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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
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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DC73147 GLPG3312
GLPG3312 is a potent and selective pan-SIK inhibitor with IC50 of 2.0/0.7/0.6 nM for SIK1/SIK2/SIK3, respectively.
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DC73144 EB-42168
EB-42168 is a potent, selective G2019S-LRRK2 kinase inhibitor with IC50 of 1.1 nM (pS935-LRRK2) in FRET-based assay, >100-fold selective over WT-LRRR2.
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DC73142 DC-ATG4in
DC-ATG4in is a small molecule autophagy related 4B (ATG4B) inhibitor, directly binds to ATG4B and inhibits its enzyme activity with IC50 of 3.08 uM, DC-ATG4in is an autophagy inhibitor.
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DC73141 YTK-2205
YTK-2205 (YTK2205) is a small molecule p62 agonist targeting ZZ domain, induces selective autophagy activation, YTK-2205 augments the translocation of p62 to mitochondria, targeting their lysosomal degradation.
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DC73140 RH1115
RH1115 is a small molecule activator and inducer of autophagy targeting Lamin A/C and LAMP1, induces changes to LAMP1 vesicle properties and alters lysosome positioning.
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DC73139 JS-017
JS-017 (JS017) is a small molecule degrader of N-retinylidene-N-retinylethanolamine (A2E), one of the components of lipofuscin, degrades A2E-BDP from ARPE-19 cells with IC50 of 3.239 uM.
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DC73138 Zharp2-1
Zharp2-1 is a novel potent, selective RIPK2 inhibitor with IC50 of 38.5 nM in ADP-Glo kinase assay, effectively blocks RIPK2 kinase function and NOD-mediated NF-κB/MAPK activation.
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DC73137 Zharp1-211
Zharp1-211 is a potent, selective, type II inhibitor of RIPK1 kinase with IC50 of 53 nM and binding Kd of 8.7 nM.
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DC73136 Oditrasertib
Oditrasertib is a potent, selective RIPK1 inhibitor.
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DC73135 GSK2593074A
GSK2593074A (GSK'074, GSK-2593074A) is novel potent, selective RIP1/RIP3 kinase dual inhibitor, directly binds to RIP1 and RIP3 with Kd of 130 and 12 nM, respectively.
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DC73133 Flizasertib
Flizasertib is a potent, selective RIP1 kinase (RIPK1) inhibitor with potential for treating prophylaxis.
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DC73132 cRIPGBM chloride
cRIPGBM (RIPGBM derivative cRIPGBM, RIPGBM-18) is a metabolite of RIPGBM induces apoptosis in GBM CSCs (EC50=68 nM in GBM 1 cells) by interacting with RIPK2 (Kd=2.3 uM).
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DC73131 aYM155
aYM155 is a brain-penetrating prodrug form of YM155 (Cat. PC-42439, potent survivin inhibitor), displays potent cell killing activity against a broad panel of patient-derived GBM cancer stem-like cells (IC50=0.7-10 nM).
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DC73129 UCI-LC0023
UCI-LC0023 is a small molecule that restores mutant p53 activity by targeting the cryptic L1/S3 pocket of p53, directly binds to mutant p53 and restores wild-type-like conformation of mutant p53R175H.
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DC73128 UCI-LC0019
UCI-LC0019 is a specific small molecule that restores mutant p53 activity by targeting the cryptic L1/S3 pocket of p53, directly binds to mutant p53 and restores wild-type-like conformation of mutant p53R175H.
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DC73127 UC2288
UC2288 is a small molecule p21 inhibitor, attenuates p21 protein abundance at 10 µM, independently of p53 activity and at the level of transcription or post-transcription.
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