Antitumoral Quinol1h Small Molecule (Tool Compound)
Cat. #:
151834
Sub-type:
Antitumoral
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Application:
Antitumor activity observed in HCT 116 (GI50 = 40 nM) and HT 29 (GI50 = 380 nM), and in breast cancer cell lines. Potent inhibitory effect in NCI 60 cells (GI50 =16 nM and LC50 = 2.24 ÂľM).
HDAC2/3 inhibitor MI-192 Small Molecule (Tool Compound)
Cat. #:
152433
Sub-type:
Inhibitor
Availability:
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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, …
Protein Kinase D inhibitor CRT5 (CRT0066051) Small Molecule (Tool Compound)
Cat. #:
152544
Sub-type:
Inhibitor
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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.
Dual DNA-PK/PI3K inhibitor KU-0060648 Small Molecule (Tool Compound)
Cat. #:
152709
Sub-type:
Inhibitor
Availability:
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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…
HDAC3:SMRT Fluorescent Probe 2-FAM-InsP5 Small Molecule (Tool Compound)
Cat. #:
153334
Sub-type:
Fluorescent Probe
Availability:
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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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