Free shipping on all orders over $ 500

TMP269

Cat. No. M3643
TMP269 Structure
Size Price Availability Quantity
10mM*1mL in DMSO USD 120  USD120 In stock
2mg USD 65  USD65 In stock
5mg USD 110  USD110 In stock
10mg USD 175  USD175 In stock
25mg USD 330  USD330 In stock
50mg USD 530  USD530 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
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.In addition, TMP269 significantly promotes reprogramming.

Customer Product Validations & Biological Datas
Source Breast Cancer Res Treat (2014). Figure 1. TMP269
Method qPCR
Cell Lines MDAMB-231 cells
Concentrations 100 nM
Incubation Time 24 h
Results Quantitation of the CV assay dose response (10nM–10μM) in MDA-MB-231 cells demonstrated a similar effect on cell proliferation by LBH589 as previously observed, while SAHA and TMP269 were much less effective
Protocol (for reference only)
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
Chemical Information
Molecular Weight 514.52
Formula C25H21F3N4O3S
CAS Number 1314890-29-3
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Sinnett-Smith J, et al. Am J Physiol Cell Physiol. Protein kinase D1 mediates class IIa histone deacetylase phosphorylation and nuclear extrusion in intestinal epithelial cells: role in mitogenic signaling.

[2] Lobera M, et al. Nat Chem Biol. Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group.

Related HDAC Products
Ac-Arg-Gly-Lys(Ac)-AMC

Ac-Arg-Gly-Lys(Ac)-AMC is a substrate for HDAC.

Chlamydocin

Chlamydocin, a fungal metabolite, is a highly potent HDAC inhibitor, with an IC50 of 1.3 nM.

HDAC-IN-30

HDAC-IN-30 is a novel multi-target HDAC inhibitor, including HDAC1 (IC50=13.4 nM),HDAC2 (IC50=28.0 nM), HDAC3 (IC50=9.18 nM), HDAC6 (IC50=42.7 nM), HDAC8 (IC50=131 nM).

Ac-Arg-Gly-Lys(Ac)-AMC acetate

Ac-Arg-Gly-Lys(Ac)-AMC acetate is a substrate for histone deacetylase (HDAC) and can be used in a novel fluorescent assay for HDAC activity.

JPS014 TFA

JPS014 TFA is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC).

  Catalog
Abmole Inhibitor Catalog




Keywords: TMP269 supplier, HDAC, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.