Millipore Sigma Vibrant Logo

505487 PKM2 Activator IV, TEPP-46 - Calbiochem

PKM2 Activator IV, TEPP-46, CAS 1221186-53-3, is a cell-permeable, allosteric PKM2 activator (AC50 = 92 nM) that stabilizes PKM2 tetramer via stoichiometric interaction with FBP-bound PKM2.

PKM2 Activator IV, TEPP-46 - Calbiochem: のSDS（安全データシート）、CoA（試験成績書）およびCoQ（品質証明書）、カタログなど製品関連の技術資料を入手いただけます。

同義語: TEPP46, Pyruvate Kinase M2 Activator IV, ML265, NCGC00186528, 6-((3-Aminophenyl)methyl)-4-methyl-2-methylsulfinylthieno[3,4]pyrrolo[1,3-d]pyridazin-5-one

Primary Target: PKM2
View This Product on Sigma-Aldrich
505487
価格＆在庫状況を照会

概要

Replacement Information

主要スペック表

CAS #Empirical Formula
1221186-53-3C₁₇H₁₆N₄O₂S₂

価格＆在庫状況

カタログ番号 在庫状況包装 Qty/Pk 価格 数量
5.05487.0001
在庫状況検索中…
—
現在国内在庫なし 現在国内在庫なし
現在国内在庫有り 
販売中止
在庫僅少
現在国内在庫あり
    Remaining : Will advise
      Remaining : Will advise
      注文対象外
      お問合せください
      Contact Customer Service

      		 ｶﾞﾗｽﾋﾞﾝ 5 mg
      価格を検索中…
      価格が見つかりません
      Minimum Quantity needs to be mulitiple of
      Maximum Quantity is
      弊社照会 詳細を表示　
      値引
      ()
       
      —
      弊社照会
      		 —
      Description
      OverviewA 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.
      Catalogue Number505487
      Brand Family Calbiochem®
      SynonymsTEPP46, Pyruvate Kinase M2 Activator IV, ML265, NCGC00186528, 6-((3-Aminophenyl)methyl)-4-methyl-2-methylsulfinylthieno[3,4]pyrrolo[1,3-d]pyridazin-5-one
      References
      ReferencesAnastasiou, D., et al. 2012. Nat. Chem. Biol. 8, 839.
      Jiang, J.K., et al. 2010. Bioorg. Med. Chem. Lett. 20, 3387.
      Product Information
      CAS number1221186-53-3
      FormWhite solid
      Hill FormulaC₁₇H₁₆N₄O₂S₂
      Chemical formulaC₁₇H₁₆N₄O₂S₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationPKM2 Activator IV, TEPP-46, CAS 1221186-53-3, is a cell-permeable, allosteric PKM2 activator (AC50 = 92 nM) that stabilizes PKM2 tetramer via stoichiometric interaction with FBP-bound PKM2.
      Biological Information
      Primary TargetPKM2
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      カタログ番号 GTIN
      5.05487.0001 04055977243383

      Documentation

      PKM2 Activator IV, TEPP-46 - Calbiochem (M)SDS

      タイトル

      英語版製品安全データシート（(M)SDS） 

      参考資料

      参考資料の概要
      Anastasiou, D., et al. 2012. Nat. Chem. Biol. 8, 839.
      Jiang, J.K., et al. 2010. Bioorg. Med. Chem. Lett. 20, 3387.

      カタログ

      タイトル
      New Products - Antibodies, Assays, Small Molecules, Inhibitors, and Proteins Volume 2, 2014
      データシート

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision10-March-2014 JSW
      SynonymsTEPP46, Pyruvate Kinase M2 Activator IV, ML265, NCGC00186528, 6-((3-Aminophenyl)methyl)-4-methyl-2-methylsulfinylthieno[3,4]pyrrolo[1,3-d]pyridazin-5-one
      DescriptionA 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.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1221186-53-3
      Chemical formulaC₁₇H₁₆N₄O₂S₂
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesAnastasiou, D., et al. 2012. Nat. Chem. Biol. 8, 839.
      Jiang, J.K., et al. 2010. Bioorg. Med. Chem. Lett. 20, 3387.