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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC74478 BSJ-04-146
BSJ-04-146 is a potent, selective FAK PROTAC (IC50=26 nM), induces potent and durable FAK degradation in pancreatic and breast cancer cell lines at 10 nM.
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DC74477 BJG-05-039
BJG-05-039 is a PAK1-selective degrader consisting of NVS-PAK1-1 conjugated to lenalidomide, a recruiter of the E3 ubiquitin ligase substrate adaptor Cereblon.
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DC74476 BI 1810284
BI 1810284 (ACBI2, BI 01810284) is a potent, selective and orally bioavailable VHL-recruiting PROTAC degrader of SMARCA2 (DC50=1 nM in RKO cells), 30-fold selectivity over SMARCA4.
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DC74475 ARD-1676
ARD-1676 (ARD1676) is a highly potent and orally efficacious PROTAC degrader of the androgen receptor (AR) with DC50 values of 0.1 and 1.1 nM in AR+ VCaP and LNCaP cell lines, respectively.
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DC74474 (R)-SL18
(R)-SL18 is a first-in-class, selective Annexin A3 (ANXA3) degrader, induces degradation of ANXA3 in MDA-MB-231 cells with DC50 value of 3.17 uM.
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DC74473 Thalidomide-O-PEG4-Acid
Thalidomide-O-PEG4-Acid is a chemical linker for PROTAC design.
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DC74472 EN106 derivative 2
EN106 derivative 2 is a EN106 derivative used for PROTAC design, EN106 is a covalent ligand and recruiter for FEM1B E3 ligase for targeted protein degradation.
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DC74471 EN106 derivative 1
EN106 derivative 1 is a EN106 derivative used for PROTAC design, EN106 is a covalent ligand and recruiter for FEM1B E3 ligase for targeted protein degradation.
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DC74469 ZD06519
ZD06519 is a novel camptothecin payload for antibody drug conjugates (ADCs) with highp ayload potency (~1 nM).
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DC74468 WHN-88
WHN-88 is a potent, selective Porcupine (PORCN) inhibitor, inhibits Wnt/β-catenin signaling with IC50 of ST-Luc of 0.02 uM.
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DC74466 AMG2008827
A potent, selective γ-secretase inhibitor that significantly reduces the right ventricular systolic pressure and right heart hypertrophy in hypoxia/SU5416 (SUHx) rats..
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DC74465 WNTinib
WNTinib is a multi-kinase inhibitor with specificity against β-catenin (CTNNB1) mutant hepatocellular carcinoma, harnesses the KIT/MAPK/EZH2 pathway, shows durable and selective transcriptional repression of mutant β-catenin/Wnt targets through nuclear tr
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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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DC74455 TRULI
TRULI is a small molecule Yap signaling activator, acts as an ATP-competitive inhibitor of Lats kinases in vitro (Lats1 kinase, IC50=0.2 nM, 10 uM ATP), prevents Yap phosphorylation in the cell-based assays with EC50 of 510 nM.
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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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