种 Acute Myeloid Leukemia (AML) 细胞株,如 OCI-AML3、THP1、MOLM13、HL60, KG1, NB4,BCL6-IN-10 显示出较强的抑制活性,其 IC50s 分别为 0.91、1.63、1.026、7.42、0.87、0.85 μM。 | |||
T36978 | AS-99 TFA | ||
AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo[1]. AS-99 TFA is tested against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2. NO significant inhibition is observed at 50 μM of AS-99 TFA on any of the tested... |