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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
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).
DC11842 BI 135585 BI 135585 (BI-135585, BI135585) is a potent, selective, orally active 11β-HSD1 inhibitor with IC50 of 4.3 nM and 53 nM in human adipocytes and primary human adipose tissue, respectively.
DC22020 BI-1388 BI-1388 is a potent, specific, macrocyclic inhibitor of HCV NS3 protease, inhibits viral replication for various HCV genotypes and for resistant mutants D168V and R155K.
DC20777 BI-1935 BI-1935 is a potent, selective small molecule inhibitor of soluble epoxide hydrolase (sEH) with IC50 of 7 nM.
DC22022 BI-1950 BI-1950 is a potent, selective LFA-1 antagonist that inhibits the binding of LFA-1 to ICAM-1 with Kd value of 9 nM.
DC11602 BI-2545 BI-2545 is a novel potent, selective, orally available Autotaxin inhibitor with IC50 of 2.1 and 3.4 nM for huamn and rat ATX, respectively.
DC22023 BI-3663 BI-3663 (BI 3663) is a cereblon-based degrader (PROTAC) of Focal adhesion tyrosine kinase (PTK2/FAK) with a median DC50 of 30 nM to >80% across a panel of eleven HCC cell lines.
DC22024 BI-4394 BI-4394 is a highly potent, selective MMP-13 inhibitor with IC50 of 1 nM, displays >1,000 fold selectivity against nine other MMP isoforms (MMP2/14, IC50=18/8.3 uM).
DC11960 BI605906 Featured BI605906 is a potent, specific IKKβ inhibitor with IC50 of 380 nM (0.1 mM ATP), does not suppress signaling downstream of mTOR or activate AMPK.
DC20784 BI8622 BI8622 (BI-8622) is a specific small molecule inhibitor of the HUWE1 ubiquitin ligase with IC50 of 3.1 uM, does not inhibit the activity of other HECT-domain ubiquitin ligases (HECW2, NEDD4,UBA1 and UbcH5b).
DC20785 BI8626 BI8626 (BI-8626) is a specific, small molecule inhibitor of the HUWE1 ubiquitin ligase with IC50 of 0.9 uM, does not inhibit the activity of other HECT-domain ubiquitin ligases (HECW2, NEDD4,UBA1 and UbcH5b, IC50>50 uM).
DC23608 BI-9627 BI-9627 is a potent, selective inhibitor of sodium-hydrogen exchanger isoform 1 (NHE1) with pHi change IC50 of 6 nM, displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform.
DC12567 BI-9667 BI-9667 (BI9667) is a potent, selective CCR1 antagonist..
DC22027 BI-99179 BI-99179 is a potent and selective inhibitor of type I fatty acid synthase (FAS) with IC50 of 79 nM.

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