DC73145 |
FX2149
Featured
|
FX2149 (FX 2149) is a potent, BBB permeable inhibitor of LRRK2 GTP binding activity with IC90 of 10 nM, reduces PD-linked mutant LRRK2 variants (G2019S and R1441C) that bound with GTP. |
|
DC73146 |
MK-1468
Featured
|
MK-1468 is a potent, selective, brain-penetrant LRRK2 inhibitor with IC50 of 0.4 nM (G2019S LRRK2), potently inhibits the phosphorylation of LRRK2 serine 935 (pSer935) in hPBMCs with IC50 of 2.8 nM. |
|
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. |
|
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. |
|
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. |
|
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. |
|
DC73151 |
SW118150 |
SW118150 is a selective small molecule inhibitor of WNK3 kinase with IC50 of 3.0 uM, 5-fold selectivity over WNK1. |
|
DC73152 |
SW118150
Featured
|
SW120619 is a specific small molecule inhibitor of WNK3 kinase with IC50 of 0.7 uM, weakly inhibits WNK1 and WNK2 with IC50 of 2.3 and 16.8 uM, respectively. |
|
DC73153 |
TH7299 |
TH7299 is a potent mitochondrial inhibitor of mitochondrial MTHFD2L with IC50 of 274 nM. |
|
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. |
|
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. |
|
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. |
|
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. |
|
DC73159 |
ML315
Featured
|
ML315 is a small molecule inhibitor of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases with IC50 of 68, 231, >10,000, 68, 282 and 1156 nM for CLK1/2/3/4 and DYRK1/2, respectively. |
|
DC73160 |
MW01
Featured
|
MW01 is a specific inhibitor for DNA damage-induced NF-κB activity, inhibits CLK2 and CLK4 with IC50 of 360 and 14.1 nM, does not inhibit CLK3. |
|
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. |
|
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. |
|
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. |
|
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. |
|
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. |
|
DC73166 |
Cyclin K degrader DS17 |
Cyclin K degrader DS17 is a selective cyclin K molecular glue degrader with TR-FRET EC50 of 19 nM. |
|
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. |
|
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. |
|
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. |
|
DC73170 |
GFH009
Featured
|
GFH009 is a potent, selective CDK9 inhibitor, inhibits the activity of the CDK9/cyclin T1 regulatory complex of P-TEFb. |
|
DC73171 |
ISM042-2-048 |
ISM042-2-048 is a potent, selective inhibitor of cyclin-dependent kinase 20 (CDK20, cell cycle-related kinase/CCRK) with IC50 of 33.4 nM (CDK20/CycT1), Kd value of 566 nM. |
|
DC73172 |
LGR6768 |
LGR6768 is a potent, selective CDK7 inhibitor with IC50 of 20 nM, >12-fold selectivity over other CDKs. |
|
DC73173 |
MER-128 |
MER-128 is a potent, selective CDK20 inhibitor with IC50 of 2 nM. |
|
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. |
|
DC73175 |
NCGC00131308 |
NCGC00131308 is a small molecule inhibitor that effectively disrupts IQGAP1-Cdc42 interaction in breast cancer cells, shows EC50 of 4.47 uM in biochemical HTRF assays. |
|