LIMK inhibitor CRT0105950 Small Molecule (Tool Compound)
Cat. #:
151832
Sub-type:
Inhibitor
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Application:
The compounds exhibit low uM potency in breast cancer cells showing dose dependent inhibition of phosphorylation of the LIMK substrate cofilin. Treatment of MDA-MB-231 breast cancer cells with the compounds significantly reduces their ability to invade a matrigel plug in an inverse in vitro invasion assay. Furthermore, the inhibitors effectively reduce fibroblast-led collective invasion in a co-culture organotypic model.
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…
AKR1C3 inhibitor CRT0036521 Small Molecule (Tool Compound)
Cat. #:
151843
Sub-type:
Inhibitor
Availability:
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Application:
The compounds showed good cellular potency, as measured by inhibition of AKR1C3 metabolism of a known dinitrobenzamide substrate, with a broad rank order between enzymic and cellular activity, but amide analogues were more effective than predicted by the cellular assay. displays potency in a cellular assay, blocking the ability of AKR1C3 to metabolize a proven substrate.
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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