br1

PRL-3 Inhibitor I (BR-1) is a phosphatase of regenerating liver 3 (PRL-3) inhibitor which blocks the migration and invasion of metastatic cancer cells.

BR102375 is a non-TZD PPAR γ full agonist (EC50: 0.28 μM) for the treatment of type 2 diabetes.

TGFBR1-IN-1 is an inhibitor of ALK5 (IC50 of 10-100 nM).

TGFBR1-IN-2 (Compound AQA) is a TGFBR1 inhibitor (KD: 0.01 μM) and antimicrobial agent. It serves as a substrate for cytochrome P450. The compound contains a pyridyl-6-methyl group, essential for inhibiting Mycobacterium tuberculosis, and effectively inhibits non-replicating and persistent strains of this bacterium.

CBR1-IN-6 (compound 1a) is a CBR1 inhibitor with chemosensitizing and cardioprotective properties.

BR103354 is a novel fibroblast activation protein (FAP) inhibitor with anti-diabetic and anti-steatotic effects. BR103354 inhibited FAP with an IC50 value of 14 nM, showing high selectivity against dipeptidyl peptidase (DPP)-related enzymes and prolyl oligopeptidase (PREP). BR103354 exhibited good pharmacokinetic properties as evidenced by oral bioavailability of 48.4% and minimal hERG inhibition. Single co-administration of BR103354 with hFGF21 reduced nonfasting blood glucose concentrations, in association with increased intact form of hFGF21 in ob/ob mice. BR103354 acts as an effective FAP inhibitor in vitro and in vivo, thereby demonstrating its potential application as an anti-diabetic and anti-NASH agent.

BR103 is a metabolically stable C3aR-selective agonist that can be used to assess the ligand affinity of G protein-coupled receptors and to induce paw edema models.

NIBR189 is a potent and selective antagonist of EBI2 (GPR183) receptor (IC50 of 11 and 15 nM for human and mouse EBI2 receptors, respectively)

CBR1-IN-3 (compound 13h) serves as a potent inhibitor of carbonyl reductase 1 (CBR1), exhibiting an IC 50 value of 0.034 μM [1].

CBR1-IN-4 (Compound 13p), with an IC50 value of 0.09 μM, acts as an inhibitor of human carbonyl reductase 1 (CBR1). This compound is applicable in cancer research [1].

CBR1-IN-5 (compound 13o) effectively inhibits CBR1, exhibiting an IC 50 value of 0.1 μM [1].

CBR1-IN-7 (Compound JV-2), with an IC50 value of 8 μM, serves as an inhibitor of human CBR1. This compound finds utility in cancer research [1].

BR102910 (4-Thiazolecarboxamide, N-[2-[(2S)-2-cyano-4,4-difluoro-1-pyrrolidinyl]-2-oxoethyl]-2-[(3,4-dichlorophenyl)methyl]-) is a selective inhibitor of fibroblast activated protein (FAP).

(Rac)-IBR120 is the racemate of IBR120, a RAD51 inhibitor that significantly suppresses the growth of MDA-MB-468 cells. It is applicable in research related to treatment-resistant cancers, such as triple-negative breast cancer.

Dabigatran etexilate (BIBR 1048) is a thrombin inhibitor that binds to thrombin, blocking its thrombogenic activity and preventing thrombus formation.

Dabigatran Etexilate Mesylate (BIBR 1048MS) is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI, Ki: 4.5 nM).

Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a potent inhibitor of dopamine uptake (IC50: 1-51 nM).

NIBR-17 is a pan class I PI3K inhibitor. NIBR-17 inhibits PI3KKα, PI3KKβ, PI3KKγ, and PI3KKδ with IC50 of 1 nM, 9.2 nM, 9 nM, and 20 nM respectively.

T-cell clones specific for this NY-BR-1 p904 A2 acetate(347142-73-8 free base) can recognize breast tumor cells expressing NY-BR-1.

AZ12601011 is an orally active, selective and potent TGFBR1 kinase inhibitor.AZ12601011 inhibits the release of inflammatory factors, interleukin (IL)-1β, IL-6 and tumor necrosis factor-α, and inhibits the growth of breast tumors.AZ12601011 directly binds to TGF-βR1 and blocks downstream Smad3 activation, which can be used to prevent renal fibrosis.

GBR 12783 can improve memory performance and increase hippocampal acetylcholine release in rats. GBR 12783 is a specific, potent and selective dopamine uptake inhibitor that inhibits the [3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively.

R-268712 is a specific activin receptor-like kinase 5 (ALK5) inhibitor(IC50 of 2.5 nM). It is also an orally active transforming growth factor-β type I receptor inhibitor.

GBR 12935 dihydrochloride (GBR 12935) can induce the increase of the extracellular levels of dopamine to basal levels.

GBR-12935 is a piperazine derivative. It is an effective and selective dopamine reuptake inhibitor. GBR-12935 is now widely used in animal research into Parkinson's disease and the dopamine pathways in the brain.