TMP269

SKU: orb1307312

Description

TMP269 is a potent and selective class IIa HDAC inhibitor, demonstrating IC50 values of 157 nM, 97 nM, 43 nM, and 23 nM for HDAC4, HDAC5, HDAC7, and HDAC9, respectively. This small molecule is a valuable research tool for investigating epigenetic mechanisms in cancer, neurodegenerative diseases, and metabolic disorders in both cellular and animal models.

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 1314890-29-3
• MW: 514.52
• Purity: 98.00% (May vary between batches)
• Formula: C₂₅H₂₁F₃N₄O₃S
• SMILES: FC(F)(F)c1nc(no1)-c1cccc(c1)C(=O)NCC1(CCOCC1)c1nc(cs1)-c1ccccc1
• Target: HDAC
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.41 mM);Ethanol:2 mg/mL (3.89 mM);DMSO:225 mg/mL (437.3 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  HDAC6:82000 nM|HDAC8:42000 nM|HDAC5:97 nM|HDAC7:43 nM|HDAC9:23 nM|HDAC4:157 nM
• In Vivo:
  TMP269 (10 μM) does not affect mitochondrial activity and/or the activity of human CD4+ T cells and can be used to identify endogenous substrates of class IIa HDAC enzymes. In IEC-18 small intestinal epithelial cells, TMP269 inhibits cellular processes, DNA synthesis, and proliferation induced by the activation of G protein-coupled receptor/PKD1 signaling.
• Cell Research:
  Human CD4+ T cells are isolated 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 plated 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.(Only for Reference)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HDAC, HDAC7, HDAC9, HDAC5, HDAC4, Histone deacetylases, Inhibitor, inhibit, TMP-269, TMP269, TMP 269

Compound Identifiers

PubChem CID

53344908