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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC74376 Ensartinib dihydrochloride
Ensartinib (X-396) dihydrochloride is a potent, selective and second-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) with biochemical IC50 of <0.4 nM, inhibits MET with IC50 of 0.74 nM.
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DC74375 SRI-31277
SRI-31277 is a tripeptide inhibitor of thrombospondin 1 activation of TGF-β, specifically inhibits TGF-β activation mediated through TSP-1 with pIC50 of 8.28 nM.
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DC74374 Ki26894
Ki26894 (Ki 26894) is a small molecule TGF-beta type I receptor (TbetaR-I) kinase inhibitor, inhibits TGF-β-induced transcriptional activation in MDA-231-D-TβFluc/Rluc cells with IC50 of 0.49 uM.
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DC74373 CDD-1653
CDD-1653 (CDD1653) is a potent, selective inhibitor of BMP type 2 receptor BMPR2 with IC50 of 2.8 nM, >360-fold over ALK1, and is inactive versus all other type 1 and type 2 TGFβ family kinases.
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DC74371 CDD-1115
CDD-1115 (CDD1115) is a potent, selective inhibitor of BMP type 2 receptor BMPR2 with IC50 of 1.8 nM and Kiapp of 6.2 nM.
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DC74370 Z640
Z640 is a novel non-selective atypical PKC (aPKC) agonist, increases PKCζ and PKCι kinase activity with EC50 of 1.09 and 3.47 µM in vitro kinase activity assays, respectively.
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DC74369 SIJ1795
SIJ1795 is a potent mutated RAS (mtRAS)-signaling pathway blocker/inhibitor with IC50 of 82 and 75 nM for Ba/F3-NRAS-G12D and Ba/F3-NRAS-G12V, respectively.
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DC74368 SIJ1772
SIJ1772 is a potent mutated RAS (mtRAS)-signaling pathway blocker/inhibitor with IC50 of 77 and 96 nM for Ba/F3-NRAS-G12D and Ba/F3-NRAS-G12V, respectively.
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DC74367 SCH53239
SCH-53239 (SCH53239) is a small molecule inhibitor of Ras nucleotide exchange with IC50 of 0.5 uM, bind competitively with GDP in the nucleotide binding site of the Ras protein.
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DC74366 RSC-1255
RSC-1255 (KRAS inhibitor 249C, V-ATPase inhibitor) is a Ras-mutant selective cytotoxic agent with nanomolar potency against a spectrum of Ras-mutant cancer cells (A549 (KRASG12S), IC50=73 nM), binds to V-ATPase (Kd=23 nM) and inhibits its activity.
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DC74364 G12Si-5
G12Si-5 is a specific small molecule that covalently target K-Ras(G12S) mutation, suppresses K-Ras(G12S) signaling, preferentially inhibits the growth of the K-Ras(G12S)-transduced cells with IC50 of 2.4 uM.
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DC74363 Fulzerasib
Fulzerasib is a potent selective inhibitor of KRAS gene mutation.
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DC74362 ERAS-5024
ERAS-5024 (ERAS5024) is a potent and selective KRAS G12D inhibitor with IC50 of 0.86 nM in RAS-RAF binding assays, inhibits ERK1/2 phosphorylation (pERK) formation with IC50 of 2.1 nM in AsPC-1 cell-based assays.
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DC74361 CSC01
CSC01 is a small molecule inhibitor of oncogenic KRAS mutant G13D (KRAS-G13D).
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DC74359 BBO-8956
BBO-8956 is a highly potent, covalent inhibitor of GTP-KRAS G12C, BBO-8956 is effective against both GDP and GTP-bound KRAS G12C.
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DC74358 ASP6918
ASP6918 (ASP 6918) is a highly potent, covalent KRAS G12C inhibitor with IC50 of 28 nM in cell-free assays, and pERK inhibition IC50 of 3.7 nM in NCI-H1373 cells.
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DC74357 ADT-007
ADT-007 (ADT007) is a potent, specific pan-RAS inhibitor, shows potential to circumvent resistance to mutant-specific KRAS inhibitors and activates antitumor immunity.
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DC74356 ACA22
ACA22 is a small molecule KRAS inhibitor, inhibits KRAS-mediated signal transduction in cells expressing wild type (WT) and G12D mutant KRAS.
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DC74355 ACA-14
ACA-14 is a small molecule direct inhibitor of KRAS, impedes the interaction of KRAS with its effector Raf and reduces both intrinsic and SOS-mediated nucleotide exchange rates.
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DC74354 6H05 trifluoroacetate
6H05 is a selective, allosteric inhibitor of oncogenic mutant K-Ras(G12C), an intermediate for the synthesis of other oncogenic K-Ras(G12C) inhibitors..
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DC74353 1-AM
A potent, selective, covalent KRAS G12C inhibitor that selectively inhibit KRAS G12C-dependent signaling and cancer cell growth at sub-micromolar concentrations..
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DC74352 Uplarafenib
Uplarafenib is a potent, selective small molecule inhibitor of BRAF kinase (IC50=50-100 nM) with antineoplastic activities.
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DC74351 IHMT-RAF-128
IHMT-RAF-128 is a highly potent pan-RAF inhibitor with IC50 of 5.9 and 3.6 nM for BRAF-V600E and CRAF, respectively.
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DC74350 VCP979
VCP979 (VCP-979) is a novel selective small molecule p38 MAPK inhibitor with a significantly greater affinity for the active form of p38 MAPK, has significant anti-fibrotic effects in vitro and in vivo.
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DC74348 NC-p38i NC-38
Non-canonical p38α inhibitor NC-38 (NC-p38i NC-38) is a potent, highly selective, non-canonical inhibitor of p38α, inhibits TAB1-induced p38α autophosphorylation in vitro with IC50 of 0.27 uM.
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DC74346 DCZ19931
DCZ19931 is a novel multi-targeting kinase inhibitor, exhibits anti-angiogenic effects in vitro and inhibits ocular neovascularization in vivo.
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DC74345 TC13172
TC13172 (TC 13172) is a highly potent necroptosis inhibitor targeting the mixed lineage kinase domain-like protein (MLKL), inhibits necroptosis with IC50 of 2 nM in TSZ-induced necroptosis assays in HT-29 cells.
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DC74344 KC-130
KC-130 (KC130, ZAK inhibitor 8) is a potent, selective and covalent leucine-zipper and sterile-α motif kinase (ZAK) inhibitor with IC50 of 11.5 nM.
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DC74342 IACS-52825
IACS-52825 is a potent, selective dual leucine zipper kinase (DLK, MAP3K12) inhibitor with binding Kd of 1.3 nM, and IC50 of 107 nM in p-c-Jun cell assays.
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DC74340 KZ-001
KZ-001 is a highly potent and selective MEK 1/2 inhibitor with IC50 values of 7.4/64 nM, respectively, exhibits greater inhibition against BRAF- and KRAS-mutant tumor cells than AZD6244.
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