Sabutoclax (BI-97C1)(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.

MCL1:0.2 μM, BCL2:0.32 μM, BCL-XL:0.31 μM, Bfl-1:0.62 μM

Sabutoclax（0.001-10 μM；72小时）抑制人类前列腺癌和肺癌细胞系的生长[2]。Sabutoclax（0.01-1 μM；24-48小时）在人类弥漫性大B细胞淋巴瘤细胞中诱导凋亡[2]。Sabutoclax（0-15 μM；48小时）在化疗抵抗性细胞中上调促凋亡蛋白水平[1]。

Sabutoclax（1-5 mg/kg；腹腔注射；每两天一次，共计18天）有效抑制裸鼠M2182肿瘤的增长[2]。

Competitive fluorescence polarization assays (FPA) : A Bak BH3 peptide (F-BakBH3) (GQVGRQLAIIGDDINR) is labeled at the N-terminus with fluorescein isothiocyanate (FITC) and purified by HPLC. For competitive binding assays, 100 nM GST-Bcl-XL ΔTM protein is preincubated with the tested compound at varying concentrations in 47.5 μL PBS (pH = 7.4) in 96-well black plates at room temperature for 10 min, and then 2.5 μL of 100 nM FITC-labeled Bak BH3 peptide is added to produce a final volume of 50 μL. The wild-type and mutant Bak BH3 peptides are included in each assay plate as positive and negative controls, respectively. After 30 min incubation at room temperature, the polarization values in millipolarization units are measured at excitation/emission wavelengths of 480/535 nm with a multilabel plate reader. IC50 is determined by fitting the experimental data to a sigmoidal dose-response nonlinear regression model. Data reported are mean of three independent experiments. Performance of Bcl-2 and Mcl-1FPA are similar. Briefly, 50 nM of GST-Bcl-2 or -Mcl-1are incubatedwith various concentrations of compound (4 and 11-14) for 2 min, and then 15 nM FITC-conjugated-Bim BH3 peptide is added in PBS buffer. Fluorescence polarization is measured after 10 min.

ATP-LITE assay(Only for Reference)