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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC73192 KY386
KY386 is a potent, selective inhibitor of RNA helicase DHX33 with IC50 of 19 nM.
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DC73190 H3B-968
H3B-968 is a potent, selective and covalent inhibitor of Werner syndrome protein (WRN) helicase activity with IC50 of 41 and 13 nM in ADP-Glo assay DNA unwinding assay, respectively.
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DC73187 NSC373981
NSC373981 (NSC 373981) is a CARD11 G-quadruplex (G4) stabilizing small molecule that downregulates CARD11 gene expression in DLBCL cells.
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DC73186 CDEAH
CDEAH is a monofunctional alkylating agent that selectively kills PARP1- and xeroderma pigmentosum A-deficient cells.
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DC73185 AST-3424 (S-isomer)
OBI-3424 S-isomer (TH-3424, OBI 3424) is a highly potent DNA alkylating prodrug that is converted by AKR1C3 to a potent DNA-alkylating agent.
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DC73184 ZSQ836
ZSQ836 (ZSQ 836) is a potent, selective and orally bioavailable CDK12/CDK13 covalent inhibitor with IC50 of 32 nM (CDK12), covalently interacts with Cys1039 of CDK12.
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DC73183 ZNL-05-044
ZNL-05-044 is a potent, selective CDK11 inhibitor with Kd of 69 nM (CDK11A), shows significantly kinome-wide selectivity. ZNL-05-044 treatment leads to G2/M cell cycle arrest, impacts CDK11-dependent mRNA splicing in cells.
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DC73182 YPN-005
YPN-005 (YPN005) is a highly potent, selective inhibitor of cyclin-dependent kinase 7 (CDK7) with IC50 of 31 nM, with low inhibition for CDK2 and CDK5.
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DC73180 TMX-2039
TMX-2039 is a pan-CDK inhibitor with low nanomolar enzymatic IC50s (0.5-50 nM) for both cell cycle CDKs (CDK1, CDK2, CDK4, and CDK6) and transcriptional CDKs (CDK7 and CDK9).
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DC73177 RGB-286199
RGB-286199 (GPC-286199) is a potent broad spectrum CDKs (cyclin dependent kinases) inhibitor with IC50 of 5-100 nM against CDKs 1-6, shows antiproliferative activity in vitro and in vivo.
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DC73174 MK256
MK256 (MK-256) is a potent, selective CDK8 inhibitor with IC50 of 2.5 nM and 3.3 nM against CDK8/cyclin C and CDK19/cyclin C, respectively.
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DC73173 MER-128
MER-128 is a potent, selective CDK20 inhibitor with IC50 of 2 nM.
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DC73172 LGR6768
LGR6768 is a potent, selective CDK7 inhibitor with IC50 of 20 nM, >12-fold selectivity over other CDKs.
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DC73169 ERP1.28a
ERP1.28a is a selective, small molecule inhibitor of cell division cell cycle kinase 7 (CDC-7) with IC50 of 140 nM, decreases the enhanced TDP-43 phosphorylation in cells derived from TDP-43-related pathogenesis such as FTLD and ALS.
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DC73168 ERP1.14a
ERP1.14a is a selective, small molecule inhibitor of cell division cell cycle kinase 7 (CDC-7) with IC50 of 125 nM, decreases the enhanced TDP-43 phosphorylation in cells derived from TDP-43-related pathogenesis such as FTLD and ALS.
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DC73167 EF-4-177
EF-4-177 is a potent, selective, allosteric and orally active CDK2 inhibitor with ITC KD of 7.4 nM. EF-4-177 binds CDK2 in a manner that is negatively cooperative with cyclin binding.
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DC73165 Crozbaciclib
Crozbaciclib is a highly potent, selective, blood-brain barrier (BBB) permeable CDK4/6 inhibitor with IC50 values of 3 nM and 1 nM against CDK4/cyclin D1 and CDK6/cyclin D3, respectively.
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DC73164 Cdk5i peptide
Cdk5i peptide is a Cdk5-derived 12-amino acid long Cdk5-derived peptide that interferes with the Cdk5/p25 complex with Kd of 0.17 uM, 40-fold more strongly to either Cdk5 or Cdk2 alone.
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DC73163 CAF-382
CAF-382 (CDKL5 inhibitor B1) is a potent, specific inhibitor of serine-threonine kinase cyclin dependent kinase-like 5 (CDKL5) with IC50 of 11 nM in NanoBRET assays, shows no activity against GSK3β.
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DC73162 BMS-357075
BMS-357075 is a potent pan inhibitor of cyclin-dependent kinases (CDKs) with IC50 of 18, 3 and 26 nM for CDK1, CDK2, and CDK4, respectively, also inhibits CDK20 with Kd of 56 nM.
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DC73161 MW05
MW05 is a specific inhibitor for DNA damage-induced NF-κB activity, inhibits CLK2 and CLK4 with IC50 of 1400 and 307 nM, does not inhibit CLK3.
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DC73158 Leucettinib-92
Leucettinib-92 is a potent DYRK/CLK inhibitor, inhibits CLK1, CLK2, CLK4, DYRK1A and DYRK1B with IC50 of 9.2, 6, 6, 1.2 and 1.8 nM, respectively.
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DC73157 GPS192
GPS192 (GPS 167) is a specific small molecule splicing regulator SRSF10 inhibitor, modulates BCLAF1 splicing with IC50 of 2 uM in human colorectal HCT116 cells, directly inhibits CLK1, CLK2 and CLK4, but not SRPK1 and DYRK1A.
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DC73156 LXY18
LXY18 is a potent orally available blocker of AURKB relocation in mitosis with minimum effective concentration (MEC) of 3.5 nM for inducing polyploidy, shows broad-spectrum growth inhibitory and apoptosis-inducing activities with low nanomolar potencies.
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DC73154 ART0380
ART0380 (ART-0380) is a potent, selective and ATP-competitive ATR kinase inhibitor, inhibits ATR-ATRIP complex enzyme activity with IC50 of 51.7 nM, and phospho-Chk1 IC50 of 22 nM in cell western assay.
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DC73153 TH7299
TH7299 is a potent mitochondrial inhibitor of mitochondrial MTHFD2L with IC50 of 274 nM.
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DC73151 SW118150
SW118150 is a selective small molecule inhibitor of WNK3 kinase with IC50 of 3.0 uM, 5-fold selectivity over WNK1.
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DC73150 MR-2088
MR-2088 is a potent and selective ULK1/2 inhibitor with IC50 of 2.0 nM and MST Kd value of 1.5-4.4 nM (ULK1), efficiently inhibits autophagy.
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DC73149 SK-124
SK-124 (SK124) is a potent, selective, orally active SIK2/SIK3 inhibitor with IC50 of 8.8/11.3 nM in cell-based NanoBRET assays, 15-fold selectivity versus SIK1.
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DC73148 JRD-SIK1/2i-4
JRD-SIK1/2i-4 is a potent, highly selective SIK1/2 inhibitor, modulates innate immune activation and suppress intestinal inflammation.
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