Merck

505487

Sigma-Aldrich

PKM2 Activator IV, TEPP-46

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別名:
PKM2 Activator IV, TEPP-46, 6-((3-Aminophenyl)methyl)-4-methyl-2-methylsulfinylthieno[3,4]pyrrolo[1,3-d]pyridazin-5-one, Pyruvate Kinase M2 Activator IV, ML265, NCGC00186528, TEPP46, Pyruvate Kinase M2 Activator IV, ML265, NCGC00186528, TEPP46, 6-((3-Aminophenyl)methyl)-4-methyl-2-methylsulfinylthieno[3,4]pyrrolo[1,3-d]pyridazin-5-one
Empirical Formula (Hill Notation):
C17H16N4O2S2
CAS番号:
分子量:
372.46

アッセイ

≥98% (HPLC)

品質水準

形状

solid

manufacturer/tradename

Calbiochem®

保管条件

OK to freeze
protect from light

white

溶解性

DMSO: 100 mg/mL

輸送温度

ambient

保管温度

2-8°C

InChI

1S/C17H16N4O2S2/c1-20-13-7-14(25(2)23)24-16(13)12-8-19-21(17(22)15(12)20)9-10-4-3-5-11(18)6-10/h3-8H,9,18H2,1-2H3

InChI key

ZWKJWVSEDISQIS-UHFFFAOYSA-N

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当該品目
550602324879550601
PKM2 Activator IV, TEPP-46

Sigma-Aldrich

505487

PKM2 Activator IV, TEPP-46

PKM2 Activator II, DASA The PKM2 Activator II, DASA modulates the biological activity of PKM2. This small molecule/inhibitor is primarily used for Biochemicals applications.

Sigma-Aldrich

550602

PKM2 Activator II, DASA

Pyruvate Kinase Activator The Pyruvate Kinase Activator controls the biological activity of Pyruvate Kinase. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

Sigma-Aldrich

550601

Pyruvate Kinase Activator

form

solid

form

powder

form

solid

form

powder

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

color

white

color

white

color

yellow-white

color

white

solubility

DMSO: 100 mg/mL

solubility

DMSO: 50 mg/mL

solubility

DMSO: 50 mg/mL

solubility

DMSO: 100 mg/mL, clear, colorless

詳細

A cell-permeable thienopyrrolopyridazinone that acts as a potent allosteric PKM2 activator (AC50 = 92 nM; [PKM2] = 0.1 nM) via stoichiometric interaction (Two activator molecules per tetramer) with FBP-bound PKM2 tetramer (One FBP per monomer) in a similar manner as PKM2 Activator III (Cat. No. 504537), resulting in highly stabilized PKM2 tetramer resistant to dissociation in the presence of phosphotyrosine-containing peptide/protein or upon PKM2 K305Q mutation. Reported to exhibit good aqueous solubility (29.6 µg/mL or 79.5 µM in PBS, pH 7.4) and retard human lung carcinoma H1299 proliferation under hypoxia, but not normoxia, condition in cultures (doubling time = 50 and 35 h, respectively, with or without 30 µM TEPP-46; 1% O2) in vitro. TEPP-46 is bioavailable in mice via i.p. (Tmax = 0.5 h; Cmax = 10.854 µg/mL; AUCINF = 26.994 hr·µg/mL; 10 mg/kg) or p.o. (Tmax = 0.25 h; Cmax = 10.179 µg/mL; AUCINF = 24.350 hr·µg/mL; 10 mg/kg) administration and shown to impair H1299 tumorigenesis in mice (%tumor development/av. tumor weight = 30%/0.13 mg and 70%/2.6 mg, respectively, with or without 50 mg/kg/12 h oral dosage for 7 wks) in vivo with no apparent toxicity.
A cell-permeable thienopyrrolopyridazinone that exhibits good aqueous solubility (29.6 µg/mL or 79.5 µM in PBS, pH 7.4) and acts as a potent allosteric PKM2 activator (AC50 = 92 nM; [PKM2] = 0.1 nM) by stabilizing PKM2 tetramer via stoichiometric interaction with FBP-bound PKM2 (2 activator/4 FBP/tetramer) in a similar manner as PKM2 Activator III (Cat. No. 504537). Reprorted to retard human lung carcinoma H1299 proliferation under hypoxia, but not normoxia, condition in cultures (doubling time = 50 and 35 h, respectively, with or without 30 µM TEPP-46; 1% O2) in vitro and impair H1299 tumorigenesis in mice (50 mg/kg/12 h p.o.) in vivo with no apparent toxicity.

生物化学的/生理学的作用

Cell permeable: yes
Primary Target
PKM2
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Use only fresh DMSO for reconstitution.

その他情報

Anastasiou, D., et al. 2012. Nat. Chem. Biol.8, 839.

Jiang, J.K., et al. 2010. Bioorg. Med. Chem. Lett.20, 3387.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

保管分類コード

11 - Combustible Solids

WGK

WGK 3

引火点(°F)

Not applicable

引火点(℃)

Not applicable


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