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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
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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DC74337 DK2403
DK2403 (DK-2403) is a highly potent, selective and covalent MAP2K7 (MEK7) inhibitor with IC50 of 10 nM, covalently engages the unique Cys218 residue within the active site.
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DC74335 MMI-0100
MMI-0100 is a cell-permeant peptide inhibitor of MAPKAP kinase 2 (MK2), inhibits MK2 and downstream fibrosis and inflammation.
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DC74334 F389-0746
F389-0746 is a potent, selective and orally active MAP4K4 inhibitor with IC50 of 120.7 nM.
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DC74332 YL5084
YL5084 (YL 5084) is a potent, selective and covalent JNK2/3 inhibitor with IC50 of 70 nM (JNK2), displays selectivity (>30-fold) for JNK2 over JNK1.
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DC74331 UM130646
UM130646 (UM 130646) is a specific small molecule E2 enzyme UBCH10 inhibitor with IC50 of 20.3 uM in TR-FRET UBCH10 autoubiquitination assays, inhibits UBCH10 E2 activity and antagonizes APC/C-mediated substrate degradation.
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DC74329 ETC-6152
ETC-6152 is a potent, specific and covalent E2 ubiquitin ligase UBE2T inhibitor with IC50 of 0.22 uM, targets Cys86 of UBE2T and shows selectivity on UBE2T over UBE2K.
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DC74328 WZ-1831
WZ-1831 is a potent and highly selective inhibitor of human constitutive proteasome chymotryptic activity (β5c) with IC50 of 10 nM, >500-fold selectivity over β5i (IC50=7.1 uM).
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DC74327 TXS-8
TXS-8 is a specific, small molecule binder of Rpn-6 with KD of 14 uM, Rpn-6 is a subunit of the 19S regulatory particle (RP) of 26s proteasome.
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DC74326 TCL-Ester
TCL-Ester is the cell-permeable derivative of TCL-1, a non-covalent ligand targeting the Pru domain of Rpn-13.
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DC74325 TCL-1
TCL-1 is a non-covalent ligand targeting the Pru domain of Rpn-13, TCL-1 binds to the Pru domain at the Rpn-2 docking site, affects proteasome-mediated proteolysis.
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DC74324 KDT-11
KDT-11 is a specific, reversible peptidomimetic binder inhibitor of Rpn-13 with binding KD of 3 uM, selectively inhibit proliferation of a broad range of cancer cell lines (NCI60, IC50=5 uM), but not non-malignant cells.
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DC74323 BT317
BT317 is a small molecule dual inhibitor of mitochondrial Lon Peptidase 1 (LonP1) and CT-L proteasome, subsequently induces ROS accumulation and autophagy-dependent cell death in high-grade IDH1 mutated astrocytoma lines.
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DC74322 VCP Activator 1
VCP Activator 1 (VA1) is a small molecule allosteric activator of valosin-containing protein (VCP)/p97, dose-dependently stimulates VCP ATPase activity up to 3-fold (EC50= 4 uM).
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DC74321 UPCDC-30766
UPCDC-30766 (UPCDC 30766) is a potent, allosteric inhibitor of AAA+ ATPase p97 (valosin-containing protein, VCP) with biochemical IC50 of 12 nM, EC50 of 226 nM in cellular UbG76V-GFP accumulation assays.
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DC74319 NW1030
NW1030 is a small molecule that target the regulatory domain of VCP/p97, increases the degradation of a p97-dependent reporter, does not affect the main catalytic domain of p97.
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DC74318 NW1028
NW1028 is a small molecule that target the regulatory domain of VCP/p97, inhibits the degradation of a p97-dependent reporter, does not affect the main catalytic domain of p97.
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DC74317 STA-1474
STA-1474 is a water soluble prodrug of Ganetespib (STA 9090), which is a potent, second generation small-molecule inhibitor of HSP90 (IC50=4 nM).
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DC74316 SOMCL-16-175
SOMCL-16-175 is a non-covalent, allosteric modulator targeting Hsp90α’s middle domain (Hsp90M) with binding Kd of 804 uM, inhibits breast cancer cell growth and proliferation.
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DC74315 SL-145
SL-145 is a novel C-terminal HSP90 inhibitor, induces apoptosis in TNBC cells via the suppression of oncogenic AKT, MEK/ERK, and JAK2/STAT3 signaling.
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