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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DC73170 |
GFH009
Featured
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GFH009 is a potent, selective CDK9 inhibitor, inhibits the activity of the CDK9/cyclin T1 regulatory complex of P-TEFb. |
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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. |
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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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DC73173 |
MER-128 |
MER-128 is a potent, selective CDK20 inhibitor with IC50 of 2 nM. |
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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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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. |
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DC73176 |
NCT02 |
NCT02 is a small moelcule that induces ubiquitination of cyclin K (CCNK) and proteasomal degradation of CCNK and its complex partner CDK12. |
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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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DC73178 |
SNX631 |
SNX631 (SNX-631) is a potent, selective inhibitor of CDK8/19 Mediator kinase with IC50 of 10.3 nM in the NF κB-dependent cell-based assays. |
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DC73179 |
SW394703 |
SW394703 is a novel DDB1-dependent molecular glue degrader for cyclin K, SW394703 is toxic to HCT116 cells (IC50=1.2 uM). |
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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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DC73181 |
XPW1 |
XPW1 is a potent and selective CDK9 inhibitor with excellent anti-ccRCC activity and low toxicity. |
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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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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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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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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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DC73186 |
CDEAH |
CDEAH is a monofunctional alkylating agent that selectively kills PARP1- and xeroderma pigmentosum A-deficient cells. |
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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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DC73188 |
QBS10072S
Featured
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QBS10072S is a novel dual-function, BBB permeable chemotherapeutic agent with alkylating moiety and a selective large neutral amino acid transporter 1 (LAT1, SLC7A5) substrate, shows excellent BBB penetration and promising efficacy in vitro (U251 cell IC5 |
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DC73189 |
H3B-960
Featured
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H3B-960 is a potent, selective and covalent inhibitor of Werner syndrome protein (WRN) helicase activity with IC50 of 60 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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DC73191 |
HRO761
Featured
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HRO761 is a potent, selective, allosteric WRN inhibitor with IC50 of 100 nM (ATPase assay) and GI50 of 40 nM (SW48 cells), respectively. HRO761 binds at the interface of the D1 and D2 helicase domains, locking WRN in an inactive conformation. |
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DC73192 |
KY386 |
KY386 is a potent, selective inhibitor of RNA helicase DHX33 with IC50 of 19 nM. |
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DC73193 |
SU0448 |
SU0448 is a specific, cell-permeable small molecule activator of the DNA repair enzyme Human MutT Homolog 1 (MTH1) with AC50 value of 5.5 uM, inhibits cell viability of HCC1806 cells with IC50 of 36.1 uM. |
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