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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC11948 CK2 inhibitor D11
A potent, selective, cell permeab anti-apoptotic protein kinase CK2 with Ki of 5 nM.
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DC20549 SHP2 inhibitor 11a-1
A potent, selective, cell active SHP2 inhibitor with IC50 of 200 nM, displays >5-fold selectivity against 20 other mammalian PTPs.
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DC11894 Foliglurax
A potent, selective, brain-penetrant and orally bioavailable mGluR4 positive allosteric modulator with EC50 of 79 nM.
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DC11895 Foliglurax hydrochloride
A potent, selective, brain-penetrant and orally bioavailable mGluR4 positive allosteric modulator with EC50 of 79 nM.
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DC23640 ASP2535
A potent, selective, brain permeable, orally available glycine transporter-1 (GlyT1) inhibitor with IC50 of 92 nM (rat GlyT1), 50-fold selectivity over GlyT2.
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DC22920 AMN 082 dihydrochloride
A potent, selective, brain penetrant, orally acitve mGluR7 allosteric agonist that inhibits forskolin-stimulated cAMP accumulation in mGluR7b CHO cells with EC50 of 64±32 nM.
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DC23695 PF-05085727
A potent, selective, brain penetrant phosphodiesterase 2A (PDE2A) inhibitor with IC50 of 2 nM, >4,000-fold selectivity over PDE1 and PDE3-11.
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DC11660 PF-4181366
A potent, selective, brain penetrant PDE9A inhibitor with IC50 of 1.8 nM.
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DC22895 VU0477573
A potent, selective, brain penetrant partial negative allosteric modulator of mGlu5 receptor with Ki of 14 nM, Ca assay IC50 of 32 nM.
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DC23964 BMS-509744
A potent, selective, ATP-competitive ITK inhibitor with IC50 of 19 nM.
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DC23070 MAP4K4-IN-11e
A potent, selective, ATP-competitive inhibitor of MAP4K4 with IC50 of 1.9 uM, without effect on other stress pathway related kinases.
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DC22500 Bay 65-1942 hydrochloride
A potent, selective, ATP-competitive inhibitor of IKKβ kinase with Ki of 2 nM.
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DC23930 Bay 65-1942
A potent, selective, ATP-competitive inhibitor of IKKβ kinase with Ki of 2 nM.
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DC12007 SOMG-833
A potent, selective, ATP-competitive c-MET inhibitor with IC50 of 0.93 nM.
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DC11733 SAR-020106
A potent, selective, ATP-competitive Chk1 inhibitor with IC50 of 13.3 nM.
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DC11711 VER-158411
A potent, selective, ATP-competitive Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively.
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DC23867 PF-00337210
A potent, selective, ATP-competitive and orally bioavailable inhibitor of VEGFR-2 with Ki of 0.7 and 8.8 nM for unactivated and fully phosphorylated VEGFR-2, respectively.
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DC22651 PF-4950834
A potent, selective, ATP-competitive and orally acitve Rho kinase inhibitor with IC50 of 33.1 and 8.5 nM for ROCK1 and ROCK2, respectively.
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DC23036 BI-69A11
A potent, selective, ATP competitive AKT inhibitor with IC50 of 2.3 uM for Akt1.
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DC23949 CX-6258 hydrochloride hydrate
A potent, selective, and orally efficacious pan-Pim inhibitor with IC50 of 5/25/16 nM for Pim1/2/3, respectively.
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DC23541 IRAK4-IN-16
A potent, selective, and orally bioavailable inhibitor of interleukin-1 receptor-associate kinase-4 (IRAK4) with IC50 of 2.8 nM, 217- and 892-fold selectivity over IRAK-1 and TAK1, respectively.
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DC21254 LY-517717
A potent, selective, and orally bioavailable factor Xa (FXa) inhibitor for prevention and treatment of thromboembolic diseases..
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DC11728 RO-5353
A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 7 nM.
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DC11727 RO-2468
A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 6 nM.
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DC11850 MK-7145
A potent, selective, and oral renal outer medullary potassium channel (ROMK) inhibitor with IC50 of 68 nM.
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DC21545 PXS-4681A
A potent, selective, and irreversible inhibitor of SSAO/VAP-1 (AOC3) with Ki of 37 nM, IC50 of <10 nM.
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DC23963 QL-47
A potent, selective, and irreversible BTK inhibitor with IC50 of 7 nM.
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DC23971 LY450108
A potent, selective, and centrally active positive allosteric modulator of AMPAR-mediated neurotransmission, which increase ion channel flux in the presence of agonist by suppressing desensitization and/or deactivation of the receptors..
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DC22916 JNJ-10397049
A potent, selective, and bioavailable OX2 receptor antagonist with Kb of 4.5 nM.
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DC21316 ML400
A potent, selective, allosteric LMPTP inhibitor with IC50 of 1.68 uM, displays good selective against other phosphatases.
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