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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC21802 VU 0364849 A potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 5.4 nM.
DC21807 VU 0465350 Featured VU 0465350 is a potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 92.3 nM; shows no activity for ALK2/4/5, also shows affinity for TGFBR2, VEGFR2 and AMPK; blocks SMAD phosphorylation in vitro and in vivo, and enhances liver regeneration after partial hepatectomy.
DC21693 SRI-29329 A potent, specific CDC-like kinase (CLK) inhibitor with IC50 of 78, 16 and 86 nM for CLK1, 2 and4, respectively.
DC21794 VH 298 Featured A potent, specific cell-active VHL E3 ubiquitin ligase inhibitor that inhibits VHL/HIF-α interaction with Kd of 90 nM in ITC assays.
DC23985 Laduviglusib trihydrochloride Featured Laduviglusib (CHIR-99021) trihydrochloride is a well-characterized small molecule inhibitor that specifically targets glycogen synthase kinase-3 alpha and beta (GSK-3α/β). It exhibits potent inhibitory activity with IC50 values of 10 nM for GSK-3α and 6.7 nM for GSK-3β. Importantly, it demonstrates high selectivity, being over 500-fold more selective for GSK-3 compared to other kinases such as CDC2 and ERK2, as well as a broad range of other protein kinases.
DC21150 PR-924 A potent, specific immunoproteasome LMP7 subunit inhibitor with IC50 of 25 nM, >100-fold selectivity over β5c, β1i, β1c, β2i and β2c subunits (IC50>3 uM).
DC21773 UK-101 A potent, specific immunoproteasome β1i (LMP2) subunit inhibitor with IC50 of 104 nM, 144- and 10-fold selectivity over β1c and β5 subunit respectivey.
DC21527 PR-893 A potent, specific immunoproteasome β5 subunit inhibitor with IC50 of 17 nM, 21-fold and 13-fold selectivity for β5 over LMP7 and LMP2 subunits, respecitvely..
DC21365 NC-005 A potent, specific immunoproteasome β5 subunit inhibitor with IC50 of 44 nM, 105 and 225-fold selectivity over β2i and β1i subunit, respecitvely.
DC21528 PR-825 A potent, specific immunoproteasome β5 subunit inhibitor..
DC24007 R-1479 Featured A potent, specific inhibitor of HCV NS5B polymerase and HCV replication (IC50=1.28 uM, replicon assay).
DC22758 SI-113 A potent, specific inhibitor of the SGK1 kinase activity, induces autophagy, apoptosis and ER stress in cancer cells.
DC11871 MMV019313 Featured MMV019313 (MMV 019313, MMV-019313) is a potent, specific malaria bifunctional farnesyl/geranylgeranyl diphosphate synthase (FPPS/GGPPS) inhibitor with IC50 of 330 nM; shows no activity against human FPPS or GGPPS (>200 uM); exhibits distinct modes of inhibition compared with bisphosphonates, inhibits P. falciparum growth with EC50 of 268 nM, overexpression and an S228T variant of PfFPPS/GGPPS confer resistance to MMV 019313.
DC20998 ES 936 A potent, specific mechanism-based human NAD(P)H: quinone oxidoreductase 1 (NQO1) inhibitor that demonstrates efficient inactivation of NQO1 at 100 nM in in cellular systems.
DC22823 Tariquidar methanesulfonate hydrate A potent, specific P-gp inhibitor with Kd of 5.1 nM.
DC21849 YU-101 A potent, specific proteasome β5 subunit inhibitor with IC50 of 0.26 uM, 7.3 and 17.3-fold selectivity over β2i and β1i subunit, respecitvely..
DC26068 BMS-753 A potent, specific RARα agonist with Ki of 2 nM, displays no significant effects on RARγ in reporter based assays..
DC22661 AB1 A potent, specific S1P2 receptor (Edg-5) antagonist with IC50 of 3 nM, with no agonistic or antagonistic activities on other S1PRs.
DC24060 YM-155 hydrochloride Featured A potent, specific survivin inhibitor that inhibits survivin promoter activity with IC50 of 0.54 nM.
DC22864 KSP-IA A potent, specific, allosteric and cell-active inhibitor of KSP with IC50 of 11 nM.
DC22865 CK-0106023 Featured A potent, specific, allosteric inhibitor of KSP motor domain ATPase with Ki of 12 nM.
DC21318 ML 171 A potent, specific, cell-active NADPH oxidase1 (Nox1) inhibitor that strongly blocks ROS generation in HT29 cells with IC50 of 0.129 uM.
DC20890 ChoK-α inhibitor CK37 Featured A potent, specific, competitive inhibitor of choline kinase-α (Chok-α) by targeting the choline binding site; significantly increases LC3II expression in MCF-7 and MCF-7/TAM cells, increases the size and number of autophagosome, causes MCF-7 and MCF-7/TAM
DC21110 HCI-2389 A potent, specific, irreversible NIMA-related Kinase 2 (NEK2) inhibitor with IC50 of 16.65 nM.
DC11977 SX-517 A potent, specific, noncompetitive dual CXCR1 and CXCR2 antagonist with IC50 of 38 nM (vs. CXCL1) and 36 nM (vs. CXCL8), respectively.
DC11716 XL-844 A potent, specific, orally available, ATP‑competitive inhibitor of Chk1 and Chk2 with Ki of 2.2 nM and 0.07 nM, respectively.
DC11766 UbcH5c-IN-6d A potent, specific, orally bioactive small-molecule inhibitor of ubiquitin-conjugating enzyme UbcH5c with Kd of 283 nM.
DC22550 TAK-220 A potent, specific, orally bioavailable CCR5 antagonist that blocks the binding of MIP-1α to CCR5 with IC50 of 1.4 nM.
DC22540 Pasireotide Featured Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity. At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Pasireotide acetate) usually boasts enhanced water solubility and stability.
DC22539 Pasireotide L-aspartate salt A potent, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (pKi=8.2/9.0/9.1/<7.0/9.9 for sst1/2/3/4/5, respectively).

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