Small molecules
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AKR1C3 inhibitor CRT0036521 Small Molecule (Tool Compound)
AKR1C3 inhibitor CRT0036521 Small Molecule (Tool Compound)Cat. #151843
Sub-type: Inhibitor
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.
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DNA-PK inhibitor NU7441 Small Molecule (Tool Compound)
DNA-PK inhibitor NU7441 Small Molecule (Tool Compound)Cat. #151889
Sub-type: Inhibitor
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...
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HDAC2/3 inhibitor MI-192 Small Molecule (Tool Compound)
HDAC2/3 inhibitor MI-192 Small Molecule (Tool Compound)Cat. #152433
Sub-type: Inhibitor
Application: Promotes apoptosis of leukemia cell lines in vitro. Also attenuates IL-6 production in rheumatoid arthritis PBMCs in vitro. MI-192 (CRT0163458) shows potent activity in a number of cell lines tested using the NCI-60 cell panel. MI-192 was tested using the following NCI-60 cell lines: Leukemia cell lines: CCRF-CEM, HL-60 (TB), K-562, MOLT-4 and RPMI-8226. Colon Cancer cell lines: COLO205, HCC-2998, HCT-116, HCT-15, HT29, KM12 and SW-620. CNS Cancer cell lines: SF-268, SF-295, SF-539, SNB-19, ...
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Protein Kinase D inhibitor CRT5 (CRT0066051) Small Molecule (Tool Compound)
Protein Kinase D inhibitor CRT5 (CRT0066051) Small Molecule (Tool Compound)Cat. #152544
Sub-type: Inhibitor
Application: PLEASE NOTE THAT THIS COMPOUND IS TOXIC IN VIVO. CRT5 blocks phosphorylation of PKD1 on Ser916 and PKD2 on Ser876, but does not affect PKC-dependent PKD phosphorylation or PKD autophosphorylation.1 It also decreases VEGF-induced endothelial migration, proliferation, and tubulogenesis.
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Mps1 inhibitor CCT251455 Small Molecule (Tool Compound)
Mps1 inhibitor CCT251455 Small Molecule (Tool Compound)Cat. #152625
Sub-type: Inhibitor
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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Dual DNA-PK/PI3K inhibitor KU-0060648 Small Molecule (Tool Compound)
Dual DNA-PK/PI3K inhibitor KU-0060648 Small Molecule (Tool Compound)Cat. #152709
Sub-type: Inhibitor
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...
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CDK2 inhibitor NU6301 Small Molecule (Tool Compound)
CDK2 inhibitor NU6301 Small Molecule (Tool Compound)Cat. #152754
Sub-type: Inhibitor
Application: 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).
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Mitochondrial Luminophore Small Molecule (Tool Compound)
Mitochondrial Luminophore Small Molecule (Tool Compound)Cat. #152785
Sub-type: Luminophore
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Nucleolar Luminophore Ag-1 Small Molecule (Tool Compound)
Nucleolar Luminophore Ag-1 Small Molecule (Tool Compound)Cat. #152786
Sub-type: Luminophore
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CDK inhibitor BS-194 Small Molecule (Tool Compound)
CDK inhibitor BS-194 Small Molecule (Tool Compound)Cat. #153191
Sub-type: Inhibitor
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HDAC3:SMRT Fluorescent Probe 2-FAM-InsP5 Small Molecule (Tool Compound)
HDAC3:SMRT Fluorescent Probe 2-FAM-InsP5 Small Molecule (Tool Compound)Cat. #153334
Sub-type: Fluorescent Probe
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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PI4K beta Inhibitor Small Molecule (Tool Compound)
PI4K beta Inhibitor Small Molecule (Tool Compound)Cat. #153578
Sub-type: Inhibitor
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PI4K alpha Inhibitor Small Molecule (Tool Compound)
PI4K alpha Inhibitor Small Molecule (Tool Compound)Cat. #153579
Sub-type: Inhibitor
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MSTI Fluorescence High-Throughput Drug Assay
MSTI Fluorescence High-Throughput Drug AssayCat. #153815
Sub-type: Fluorescent Probe
