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.

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].

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].