Chk2 inhibitor CCT241533 Small Molecule (Tool Compound)
Cat. #:
151833
Sub-type:
Inhibitor
Availability:
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Application:
CCT241533 blocked CHK2 activity in human tumor cell lines in response to DNA damage, as shown by inhibition of CHK2 autophosphorylation at S516, band shift mobility changes, and HDMX degradation. CCT241533 did not potentiate the cytotoxicity of a selection of genotoxic agents in several cell lines. However, this compound significantly potentiates the cytotoxicity of two structurally distinct PARP inhibitors. Clear induction of the pS516 CHK2 signal was seen with a PARP inhibitor alone, and th…
DNA-PK inhibitor NU7441 Small Molecule (Tool Compound)
Cat. #:
151889
Sub-type:
Inhibitor
Availability:
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Application:
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…
Mps1 inhibitor CCT251455 Small Molecule (Tool Compound)
Cat. #:
152625
Sub-type:
Inhibitor
Availability:
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Application:
CCT251455 displays a favorable oral pharmacokinetic profile, shows dose-dependent inhibition of MPS1 in an HCT116 human tumor xenograft model, and is an attractive tool compound to elucidate further the therapeutic potential of MPS1 inhibition. In Female Balb/C mice it had an oral bioavailabilty of 83%.
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