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TMP269 HDAC 4/5/7/9 inhibitor

Catalog No.A8806
Size Price Stock Qty
10mM (in 1mL DMSO)
$180.00
In stock
5mg
$110.00
In stock
10mg
$180.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Quality Control & MSDS

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Chemical structure

TMP269

Biological Activity

Description TMP269 is a potent, selective inhibitor of class IIa HDAC with IC50 values of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.
Targets HDAC9 HDAC7 HDAC5 HDAC4    
IC50 23 nM 43 nM 97 nM 157 nM    

Protocol

Cell experiment [1]:

Cell lines

IEC-18 cells

Preparation method

The solubility of this compound in DMSO is >23mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

4 μM, 18 h, 37°C

Applications

In IEC-18 intestinal epithelial cells, TMP269 potently inhibited [3H]thymidine incorporation induced by ANG II with the EC50 of ~1.5 μM. TMP269 completely prevented the striking shift from the G0/G1 to the G2/M phase stimulation by ANG II.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Sinnett-Smith J, Ni Y, Wang J, et al. Protein kinase D1 mediates class IIa histone deacetylase phosphorylation and nuclear extrusion in intestinal epithelial cells: role in mitogenic signaling[J]. American Journal of Physiology-Cell Physiology, 2014, 306(10): C961-C971.

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Chemical Properties

Cas No. 1314890-29-3 SDF Download SDF
Synonyms TMP 269;TMP-269
Chemical Name (Z)-N-((4-(4-phenylthiazol-2-yl)tetrahydro-2H-pyran-4-yl)methyl)-3-(5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl)benzimidic acid
Canonical SMILES FC(F)(F)C1=NC(C2=CC(/C(O)=N/CC3(C4=NC(C5=CC=CC=C5)=CS4)CCOCC3)=CC=C2)=NO1
Formula C25H21F3N4O3S M.Wt 514.52
Solubility >23mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

TMP269 is a novel and selective inhibitor of class IIa histone deacetylase with IC50 values of 126, 80, 36, 9 nM for HDAC 4, 5, 7, 9, respectively [1].

Histone deacetylases (HADC) are a series of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone and make the histones to wrap the DNA more tightly, which prevent transcription.

TMP269 is a novel and selective class IIa HDAC inhibitor. In MM cell lines, TMP269 induced modest cytotoxicity with IC50 values ranging from 22 to 38 μM in a dose-dependent way, which was associated with cleavage of caspase-3, -8, -9 and PARP. Also, TMP269 enhanced CFZ-induced apoptosis and increased the expression of activating transcription factor 4 (ATF4) and proapoptotic transcription factor C/EBP homologous protein (CHOP). In the presence of BMSCs or IL-6, TMP269 and CFZ also showed significant cytotoxicity [2]. In IEC-18 intestinal epithelial cells, TMP269 inhibited cell proliferation, cell cycle progression and DNA synthesis in response to G protein-coupled receptor/protein kinase D1 (PKD1) activation [3].

References:
[1].  Lobera M, Madauss KP, Pohlhaus DT, et al. Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group. Nat Chem Biol, 2013, 9(5): 319-325.
[2].  Kikuchi S, Suzuki R, Ohguchi H, et al. Class IIa HDAC inhibition enhances ER stress-mediated cell death in multiple myeloma. Leukemia, 2015.
[3].  Sinnett-Smith J, Ni Y, Wang J, et al. Protein kinase D1 mediates class IIa histone deacetylase phosphorylation and nuclear extrusion in intestinal epithelial cells: role in mitogenic signaling. Am J Physiol Cell Physiol, 2014, 306(10): C961-71.