bcl2 in 1

A-1211212 (BCL2-IN-1) is a potent and selective Bcl-2 inhibitor. It promotes lymphocyte apoptosis, alters colonic mucosa in mice, and improves inflammation.

MCL-1/BCL-2-IN-2 (Compound Nap-1) is a potent and selective dual inhibitor of Mcl-1 and Bcl-2, with IC50 values of 4.45 μM and 3.18 μM, respectively [1].

c-MYC/BCL2 ligand 1 iodide is a dual-target ligand that specifically interacts with the G-quadruplex (G4) regions of the c-MYC and Bcl-2 promoters, exhibiting Kd values of 0.90 μM for c-MYCG4 and 0.56 μM for Bcl-2G4. It works by binding to these G4-forming sequences to inhibit transcription of the c-MYC and Bcl-2 genes, leading to reduced protein expression. This compound effectively suppresses MCF-7 cell proliferation and migration, induces G1 phase cell cycle arrest, and triggers apoptosis. Additionally, it significantly hampers tumor growth in the 4T1 homogenous model with negligible toxicity. c-MYC/BCL2 ligand 1 iodide is applicable in breast cancer research.

PROTAC Bcl2 degrader-1 is a PROTAC, which potently and selectively induces the degradation of Mcl-1 (IC50: 11.81 μM) and Bcl-2 (IC50: 4.94 μM; DC50: 3.0 μM).

CDK2/Bcl2-IN-1 (compound 1) is a saponin-based inhibitor of CDK-2 (IC50=117.6 nM) with potent cytotoxic effects on cancer cells, also inhibiting Bcl-2 and promoting apoptosis in A549 lung cancer cells [1].

Bcl-2-IN-18 (Compound 23) is a Bcl-2 inhibitor targeting breast cancer with an IC50 value of 4.7 μM against MCF-7 cells. It exhibits antitumor activity.

Bcl-2-IN-19 (compound 27) is a potent Bcl-2 inhibitor used specifically to target breast cancer.

GPER/Bcl-2 Inhibitor is a GPER/Bcl-2 inhibitor that suppresses the proliferation of glioblastoma cells and the formation of neurospheres. It is applicable in glioblastoma (GBM) research.

Bcl-2-IN-11 (compound 6) is a potent and selective Bcl-2 activity inhibitor with an IC50 of 0.9 nM and minimal inhibition against Bcl-xl (IC50 > 1000 nM). It is used in cancer research related to Bcl-2 family protein overexpression, particularly in hematologic malignancies like acute lymphoid leukemia, while minimizing the risk of side effects such as thrombocytopenia [1] by sparing Bcl-xl.

Bcl-2-IN-16 is an inhibitor of Bcl-2 (B-cell lymphoma 2) [1].

Bcl-2-IN-15 (Compound 13d) is a Bcl-2 inhibitor with an IC50 of 363 nM that impedes the proliferation of the NCI leukemia cancer cell line [1].

Bcl-2-IN-14 (Compound 13c), a BCL-2 inhibitor with an inhibitory concentration (IC50) of 0.471 μM, is applicable in cancer research [1].

Bcl-2-IN-13, a potent Bcl-2 inhibitor with an IC50 of 17 nM, shows promise for cancer research applications [1].

Bcl-2-IN-12 (Compound 1) is a potent Bcl-2 inhibitor with an IC50 value of 6 nM, used in cancer research [1].

AZD-5991 Racemate is the racemate of AZD-5991. (Rac)-AZD-5991 is a novel Mcl-1 inhibitor with IC50 <3 nM in FRET assay and induces upregulation of BCL2,BCL-XL, CMYC and MCL1 in AML cell lines.

AZD5991 is a potent and selective Mcl-1 inhibitor aimed at treating hematological cancers. As a well-designed macrocyclic compound, AZD5991 exhibits sub-nanomolar affinity for Mcl-1. It primarily inhibits the myeloid cell leukemia-1 protein (Mcl-1; Bcl2-L-3), showing potential pro-apoptotic and anti-tumor activity. AZD5991 binds to Mcl-1, preventing its interaction with certain pro-apoptotic proteins, leading to apoptosis in cells overexpressing Mcl-1.

Hymeglusin, A selective 3-hydroxy-3-methylglutaryl Coenzyme A (HMG-CoA) synthase 1 inhibitor, is also an antibiotic that reduces the expression level of BCL2 in HL-60 and KG-1 cells and can be used to study leukemia.

S)-(-)-Perillic acid is a terpenoid natural product capable of inhibiting protein pentosylisation and protein acylation. It exhibits anti-infective and anti-cancer activity, inducing cell cycle arrest and apoptosis in non-small cell lung cancer cells while increasing intracellular protein levels of Bax, p21, and caspase-3.

Serpinin, an agonist of the protease inhibitor Nexin-1 (PN-1), upregulates PN-1 expression via the cAMP-PKA-Sp1 signaling pathway, facilitating granule biogenesis in endocrine cells. It is employed in research on secretory function regulation [1]. Serpinin selectively targets β-adrenergic receptors, particularly interacting with β1-adrenergic receptors to activate the AC-cAMP-PKA pathway, thereby regulating myocardial systolic and diastolic function. Additionally, pGlu-serpinin upregulates Bcl2 mRNA transcription and provides neuroprotective effects [2].