Antitumoral Quinol2 Small Molecule (Tool Compound)
Cat. #:
151840
Sub-type:
Inhibitor
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Displays in vivo antitumor activity against human RXF 944XL renal xenografts in nude NMRI mice. Inhibits thioredoxin reductase with potencies correlated with their antiproliferative and cytotoxic efficacies. Potent activity against renal, colon, and breast cancer cell lines in the NCI 60-cell panel. Shows potent antitumor activity in HCT 116 and HT 29 human colon as well as MCF 7 and MDA 468 human breast cancer cell lines.
DNA-PK inhibitor NU7441 Small Molecule (Tool Compound)
Cat. #:
151889
Sub-type:
Inhibitor
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NU7441 intraperitoneally administrated at dose of 10 mg/kg maintains for at least 4 hours shows nontoxic and increases etoposide-induced tumor growth delay 2-fold in mice bearing SW620 xenografts. NU7441 increases the persistence of ÎłH2AX foci after ionizing radiationâinduced or etoposide-induced DNA damage. NU7441 (0.5 ÎźM or 1 ÎźM) appreciably increases G2-M accumulation induced by ionizing radiation, etoposide, and doxorubicin in both SW620 and LoVo cells. NU7441 causes persistence of d…
Dual DNA-PK/PI3K inhibitor KU-0060648 Small Molecule (Tool Compound)
Cat. #:
152709
Sub-type:
Inhibitor
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Application:
KU-0060648 enhances the anti-tumour activity of etoposide in both MCF7 and SW620 xenograft models, and has single-agent activity in the MCF7 xenograft model. KU-0060648 exhibits differential effects on growth inhibition, but is not profoundly cytotoxic in a panel of human cancer cell lines. It inhibits DNA-PK and PI-3K with greater potency in MCF7 than SW620 cell using cell-based assays. Five-day exposure to 1 mM KU-0060648 inhibits cell proliferation by more than 95% in MCF7 cells but only b…
CDK2 inhibitor NU6301 Small Molecule (Tool Compound)
Cat. #:
152754
Sub-type:
Inhibitor
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The prodrug NU6301 rapidly generated NU6102 in vitro in mouse plasma, and tumour NU6102 levels in vivo consistent with activity in vitro. Eight or 12 hourly dosing of 120 mg/kg NU6301 for 10 days was well tolerated in SKUT-1B tumour-bearing mice and inhibited Rb phosphorylation in tumour tissue. Two (8 hourly dosing) and 3 (12 hourly dosing) day tumour growth delay was observed (p=0.04 and p=0.007, respectively) following NU6301 administration. NU6102 selectively inhibited the growth of CDK2 WT (wild type) versus KO MEFs (knockout mouse embryo fibroblasts) (GIâ â (concentration required to inhibit cell growth by 50%) 14 ÎźM versus >30 ÎźM), and was more growth-inhibitory in p53 mutant or null versus p53 WT cells (p=0.02), and in Rb (retinoblastoma protein) WT SKUT-1B versus SKUT 1 Rb deficient cells (p=0.01). In SKUT-1B cells NU6102 induced a G2 arrest, inhibition of Rb phosphorylation and cytotoxicity (LCâ â 2.6 ÎźM for a 24h exposure).
HDAC3:SMRT Fluorescent Probe 2-FAM-InsP5 Small Molecule (Tool Compound)
Cat. #:
153334
Sub-type:
Fluorescent Probe
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Application:
2-FAM-InsP5 [2-FAM-Ins(1,3,4,5,6)P5] is a fluorescent derivative of Ins(1,3,4,5,6)P5. 2-FAM-InsP5 activates the HDAC3:SMRT complex in a similar manner to the natural ligand, Ins(1,4,5,6)P4. The binding constant (Kd) for binding of 2-FAM-InsP5 to HDAC3:SMRT measured by a direct binding assay, 0.3 Âą 0.01 ÎźM, was approximately 10-fold lower than the Kdapp for activation of the catalytic activity of HDAC3:SMRT by Ins(…
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