Bcl-2/Mcl-1-IN-1 (compound 3) is a Bcl-2/Mcl-1 inhibitor, with Kis of 1.19 μM and 4.53 μM for Mcl-1 and Bcl-2, respectively. Bcl-2/Mcl-1-IN-1 can be used for the research of cancer.

Bim-IN-1 is a potent Bim expression inhibitor. Bim-IN-1 reduces Bim expression levels and has little inhibitory effect upon protein kinase A activity and minimal toxicity.

A derivative of BAM-7 that acts as a nove potent, direct activator of Bax with EC50 of 700 nM; inhibits GBM cell proliferation, arrests the cell cycle, and induces apoptosis through the induction of mitochondrial membrane permeabilization; also blocks proliferation and self-renewal of GSCs and induces their apoptosis; sensitizes both GBM cells and GSCs to the alkylating agent Temozolomide.

BFL-1 inhibitor 4E14 (4E14) is a potent, selective, covalent BFL-1 inhibitor that disrupt BH3-binding activity with IC50 of 1.3 uM, targets a unique C55 residue in the BFL-1 groove.4E14 blocks BFL-1 suppression of BAX-mediated mitochondrial apoptosis.

CCT369347 (CCT-369347) is potent selective inhibitor of BCL-6 with TR-FRET IC50 of 26 nM.CCT369347 demonstrated antiproliferative activity in a panel of BCL6-positive lymphoma cell lines (OCI-Ly1, SU-DHL-4, and SU-DHL-6) with IC50 of 1.68-3.45 uM, with weaker activity against low BCL6 expression cells and noncytotoxocity. CCT369347 inhibits BCL6 in a cellular assay with a submicromolar IC50 and shows promising early PK.

D-NA-NOXA SAHB-15 R31E is a peptidic, functionally selective and cell-permeable BFL-1/A1 inhibitor that is specifically cytotoxic to BFL-1/A1-dependent human cancer cells.

ZH07 (Dual Mcl-1/Bfl-1 inhibitor 24) is a potent, selective dual Mcl-1 and Bfl-1 inhibitor, binds both Mcl-1 and Bfl-1 with Ki of 97 nM and 100 nM, respectively.ZH07 displays appreciable selectivity (>250-fold) over Bcl-2/Bcl-xL.ZH07 induces dose-dependent disruption of interactions between BL-Bim and endogenous Mcl-1 and Bfl-1, without affecting the complexes between BL-Bim and Bcl-2 or Bcl-xL.ZH07 demonstrates on-target cellular activity in model lymphoma cell lines.

ZH97 is a selective and covalent small-molecule inhibitor of BFL-1 protein with binding Ki of 0.41 uM, >200-fold selectivity over MCL-1.ZH97 does not bind to BCL-xL, BCL-2, TEAD2, TEAD4, MDM2, MDMX, BRD2 BD1, BRD2 BD2, BRD3 BD1, BRD3 BD2, BCL9, PD1/PD-L1 (Ki>400 uM).ZH97 modifies BFL-1 at the C55 residue, blocks BFL-1/BID interaction in vitro.ZH97 dose-dependently increased cytoplasmic cytochrome c level in U937 cells, has cell growth inhibition with IC50 of 2.8 uM, 5.5 uM, 7.7 uM, 6.8 uM, and 3.9 uM in U937, Kasumi-1, K562, MM.1S, and MV4-11 cell lines, respectively.ZH97 inhibits BFL-1/PUMA interaction in cell lysate and is effective in cancer cells that harboring highexpression level of BFL-1.

M24 is a Mcl-1 selective inhibitor. M24 exhibits good binding affinity against Mcl-1 with Ki value of 0.33 μM. M24 exhibits good anti-proliferative activity and induce apoptosis in HepG2 cells.

BM-1074 is a potent and specific Bcl-2/Bcl-xL inhibitor with Ki values of < 1 nM and IC50 values of 1.8 nM and 6.9 nM for Bcl-2 and Bcl-xL, respectively. BM-1074 induces apoptosis, and exhibits antiproliferative activity against four small-cell lung cancer cell lines (H146, H1963, H187 and H1417) with IC50 values of 1-2 nM.

UBX1325 is an Bcl-xL inhibitor that promotes apoptosis in senescent cells. UBX1325 is a potent anti-aging agent that can be used in studies of age-related eye diseases such as diabetic macular oedema (DME), age-related macular degeneration (AMD) and diabetic retinopathy (DR).

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.

CYD-4-61 is a novel Bax activator used for breast cancer research. CYD-4-61 inhibits triple-negative breast cancer MDA-MB-231 and ER-positive breast cancer MCF-7 cell lines proliferation. CYD-4-61 activates Bax protein to induce cytochrome c release and regulate apoptotic biomarkers, leading to cancer cell apoptosis.

BAU-243 (BAU243) is a novel BH3 mimetic Bcl-2 inhibitor with a high affinity, effectively reduces overall GBM cell proliferation including a subpopulation of cancer-initiating cells.

BDM44898 is a small molecule inhibitor of anti-apoptotic protein BCL2A1/Bfl-1 with IC50 of 1.6 uM.

BDM44931 is a small molecule inhibitor of anti-apoptotic protein BCL2A1/Bfl-1 with IC50 of 1.3 uM.

BDM49234 is a selective small molecule inhibitor of anti-apoptotic protein BCL2A1/Bfl-1 with IC50 of 6.3 uM (inhibition FITC–Bim BH3 binding to Bfl-1).

BDM53787 is a selective small molecule inhibitor of anti-apoptotic protein BCL2A1/Bfl-1 with IC50 of 0.8 uM (inhibition FITC–Bim BH3 binding to Bfl-1).

BI-5273 is a negative control compound of BI-3802 and BI-3812, which are potent and efficacious BCL6 degrader and inhibitor, respectively.

CCT372064 is a potent, ligand-efficient inhibitor of BCL6 with IC50 of 3.9 nM and 12 nM in TR-FRET and cellular NanoBRET assays, respectively.

CCT373566 is a highly potent, in vivo active BCL6 degarder with IC50 of 2.2 nM and DC50 of 0.7 nM in TR-FRET and cellular BCL6 degradation assays, respectively.

CCT373567 is a potent, selective and cell-active BCL6 inhibitor with IC50 of 2.9 nM in TR-FRET assays, and 25.9 nM in NanoBRET cellular inhibition assays.