HDAC2/3 inhibitor MI-192 Small Molecule (Tool Compound)
Cat. #:
152433
Sub-type:
Inhibitor
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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, …
CDK2 inhibitor NU6301 Small Molecule (Tool Compound)
Cat. #:
152754
Sub-type:
Inhibitor
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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).
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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