bd 2

BD-AcAc 2 (Ketone Ester) is a ketone monoester and can be used as a source of oral nutritional ketones. BD-AcAc 2 can elevate plasma levels of acetoacetate and β-hydroxybutyrate, blood Na+, blood glucose levels and blood creatinine levels after oral administration in mice. BD-AcAc 2 can partly prevent muscle weakness in septic mice. BD-AcAc 2 exhibits potential to improve endurance and exercise performance in animal body. BD-AcAc 2 can also be used to research diabetes or Parkinson’s disease.

(S,S)-BD-AcAc 2 ((S,S)-Ketone Ester), an (S,S)-enantiomer of BD-AcAc 2, increases AcAc and acetone levels, inducing sustained ketosis and significantly delaying seizures associated with central nervous system oxygen toxicity (CNS-OT).

PBRM1-BD2-IN-3 (compound 12) is a potent inhibitor of PBRM1-BD2, exhibiting an IC50 value of 1.1 μM, and is utilized in anticancer research.

PBRM1-BD2-IN-7, a selective and cell-active inhibitor targeting the polybromo-1 (PBRM1) bromodomain, demonstrates inhibitory efficacy against PBRM1-BD2 with an IC50 value of 0.29 μM. This compound is utilized in cancer research.

BRD4-BD1-IN-2 is a selective and potent BRD4-BD1 inhibitor with an IC50 value of 2.51 µM, which is 20-fold greater than the inhibitory activity against BRD4-BD2.BRD4-BD1-IN-2 can be used in the study of cardiovascular and cancer-related diseases.

PBRM1-BD2-IN-2, a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, exhibits binding affinity and inhibitory activity specifically targeting the PBRM1-BD2 domain, with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. This compound is utilized in cancer research.

PBRM1-BD2-IN-8 (compound 34) is a potent PBRM1 Bromodomain inhibitor (PBRM1-BD2 Kd=4.4 μM, PBRM1-BD2 IC50=0.16 μM; PBRM1-BD5 Kd=25 μM). PBRM1-BD2-IN-8 shows anti-cancer activity.

PBRM1-BD2-IN-5 is a potent inhibitor of the PBRM1 Bromodomain, demonstrating dissociation constant (Kd) values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and boasts an inhibitory concentration 50 (IC50) value of 0.26 μM for PBRM1-BD2. This compound effectively diminishes the interaction between the full-length PBRM1 and acetylated histone peptide within the PBAF complex in cell lysates, which positions it as a promising candidate for anticancer research.

BRD4-BD1/2-IN-1 is a highly effective inhibitor of BRD4, specifically targeting the BRD4 BD-1 and BRD4 BD-2 domains with IC 50 values of <100 nM each (US20150148375A1, compound 5) [1].

PBRM1-BD2-IN-6, a potent inhibitor of the PBRM1 bromodomain, exhibits an IC50 value of 0.22 µM and demonstrates antiproliferative activity. It holds potential for research in PBRM1-dependent cancer treatment.

BRD4-BD1/2-IN-2 is a potent inhibitor of BRD4-BD2, capable of acting on both BRD4 BD2 (IC50<0.5 nM) and BRD4 BD1 (IC50<300 nM).

PBRM1-BD2-IN-1 is a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, displaying binding affinity and inhibitory efficacy with Kd and IC50 values of 0.7 μM and 0.2 μM, respectively. This compound is utilized in cancer research.

BET BD2-IN-1 (compound 45) is a potent, selective inhibitor of BET BD2, exhibiting an IC50 value of 1.6 nM. It suppresses Th17 cell differentiation through the reduced activation of STAT3 and NF-κB, making it relevant in research on psoriasis and inflammatory bowel disease (IBD) [1].

BD 1008 dihydrobromide is a selective antagonist of the sigma 1 (σ1) receptor (Ki = 2 nM). BD 1008 dihydrobromide have high affinity for sigma1 receptors, moderate affinity for sigma2 receptors.

BD 1008 Free Base is a selective sigma receptor antagonist, with a reported binding affinity of Kᵢ = 2 ± 1 nM for the sigma-1 receptor and 4 times selectivity over the sigma-2 receptor.

BRD4 Inhibitor-23 is a potent, orally active BRD4 inhibitor that acts on BRD4 BD-1 (IC50: 6.21 nM) and BRD4 BD-2 (IC50: 1.44 nM).