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Home > Inhibitors & Agonists > Cell Cycle/DNA Damage > PARP

G007-LK

  Cat. No.:  DC8222   Featured
Chemical Structure
1380672-07-0
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More than 5000 active chemicals with high quality for research!
Field of application
G007-LK is a potent, "rule of 5" compliant and a metabolically stable TNKS1/2 inhibitor.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1380672-07-0
Chemical Name: 4-[5-[(E)-2-[4-(2-Chlorophenyl)-5-(5-methylsulfonylpyridin-2-yl)-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]benzonitrile
Synonyms: G007LK;(E)-4-(5-(2-(4-(2-chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)vinyl)-1,3,4-oxadiazol-2-yl)benzonitrile;G007-LK;4-{5-[(E)-2-{4-(2-Chlorophenyl)-5-[5-(Methylsulfonyl)pyridin-2-Yl]-4h-1,2,4-Triazol-3-Yl}ethenyl]-1,3,4-Oxadiazol-2-Yl}benzonitrile;benzonitrile, 4-[5-[(1E)-2-[4-(2-chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]-;4hyf;HIWVLHPKZNBSBE-OUKQBFOZSA-N;C25H16ClN7O3S;4-[5-[(E)-2-[4-(2-Chlorophenyl)-5-(5-methylsulfonylpyridin-2-yl)-1,2,4-triazol-3-yl]ethenyl]-1,3,4-o
SMILES: ClC1=C([H])C([H])=C([H])C([H])=C1N1C(/C(/[H])=C(\[H])/C2=NN=C(C3C([H])=C([H])C(C#N)=C([H])C=3[H])O2)=NN=C1C1C([H])=C([H])C(=C([H])N=1)S(C([H])([H])[H])(=O)=O
Formula: C25H16ClN7O3S
M.Wt: 529.9576
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: G007-LK is a potent and selective inhibitor of TNKS1 and TNKS2, with IC50s of 46 nM and 25 nM, respectively.
In Vivo: G007-LK displays great pharmacokinetic profile in ICR mice[1]. G007-LK (100 mg/kg chow, p.o.) significantly reduces lineage tracing from LGR5+ intestinal stem cells in mice. G007-LK (100 mg/kg chow, p.o.) specifically targets LGR5+ WNT-dependent intestinal stem cells in Lgr5-EGFP-CreERT2;R26R-tdTomato mice. G007-LK (10, 50 mg/kg, p.o.) also suppressses canonical WNT signalling. Furthermore, G007-LK (100, 1000 mg/kg chow, p.o) shows no effect on the alteration of duodenal morphology[2].
In Vitro: G007-LK is a potent inhibitor of TNKS1 and TNKS2, with IC50s of 46 nM and 25 nM, respectively, and a cellular IC50 of 50 nM. G007-LK shows no inhibition of PARP1 at doses up to 20 μM, and has a high CYP3A4 inhibition IC50 value (>25 μM)[1]. G007-LK (0-20 μM) dose-dependently inhibits hepatocellular carcinoma (HCC) cell growth. G007-LK also downregulates the levels of YAP by upregulating AMOTL1 and AMOTL2 in HCC cell lines. In addition, G007-LK (0-20 μM) synergizes with MEK and AKT inhibitors to suppress HCC cell proliferation[3].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC5151 Rucaparib phosphate (AG-14699, PF-01367338) Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM with binding affinity to nine PARP domains. Phase 1/2.
DC7237 PJ34 HCl PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.
DC4110 AZD-2281 (Olaparib) Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1 and PARP2 with IC50 of 5 nM and 1 nM, respectively.
DC8463 NVP-TNKS656 NVP-TNKS656(TNKS-656) is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM; > 300 fold selectivity against PARP1 and PARP2.
DC7935 NU1025 NU 1025 is an inhibitor of poly(ADP-ribose) polymerases (PARP) (IC50 = 400 nM).
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