Bcl-B inhibitor 1 is a Bcl-B inhibitor[1].
AZD4320 is a novel BH3-mimicking dual BCL2/BCLxL inhibitor with IC50s of 26 nM, 17 nM, and 170 nM for KPUM-MS3, KPUM-UH1, and STR-428 cells, respectively.
Furowanin A is a flavonoid with anti-neoplastic effects. Furowanin A inhibits STAT3/Mcl-1 axis to suppress proliferation, block cell cycle progression, induce apoptosis and promote autophagy. Furowanin A potently inhibits colorectal cancer (CRC) cells[1].
S55746 is an orally active, selective and potent BCL-2 inhibitor, with a Ki of 1.3 nM.
Thevetiaflavone could upregulate the expression of Bcl‑2 and downregulate that of Bax and caspase‑3.
WEHI-539 hydrochloride is a selective inhibitor of Bcl-XL with an IC50 of 1.1 nM.
Mcl1-IN-4 is an inhibitor of Mcl1 with an IC50 of 0.2 μM.
Mcl-1 inhibitor 8 is a MCL-1 inhibitor, example 228, extracted from patent WO2019222112[1].
A-1155463 is a highly potent and selective BCL-XL inhibitor with an EC50 of 70 nM in Molt-4 cell.
Aspidin BB is a phloroglucinol derivative, which can be isolated from the aerial part of Dryopteris championii. Aspidin BB has anticancer activity. Aspidin BB induces cell cycle arrest and apoptosis in human ovarian HO-8910 cells[1][2].
(R)-(-)-Gossypol (AT-101) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.
Ginsenoside Rh4 is a rare saponin obtained from Panax notoginseng. Ginsenoside Rh4 activates Bax, caspase 3, caspase 8, and caspase 9. Ginsenoside Rh4 also induces autophagy.
Jaceosidin is a flavonoid isolated from Artemisia vestita, induces apoptosis in cancer cells, activates Bax and down-regulates Mcl-1 and c-FLIP expression[1]. Jaceosidin exhibits anti-cancer[2], anti-inflammatory activities, decreases leves of inflammatory markers, and suppresses COX-2 expression and NF-κB activation[3].
ABT-737 is a selective and BH3 mimetic Bcl-xL, Bcl-2 and Bcl-w inhibitor with EC50s of 78.7 nM, 30.3 nM and 197.8 nM, respectively.
Pyridoclax is a potential Mcl-1 inhibitor.
Mcl1-IN-14 (compound C3), a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM. Mcl1-IN-14 induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1 inhibitor S1-6 with μM-range affinity[1].
anti-TNBC agent-3 (compound 3g) is an apoptosis inducer with anti-cancer cell proliferation activity. anti-TNBC agent-3 inhibits tumor growth and metastasis in triple-negative breast cancer (TNBC) xenograft models[1].
Spicamycin, an adenine nucleoside antibiotic with antifungal and antitumor activities. Spicamycin is also a potent inducer of differentiation of myeloid leukemia cells. Spicamycin induces apoptosis in NB4 cells via down-regulation of Bcl-2 expression and modulation of PML protein[1][2].
Bcl-2-IN-5 is a BCL-2 inhibitor with IC50s of 0.12 nM, 0.14 nM and 0.22 nM for Bcl-2 wild type, Bcl-2 D103Y and Bcl-2 G101V, respectively. Bcl-2-IN-5 inhibits the cell growth with IC50 values of 0.2 nM and 0.44 nM for Bcl 2-G101V knock-in RS4; 11 and RS4; 11 cells, respectively (WO2021208963A1; Example 155)[1].
CCT373566 is a potent and orally active degrader of transcriptional repressor BCL6, with an IC50 of 2.2 nM. CCT373566 shows strong antiproliferative efficacy in vitro and reduction in tumor growth in vivo[1].
Bcl-2-IN-11 (compound 6) is a potent and selective Bcl-2 activity inhibitor, with an IC50 of 0.9 nM. Bcl-2-IN-11 shows weak inhibition of Bcl-xl (IC50 > 1000 nM). Bcl-2-IN-11 can be used for the research of a variety of cancers caused by abnormal overexpression of Bcl-2 family proteins: especially malignant hematologic diseases of acute lymphoid leukemia, etc. Bcl-2-IN-11 can also avoid toxic side effects caused by Bcl-xl inhibition, such as thrombocytopenia[1].
CCT373567 is a potent degrader of transcriptional repressor BCL6, with an IC50 of 2.9 nM. CCT373567 exhibits antiproliferative activity[1].
(+)-Apogossypol is a pan-BCL-2 antagonist. (+)-Apogossypol binds to Mcl-1, Bcl-2 and Bcl-xL with EC50s of 2.6, 2.8 and 3.69 µM, respectively.
BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a Ki of 2.4±0.2 μM in FP assay. BH3I-1 has a Kd of 5.3 μM against the p53/MDM2 pair.
MSN-125 (MSN 125, MSN125) is a small molecule Bax inhibitor that inhibits Bax/Bak oligomerization and prevents mitochondrial outer membrane permeabilization (MOMP) with IC50 of 4 uM; potently inhibits Bax/Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons, protects primary neurons against glutamate excitotoxicity.
Mcl1-IN-3 is an inhibitor of Mcl1 extracted from patent WO2015153959A2, compound example 57; has an IC50 and Ki of 0.67 and 0.13 μM, respectively.
TW-37 is a potent Bcl-2 inhibitor with Ki values of 260, 290 and 1110 nM for Mcl-1, Bcl-2 and Bcl-xL, respectively.
A novel potent, selective Mcl-1 inhibitor with IC50 of <3 nM in FRET assays; displays >1,000-fold selectivity over Bcl-2 and Bcl-xL; induces cleaved caspase-3 in MV4-11 cells with IC50 of 3.78 uM.
Aviculin, a lignan glycoside, is a potent anticancer agent. Aviculin reduces metabolic activity on MCF-7 cells below 50%, with an IC50 of 75.47 μM. Aviculin induces breast cancer cell apoptosis through the intrinsic apoptosis pathway. Aviculin increases expression of initiator caspase-9, executioner caspase-7, and poly (ADP-ribose) polymerase (PARP). Aviculin shows an increase in the Bax/Bcl-2 ratio[1].
TMX-2164 is a potent, irreversible B-cell lymphoma 6 (BCL6) inhibitor with an IC50 value of 152 nM. TMX-2164 displays sustained target engagement and antiproliferative activity in cells[1].