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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC8830 Betahistine Featured Betahistine is a strong affinity histamine H3 receptor antagonist and weak affinity agonist of histamine H1 receptors.
DC12320 Betanin Betanin has potent antioxidant and anti-inflammatory effect, that could inhibit peroxynitrite (ONOO-), with an IC50 of 19.2 μM. Betanin is a red glycoside obtained from beets that can be used as colorant.
DC8556 BET-BAY 002 BET-BAY 002 is a potent BET inhibitor; shows efficacy in a multiple myeloma model.
DC11566 BETd-260 Featured BETd-260 (ZBC260, BETd260) is a novel PROTAC BET degrader that tether HJB97 to a ligand for the E3 ubiquitin ligase VHL.
DC11567 BETd-260 trifluoroacetate BETd-260 trifluoroacetate (ZBC260, BETd 260 TFA) is a novel PROTAC BET degrader that tether HJB97 to a ligand for the E3 ubiquitin ligase VHL.
DC12131 BF-227(E/Z) Featured BF 227 is a candidate for an amyloid imaging probe for PET, with a Ki of 4.3 nM for Aβ1-42 fibrils.
DC20797 BF 844 BF 844 (BioFocus 844) is a small molecules capable of stabilizing mutant USH3 mutation CLRN1(N48K).
DC12136 BF-168 BF-168, a candidate probe for PET, is found to specifically recognize both neuritic and diffuse plaques, with a Ki of 6.4 nM for Aβ1-42.
DC20767 BF738735 BF738735 is a novel, broad-spectrum inhibitor of enterovirus replication (EC50=4-71 nM) that specifically targets host cell factor PI4KIIIβ with IC50 of 5.7 nM, 300-fold less potent for PI4KIIIα (IC50=1.7 uM).
DC10335 BGB-3111 BGB-3111 is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
DC22196 BGC20-1531 BGC20-1531 (PGN-1531, AP 1531) is a potent, selective prostanoid EP receptor EP antagonist, exhibits high affinity at recombinant human EP4 receptors expressed in cell lines (pKB=7.6) and native EP4 receptors in human cerebral and meningeal artery (pKB=7.
DC10059 BGG463 Featured BGG463 can inhibit c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants with a 50% inhibitory concentration (IC50) of 0.25 μM, 0.09 μM and 0.590 μM, respectively.
DC21359 BHC BHC (Myosin inhibitor BHC) is a small-molecule screen of skeletal muscle myosin inhibitor that suppresses movements without affecting membrane currents.
DC23177 BHPI BHPI is a potent, noncompetitive small molecule ERα inhibitor (biomodulator) that selectively blocks proliferation of drug-resistant ERα-positive breast and ovarian cancer cells.
DC9426 B-HT 920 B-HT 920(Talipexole 2Hcl) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays antiParkinsonian activity.
DC21546 BI-1467335 HCl Featured BI 1467335 (PXS-4728A, PXS-4728) is a potent, selective, orally active SSAO/VAP-1 (AOC3) inhibitor with IC50 of 5 nM; displays >500-fold selective for VAP-1/SSAO over all the related human amine oxidases; diminishes leukocyte rolling and adherence induced by CXCL1/KC, also inhibits the migration of neutrophils to the lungs in response to LPS, Klebsiella pneumoniae lung infection and CLP induced sepsis.
DC22021 BI 167107 Featured BI 167107 is a highly potent agonist of the β2 adrenergic receptor (β2AR) and β1AR (IC50=3.2 nM) and shows some activity as α1A antagonist (IC50 = 32 nM).
DC20776 BI 187004 BI 187004 (VTP-34072) is a novel potent, selective 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor intended to treat type 2 diabetes mellitus (T2D)..
DC20778 BI 207524 BI 207524 is a potent inhibitor of HCV thumb pocket 1 NS5B inhibitor with IC50 of 84 nM, inhibits Gt 1a/1b replicons with EC50 of 29/11 nM..
DC22026 BI 665915 BI 665915 is a highly potent, selective, orally active 5-lipoxygenase-activating protein (FLAP) inhibitor with binding IC50 of 1.7 nM.
DC20781 BI 671800 Featured BI 671800 is a potent, oral prostaglandin D2 receptor (CRTH2) antagonist for treatment of asthma..
DC23527 BI 6901 BI 6901 is a potent, selective CCR10 antagonist with Aequorin Ca2+ flux pIC50 of 9.0, shows high selectivity over other GPCRs.
DC23347 BI 7189 BI 7189 is a highly selective bromodomains of BRD9 and BRD7 inhibitor with IC50<50 nM for BRD9, displays >1,000 fold selectivity over the bromodomains of BRD4.
DC23391 BI 7271 BI 7271 is a highly selective bromodomains of BRD9 and BRD7 inhibitor with IC50<50 nM for BRD9.
DC20783 BI 831266 BI 831266 is a potent, selective inhibitor of Aurora kinase B (AURKB) with IC50 of binding IC50 of 42 nM.
DC11760 BI 885578 BI 885578 (BI-885578, BI885578) is a potent,selective, ATP-competitive IGF1R/InsR tyrosine kinase inhibitor with Kd of 9 nM/12 nM, IC50 of 1 nM/1 nM, respectively.
DC23348 BI 894999 BI 894999 is a novel potent, selective BET inhibitor with IC50 of 5 and 41 nM for BRD4-BD1 and BRD4-BD2 bromodomains, respectively.
DC23560 BI01383298 Featured BI01383298 (BI-01383298) is a potent, specific sodium-citrate co-transporter SLC13A5 (NaCT, INDY), highly selective over other family members and other transporters..
DC12406 BI-0314 Featured BI-0314 (BI0314) is an allosteric activator of protein tyrosine phosphatase non-receptor type 5 (PTPN5, STEP) with potency of 56% at 500 uM, displays no activity against hPTP1B and hTCPTP.
DC23049 BI1002494 BI1002494 (BI-1002494) is a novel, potent, and selective spleen tyrosine kinase (SYK) inhibitor with enzyme IC50 of 30 nM, cell IC50 of 7 nM (FcεR1-mediated histamine release in human monocyte-derived mast cells, in the presence of 0.1% albumin).

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