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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC74464 LPD-01
LPD-01 is a small molecule inhibitor of the Wnt/β-catenin signaling pathway, directly binds to importin7, inhibits the transactivation of target genes of the Wnt/β-catenin signaling pathway.
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DC74463 ISQ-1
ISQ-1 is a potent in vitro inhibitor of several cancer cell lines (LS174T cell proliferation, IC50=100 nM), inhibits Wnt signaling and also activates adenosine monophosphate kinase (AMPK).
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DC74462 C644-0303
C644-0303 is a novel Wnt/β-catenin signaling inhibitor (IC50=4.2 uM) with antitumor efficacy, inhibits both constitutive and ligand activated Wnt signals and its downstream gene expression.
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DC74461 INS018_055
INS018_055 (INS018-055) a selective small-molecule TRAF2- and NCK-interacting kinase (TNIK) inhibitor with Kd value of 4.32 nM and IC50 of 31 nM, inhibits TGF-β-induced α-SMA protein expression in MRC-5 cells with IC50 of 27.14 nM.
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DC74460 MRT-92
MRT-92 is a potent selective Smoothened (Smo) receptor antagonist (Kd=0.3 nM), inhibits rodent cerebellar granule cell proliferation induced by Hh pathway activation with IC50 of 0.4 nM.
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DC74458 AG-1031
AG-1031 (AG1031) is a specific small molecule inhibitor of the double-stranded DNA binding activity of positive coactivator 4 (PC4) with IC50 of 2.5 uM, more effectively than its single-stranded DNA binding activity (IC50=15 uM).
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DC74457 UNC-SOB-5-16
UNC-SOB-5-16 is a potent, selective STK3 small-molecule inhibitor with IC50 of 22 nM, also inhibits LRRK2.
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DC74456 UNC-BE4-017
UNC-BE4-017 is a selective STK3 small-molecule inhibitor, also potently inhibits JAK1, JAK2, and JAK3, but not other kinases in a panel of 48 kinases.
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DC74453 Picoberin
Picoberin is a highly potent (low picomolar) inhibitor of purmorphamine- and Sonic Hedgehog (Shh)-induced osteogenesis with IC50 of 3 pM, acts as an AhR agonist and induces the expression of AhR target genes, thereby suppressing osteoblast differentiation
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DC74452 MDB5
MDB5 is a potent hedgehog (Hh) signaling pathway inhibitor, exhibits stronger inhibition of the Hh pathway and anticancer effect in vitro and vivo than GDC-0449.
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DC74451 NPL-4011
NPL-4011 is a specific small molecule inhibitor of PDZ domain of human Dvl1 (Dvl1-PDZ) with KD vaule of 34.5 uM in NMR titration experiments.
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DC74450 BMD4722
BMD4722 is a highly potent, small-molecule inhibitor of Dvl-CXXC5 interaction with IC50 of 2.59 uM, directly binds to the Dvl PDZ domain (Kd=22.3 uM).
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DC74449 BMD4702
BMD4702 is a small molecule Dishevelled (Dvl) PDZ domain with binding Kd of 186 nM.
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DC74448 SR-4133
SR-4133 (SR4133) is a potent and highly selective CK1ε isoform inhibitor with IC50 of 58 nM, no significant acitivity agianst CK1δ (IC50>10,000 nM).
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DC74447 SGC-CK2-1 analog 2h
SGC-CK2-1 analog 2h is potent, selective and in vivo active inhibitor of casein kinase 2α (CSNK2A, CK2α) with pIC50 of 7.5 and 7.7 against CSNK2A1 and CSNK2A2, respectively.
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DC74444 CKR-49-17
CKR-49-17 is a potent, allosteric small molecule activator of CK1γ2 with Kd value of 180 nM in MST assays.
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DC74443 AB668
AB668 is a selective, bivalent Casein Kinase 2 (CK2) inhibitor targeting the ATP site and the αD pocket, AB668 inhibits the CK2 holoenzyme with Ki value of 41 nM (IC50=65 nM).
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DC74442 IMU1003
IMU1003 (IMU-1003) is a small molecule inhibitor of Wnt/β-catenin signaling, decreases β-catenin levels and inhibits target gene expression that promotes cancer cell proliferation.
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DC74439 SYHA1813
SYHA1813 is a potent dual inhibitor of CSF1R and VEGFR with IC50 of 19.3, 2.8, 0.3, and 4.3 nM for CSF1R, VEGFR1, 2, and 3, respectively.
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DC74437 NRP1-4
NRP1-4 (Neuropilin 1-4) is a highly potent, specific small molecule inhibitor of VEGF-A binding to neuropilin 1 (NRP1) with IC50 of 0.598 nM, reduces calcium and sodium currents through binding to NRP1 and inhibits the effects of VEGF-A.
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DC74436 COB223
COB223 is a chemical inhibitor of angiogenesis and tumorigenesis, targets the VEGF signaling pathway upstream of Ras, inhibits endothelial cell migration with IC50 of 5 uM.
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DC74435 PTX-BD10-2
PTX-BD10-2 (BD10-2) is a selective, brain-penetrant small molecule TrkB/C receptor partial agonist, shows survival-promoting activity.
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DC74434 Emzeltrectinib
Emzeltrectinib is a potent, selective neurotrophic factor tyrosine kinase receptor TrkB inhibitor, shows potential for treatment of Trk kinase-mediated tumor.
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DC74433 Anizatrectinib
Anizatrectinib is a potent and orally active inhibitor of TrkA kinase with potential for inflammatory disease such as prostatitis.
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DC74432 UNC2025 hydrochloride
UNC2025 is a potent, orally bioavailable Mer/FLT3 dual inhibitor with IC50 of 0.74/0.8 nM, 700-fold less active against Met compared to Mer.
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DC74431 R992
R992 (MERTK inhibitor) is a novel potent, selective and orally bioavailable inhibitor of Mer tyrosine kinase (MerTK) with IC50 of 18 nM in ADP-Glo assays.
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DC74430 INCB081776
INCB081776 is a potent and selective dual inhibitor of AXL and MERTK with IC50 of 16 and 14 nM respectively, 30-fold selectivity over TYRO3.
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DC74429 ER-851
ER851 (ER-851) is a potent and highly selective AXL inhibitor.
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DC74428 Adrixetinib
Adrixetinib is a small molecule inhibitor of Axl/Mer RTK.
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DC74427 RDN2150
RDN2150 is a potent, selective and covalent ZAP-70 inhibitor with IC50 of 14.6 nM, shows no significant activity against Syk, covalently binds to the C346 residue of ZAP-70.
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