r 112

R112 is an ATP-competitive inhibitor of Syk kinase. Ki=6 nM,IC50=226 nM.

DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM for EGFRWT and 48 nM for EGFRL858R/T790M, capable of occupying the ATP-binding site and demonstrating significant antitumor efficacy.

SR11237 is a Pan retinoid X receptor (RXR) agonist. SR11237 causes RXR/RXR homodimers to form and transactivate a reporter gene containing a RXR-response element.

(12aR)-1,12-Bis(diphenylphosphino)-6,7-dihydrodibenzo[e,g][1,4]dioxocine is a useful organic compound for research related to life sciences and the catalog number is T67395.

DBPR112 is a potent EGFR inhibitor (IC50=487 nM) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. DBPR112), DBPR112 not only displayed a potent inhibitory activity against EGFRL858R/T790M double mutations but also exhibited tenfold potency better than the third-generation inhibitor, osimertinib,against EGFR and HER2 exon 20 insertion mutations. Overall, pharmacokinetic improvement through lead-to-candidate optimization yielded fourfold oral AUC better that afatinib along with F = 41.5%, an encouraging safety profile, and significant antitumor efficacy in in vivo xenograft models.

Berupipam is a dopamine D1 receptor antagonist.

GR-112000 is a peptide-based tachykinin NK2 receptor antagonist.

UR-144, a synthetic cannabinoid, exhibits high affinity for the peripheral cannabinoid receptor (CB2) with a Ki of 1.8 nM, markedly greater than its affinity for the central cannabinoid receptor (CB1), for which it has a Ki of 150 nM. XLR-11 differs from UR-144 by featuring a fluorine atom on the terminal carbon of the alkyl chain and a methyl group on the C2 carbon of the indole. The specific biological activities of XLR-11 remain uncharacterized. It is designed for forensic and research use only.

SR11254-CoA (SR11254-coenzyme A) is a derivative of coenzyme A.

Histone H2B (108-125) is a peptide fragment of histone H2B that corresponds to amino acid residues 109-126 of the human histone H2B sequence. It contains an N-terminal biotinylated lysine followed by a tryptophan linker. Histone H2B can be modified by addition of an O-linked N-acetylglucosamine (GlcNAc) moiety to the serine residue at position 112, which promotes monoubiquitination of the lysine at position 120.1 Both of these modifications are associated with active transcription. Histone H2B also has lysine residues at positions 108, 116, and 120 that are subject to acetylation.2References1. Fujiki, R., Hashiba, W., Sekine, H., et al. GlcNAcylation of histone H2B facilitates its monoubiquitination. Nature 480(7378), 557-560 (2011).2. Portela, A., and Esteller, M. Epigenetic modifications and human disease. Nat. Biotechnol. 28(10), 1057-1068 (2010). Histone H2B (108-125) is a peptide fragment of histone H2B that corresponds to amino acid residues 109-126 of the human histone H2B sequence. It contains an N-terminal biotinylated lysine followed by a tryptophan linker. Histone H2B can be modified by addition of an O-linked N-acetylglucosamine (GlcNAc) moiety to the serine residue at position 112, which promotes monoubiquitination of the lysine at position 120.1 Both of these modifications are associated with active transcription. Histone H2B also has lysine residues at positions 108, 116, and 120 that are subject to acetylation.2 References1. Fujiki, R., Hashiba, W., Sekine, H., et al. GlcNAcylation of histone H2B facilitates its monoubiquitination. Nature 480(7378), 557-560 (2011).2. Portela, A., and Esteller, M. Epigenetic modifications and human disease. Nat. Biotechnol. 28(10), 1057-1068 (2010).

Pseurotin A has immunosuppressive activity, it inhibits immunoglobulin E(IgE) production in vitro.It shows a moderate effect against the phytopathogenic bacteria Erwinia carotovora and Pseudomonas syringae, with IC50 values of 220 and 112 microg ml(-1), r