| DC72590 |
RBN-3143 |
RBN-3143 is a potent and NAD+-competitive catalytic PARP14 inhibitor with an IC50 value of 4 nM. RBN-3143 inhibits PARP14-mediated ADP-ribosylation and stabilizes PARP14 in cell lines. RBN-3143 can be used in research of lung inflammation. |
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| DC72591 |
OUL232
Featured
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OUL232 is a potent inhibitor of mono-ARTs PARP7, PARP10, PARP11, PARP12, PARP14, and PARP15. OUL232 is the most potent PARP10 inhibitor described to date (IC50=7.8 nM), as well as the first PARP12 inhibitor ever reported. |
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| DC72592 |
Zelasudil
Featured
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Zelasudil is a Rho-associated coiled-coil kinase (ROCK) inhibitor with a specific binding affinity for ROCK2, a key enzyme in the Rho/ROCK signaling pathway. This pathway plays a critical role in regulating cellular processes such as cytoskeletal organization, cell motility, smooth muscle contraction, and gene expression. By selectively inhibiting ROCK2, Zelasudil modulates these processes, offering therapeutic potential for a variety of diseases characterized by fibrosis, inflammation, and vascular dysfunction, including pulmonary fibrosis, glaucoma, and cardiovascular diseases. |
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| DC72593 |
CAY10746 |
CAY10746 is a selective Rho kinase (ROCK) inhibitor. CAY10746 has inhibitory activity for ROCK I, ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively. CAY10746 can be used for the research of diabetic retinopathy (DR). |
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| DC72594 |
PT-262 |
PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity. |
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| DC72595 |
WF-536 |
WF-536 is an orally active inhibitor of Rho-associated coiled-coil-containing protein kinase (ROCK). WF-536 has tumor anti-metastatic activity. WF-536 can be used for the research of cancer. |
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| DC72596 |
MSC-1186 |
MSC-1186 is a highly selective pan-SRPK inhibitor. MSC-1186 has activity for SRPK1, SRPK2 and SRPK3 with IC50 values of 2.7 nM, 81 nM and 0.6 nM, respectively. MSC-1186 can be used for the research of cancer. |
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| DC72597 |
Elomotecan |
Elomotecan (BN 80927 free base) is a potent inhibitor of topoisomerases I and II. Elomotecan is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan reduces the proliferation of different tumor cells with higher potency than other anticancer drugs of reference targeting topoisomerases I and II. |
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| DC72807 |
Tanuxiciclib trihydrochloride |
Tanuxiciclib trihydrochloride is a cyclin dependent kinase (CDK) inhibitor. |
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| DC72842 |
3’-Deoxy-methyl-2-thiouridine |
3’-Deoxy-methyl-2-thiouridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc. |
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| DC72843 |
2’-O-Methyl-N1-methyladenosine |
2’-O-Methyl-N1-methyladenosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc. |
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| DC72845 |
N4-Benzoyl-3’-O-methylcytidine |
N4-Benzoyl-3’-O-methylcytidine is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities. |
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| DC72861 |
Diethyl Pyrocarbonate |
Diethyl pyrocarbonate is a potent, non-specific inhibitor of RNase. It has been useful as an in vitro agent, relatively specific for binding to imidazole of histidine. It inhibits central chemosensitivity in rabbit and can modify Ser, Thr, His and Tyr residues. |
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| DC72889 |
TP-1287 |
TP-1287, a prodrug of Alvocidib, is an orally active CDK9 inhibitor. |
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| DC73153 |
TH7299 |
TH7299 is a potent mitochondrial inhibitor of mitochondrial MTHFD2L with IC50 of 274 nM. |
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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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| 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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| 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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| 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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| DC73159 |
ML315
Featured
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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. |
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| DC73160 |
MW01
Featured
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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. |
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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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| 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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| 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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| 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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| 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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| DC73166 |
Cyclin K degrader DS17 |
Cyclin K degrader DS17 is a selective cyclin K molecular glue degrader with TR-FRET EC50 of 19 nM. |
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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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| 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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| 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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