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BENZOTRIAZOL-1-YL-(2,4-DICHLORO-PHENYL)-METHANONE

BENZOTRIAZOL-1-YL-(2,4-DICHLORO-PHENYL)-METHANONE Structure
BENZOTRIAZOL-1-YL-(2,4-DICHLORO-PHENYL)-METHANONE
  • CAS No.200626-61-5
  • Chemical Name:BENZOTRIAZOL-1-YL-(2,4-DICHLORO-PHENYL)-METHANONE
  • CBNumber:CB4697730
  • Molecular Formula:C13H7Cl2N3O
  • Formula Weight:292.12
  • MOL File:200626-61-5.mol
BENZOTRIAZOL-1-YL-(2,4-DICHLORO-PHENYL)-METHANONE Property
  • Melting point 119-121°C
  • storage temp. Inert atmosphere,2-8°C
  • solubility DMSO: ~28mg/mL
  • form solid
  • color White to Off-White
Safety
  • Hazard Codes  :Xn
  • Risk Statements  :22
  • WGK Germany  :3
  • NFPA 704:
    0
    2 0
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H302
  • Precautionary statements P264-P270-P301+P312-P330-P501

BENZOTRIAZOL-1-YL-(2,4-DICHLORO-PHENYL)-METHANONE Chemical Properties,Usage,Production

  • Uses Histone deacetylase (HDAC) inhibitors?are able to interrupt cell cycle progression in transformed cell lines and may be explored as new clinical agents in cancer therapy. 1-(2,4-Dichlorobenzoyl)-1H-benzotriazole has been shown to suppress the biological effects induced by the HDAC inhibitor, Trichostatin A (T774710).
  • Definition ChEBI: 1-(2,4-dichlorobenzoyl)-1H-1,2,3-benzotriazole is a member of the class of benzamides that is obtained by the formal condensation of 2,4-dichlorobenzoic acid and benzotriazole. It acts as an inhibitor for tubulin acetylation mediated by trichostatin A. It has a role as an inhibitor. It is a member of benzotriazoles, a member of benzamides and a dichlorobenzene. It is functionally related to a 2,4-dichlorobenzoic acid and a benzotriazole.
  • Biological Activity itsa-1 (itsa1) is an hdac activator through trichostatin a (tsa) suppression.trichostatin a (tsa), a streptomyces metabolite, can specifically inhibit mammalian histone deacetylase at a nanomolar concentration causing accumulation of highly acetylated histone molecules in mammalian cells.
  • in vitro previous study reported that in murine embryonic stem cells, tsa treatment for 23 hours inhibited brdu incorporation compared with the control. tsa-pretreated cells incubated with itsa1, however, could incorporate brdu at concentrations where it was inhibited by tsa alone. moreover, itsa1 treatment was able to revert the tsa-arrested population to a normal cell cycle distribution. tsa treatment at 300 nm to a549 cells for 2 hours noticeably increased the levels of acetyl-histone h3, whereas subsequent incubation with itsa1 at 50 μm for 2 hours reduced histone acetylation to the baseline level. in addition, cells pretreated with itsa1 before addition of tsa showed increased acetylation levels, which was a characteristic of tsa treatment alone. these results suggested that the target of itsa1 was not present until induced by tsa. furthermore, the itsa1 treatment alone at 50 or 100 μm was not effective on hdac activity, demonstrating that itsa1 could directly affect hdac function [1].
  • in vivo

    ITSA-1 (0.5 mg/kg; intraperitoneal injection; 3 times/week; for 8 weeks; CBS+/ mice) balances deacetylation activity and suppresses IL-6 and TNF-α expression and thereby attenuated histone acetylationdependent infammatory signaling[2].

    Animal Model:CBS+/? mice[2]
    Dosage:0.5 mg/kg
    Administration:Intraperitoneal injection; 3 times/week; for 8 weeks
    Result:Balanced deacetylation activity and suppressed IL-6 and TNF-α expression.
  • IC 50 HDAC
  • References [1] koeller km, haggarty sj, perkins bd, leykin i, wong jc, kao mc, schreiber sl. chemical genetic modifier screens: small molecule trichostatin suppressors as probes of intracellular histone and tubulin acetylation. chem biol. 2003 may;10(5):397-410.
BENZOTRIAZOL-1-YL-(2,4-DICHLORO-PHENYL)-METHANONE Preparation Products And Raw materials
Raw materials
Preparation Products
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BENZOTRIAZOL-1-YL-(2,4-DICHLORO-PHENYL)-METHANONE Spectrum
200626-61-5, BENZOTRIAZOL-1-YL-(2,4-DICHLORO-PHENYL)-METHANONERelated Search:
  • 抑制剂
  • 化工试剂
  • 药靶配体
  • 标准品
  • 活性小分子库
  • DNA-RNA Transcription Regulators
  • Gene Regulation and Expression
  • BioChemical
  • Cell Biology
  • Cell Signaling and Neuroscience
  • 化合物ITSA1,10 MM DMSO 溶液
  • ITSA-1,HDAC活化剂
  • ITSA-1,HDAC激活剂
  • (1H-苯并[D][1,2,3]三唑-1-基)(2,4-二氯苯基)甲酮
  • 化合物ITSA1
  • 200626-61-5
  • ITSA-1, 10 mM in DMSO
  • ITSA-1, HDAC activator
  • inhibit,Histone deacetylases,ITSA-1,Inhibitor,HDAC,ITSA 1
  • (1H-Benzo[d][1,2,3]triazol-1-yl)(2,4-dichlorophenyl)methanone
  • Methanone, 1H-benzotriazol-1-yl(2,4-dichlorophenyl)-
  • CS-2249
  • ITSA-1(ITSA1)
  • 1-(2,4-Dichlorobenzoyl)-1H-benzotriazole
  • BENZOTRIAZOL-1-YL-(2,4-DICHLORO-PHENYL)-METHANONE
  • IFLAB-BB F0451-3184

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