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TMP269

Cat. No. M3643

TMP269 Structure
Size Price Availability Quantity
2mg USD 75 In stock
5mg USD 100 In stock
10mg USD 180 In stock
25mg USD 390 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

TMP269 is a novel and selective class IIa histone deacetylase inhibitor with IC50s of 126/80/36/9 nM for HDAC 4/5/7/9, respectively; 20-400 fold selectivity over class1 HDACs. TMP269 showes no effect at the acetylation level of histone H3-K9, no signifcant effects (2-fold) in gene expression on T-cells and no cytotoxicity in T cell expansion assay. TMP269 prevents cell cycle progression, DNA synthesis, and proliferation induced in response to G protein-coupled receptor/PKD1 activation.

Protocol
Cell Experiment
Cell lines Human CD4+ T cells
Preparation method Isolating human CD4+ T cells from whole blood via negative selection according to manufacturer's instructions (RosetteSep Human CD4+ T cell enrichment kit), re-suspended in T-cell culture medium (10% FBS, 2 mM L-glutamine, 1 mM pyruvate, 10 mM HEPES, 10 U/10 mg penicillin/streptomycin, 0.5% DMSO in RPMI) and plating at 50,000 cells/well with IL-2 (10 BRMP units/mL) and 100,000 human T-expander Dynabeads for 72 h. Determination of mitochondrial function or cell viability is done according to manufacturer’s instructions (Cell Proliferation Assay Kit I (MTT)) and is represented as a percent of control (no inhibitor) wells.
Concentrations 10 μM
Incubation time 72 hours
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 514.52
Formula C25H21F3N4O3S
CAS Number 1314890-29-3
Purity >99%
Solubility DMSO
Storage at -20°C
References

Protein kinase D1 mediates class IIa histone deacetylase phosphorylation and nuclear extrusion in intestinal epithelial cells: role in mitogenic signaling.
Sinnett-Smith J, et al. Am J Physiol Cell Physiol. 2014 May 15;306(10):C961-71. PMID: 24647541.

Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group.
Lobera M, et al. Nat Chem Biol. 2013 May;9(5):319-25. PMID: 23524983.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: TMP269 supplier, HDAC, inhibitors

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