| DC73191 |
HRO761
|
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. |
| DC73189 |
H3B-960
|
H3B-960 is a potent, selective and covalent inhibitor of Werner syndrome protein (WRN) helicase activity with IC50 of 60 nM. |
| 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. |
| DC73192 |
KY386
|
KY386 is a potent, selective inhibitor of RNA helicase DHX33 with IC50 of 19 nM. |
| 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. |
| DC70259 |
BLM inhibitor 2
|
BLM inhibitor 2 is a specific inhibitor of BLM (Bloom syndrome protein) ATPase-coupled DNA helicase activity (IC50=2.2 uM) via the allosteric binding site.BLM inhibitor 2 displays high selectivity over members of the RecQ-helicase family in ATP-turnover assays, including recombinant helicase domains (HD) from human WRN, human RecQ5 or E. coli helicase UvrD, and human RecQ1.BLM inhibitor 2 is a non-competitive inhibitor, does not interfere with ATP-binding, unliker ML216.BLM inhibitor 2 inhibits production of the single-stranded DNA product in a dose-dependent manner (IC50=1.8 uM) via inhibition of the helicase activity of BLM-HD.BLM (Bloom syndrome protein) is a RECQ-family helicase involved in the dissolution of complex DNA structures and repair intermediates (BLM, WRN, RECQ1, RECQ4, and RECQ5 in humans). |
| DC70198 |
And1 inhibitor CH3
|
And1 inhibitor CH3 is potent acidic nucleoplasmic DNA-binding protein 1 (And-1) inhibitor, reducess And‐1 expression level in IGROV1 cells with IC50 of 2.08 uM.CH3 induces acidic nucleoplasmic DNA‐binding protein 1 (And‐1) degradation via the E3 ubiquitin ligase CUL4B‐mediated proteasome degradation pathway.CH3 promotes the interaction between And‐1 and CUL4B by altering And‐1 conformation.CH3 exhibits the significant inhibition in a broad range of cancer cells in vitro and in vivo.CH3 (20 mg/kg and 40 mg/kg) reduced tumor growth of ovarian IGROV1 and breast MCF7 xenografts at both treated doses.CH3 also could overcome cisplatin resistance in ovarian cancer.And1 is an important factor for deoxyribonucleic acid (DNA) replication and repair, is overexpressed in many types of cancer but not in normal tissues. |
| DC70162 |
A83B4C63
|
A83B4C63 is a potent small molecule DNA repair protein, polynucleotide kinase 3'-phosphatase (PNKP) inhibitor with Kd of 80 nM.A83B4C63 is a nano-encapsulated potent, but poorly water-soluble lead PNKP inhibitor with therapeutic potential for PTEN-deficient CRC.Nano-carriers of A83B4C63 effectively inhibited the growth of HCT116/PTEN-/- xenografts in NIH-III nude mice following intravenous (IV) administration, but not that of wild-type HCT116/PTEN+/+ xenografts.A83B4C63 encapsulated in NPs (NP/A83) based on mPEO-b-PBCL or solubilized with CE/A83, sensitized colorectal cancer cells to DNA damaging therapeutics in human HCT116 colorectal cancer (CRC) models. |
