T0070907

Names

[ Name ]:
T0070907

[Synonym ]:
2-Chloro-5-nitro-N-4-pyridinyl-benzamide Benzamide,2-chloro-5-nitro-N-4-pyridinyl
Benzamide,2-chloro-5-nitro-N-4-pyridinyl
2-chloro-5-nitro-N-pyridin-4-yl-benzamide
Benzamide, 2-chloro-5-nitro-N-4-pyridinyl-
2-Chloro-5-nitro-N-(4-pyridinyl)benzamide
2-Chloro-5-nitro-N-4-pyridinylbenzamide
2-chloro-5-nitro-N-(pyridin-4-yl)benzamide
T0070907

Biological Activity

[Description]:

T0070907 is a potent PPARγ antagonist with a Ki of 1 nM.

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> PPAR

Signaling Pathways >> Cell Cycle/DNA Damage >> RAD51

Research Areas >> Cancer

[Target]

PPARγ:1 nM (Ki)

PPARδ:1.8 μM (Ki)

PPARα:0.85 μM (Ki)

[In Vitro]

T0070907 (50 μM) pre-treatment impairs repair of IR-induced DNA DSBs in both ME-180 and SiHa cells treated with irradiated (4 Gy). T0070907 (0-50 μM) significantly decreases the levels of DNA-PKcs and RAD51 proteins in ME-180 and SiHa cells[1]. T0070907 (50 μM) treatment reduces the levels of α- and β-tubulin protein in a time-dependent manner, decreases the synthesis of DNA, and prevents the radiation-induced alterations in the cell cycle regulatory proteins of ME180 and SiHa cells[2]. T0070907 (10 µM) has cytotoxicity in an adipocyte-specific and PPARγ-independent manner. T0070907 increases oxidative stress in immature adipocytes[3]. T0070907 (1 μM) blocks the induction of adipogenesis by various treatments of the adipogenic cell line 3T3-L1. T0070907 covalently modifies PPAR on cysteine 313 in helix 3 of human PPAR 2[4].

[Kinase Assay]

To determine the binding affinity of T0070907 to the PPARs, scintillation proximity assay (SPA) is performed with the following modifications. A 90 μL reaction contains SPA buffer (10 mM K2HPO4, 10 mM KH2PO4, 2 mM EDTA, 50 mM NaCl, 1 mM dithiothreitol, 2 mM CHAPS, 10% (v/v) glycerol, pH 7.1), 50 ng of GST-PPAR (or 150 ng of GST-PPAR), 5 nM 3H-labeled radioligands, and 5 μL of T0070907 in Me2SO. After incubation for 1 h at room temperature, 10 μL of polylysine-coated SPA beads (at 20 mg/mL in SPA buffer) are added, and the mixture is incubated for 1 h before reading in Packard Topcount. [3H]Rosiglitazone is used for PPAR, and [3H]GW2433 is used for PPAR and PPAR.

[References]

[1]. An Z, et al. T0070907 inhibits repair of radiation-induced DNA damage by targeting RAD51. Toxicol In Vitro. 2016 Dec;37:1-8

[2]. An Z, et al. T0070907, a PPAR γ inhibitor, induced G2/M arrest enhances the effect of radiation in human cervical cancer cells through mitotic catastrophe. Reprod Sci. 2014 Nov;21(11):1352-61.

[3]. Kawahara A, et al. Peroxisome proliferator-activated receptor γ (PPARγ)-independent specific cytotoxicity against immature adipocytes induced by PPARγ antagonist T0070907. Biol Pharm Bull. 2013;36(9):1428-34

[4]. Lee G, et al. T0070907, a selective ligand for peroxisome proliferator-activated receptor gamma, functions as an antagonist of biochemical and cellular activities. J Biol Chem. 2002 May 31;277(22):19649-57. Epub 2002 Mar 4

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
381.7±37.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₂H₈ClN₃O₃

[ Molecular Weight ]:
277.663

[ Flash Point ]:
184.6±26.5 °C

[ Exact Mass ]:
277.025421

[ PSA ]:
87.81000

[ LogP ]:
2.25

[ Appearance of Characters ]:
white

[ Vapour Pressure ]:
0.0±0.9 mmHg at 25°C

[ Index of Refraction ]:
1.684

[ Storage condition ]:
Store at RT

[ Water Solubility ]:
DMSO: >10mg/mL | Soluble in DMSO at 10mg/ml. Insoluble in water.

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H319

[ Precautionary Statements ]:
P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xn

[ Risk Phrases ]:
22-36

[ Safety Phrases ]:
26

[ RIDADR ]:
NONH for all modes of transport

[ HS Code ]:
2933399090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2933399090

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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Related Compounds

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