531711 DOT1L Inhibitor, SYC-522 - Calbiochem

531711
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₇H₄₀N₈O₄

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      Glass bottle 5 mg
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      Description
      OverviewA cell permeable S-adenosyl-L-methionine (SAM) derivative that acts as a highly potent and selective inhibitor of histone 3-lysine79 (H3K79) methyltransferase DOT1L (Ki = 500 pM ) and inhibits H3K79 methylation. Does not affect the activity of PRMT1, CARM1 and SUV39H1 (IC50 > 100 µM). Blocks cell cycle at the G0/G1 phase. Although it does not induce apoptosis, it sensitizes MLL rearranged leukemia cells to chemotherapeutic agents (mitoxantrone, etoposide, cytarabine) to cause apoptotic cell death. Shown to down-regulate the expression of HOXA9 and MEIS1, leukemia-relevant genes, by over 50%.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number531711
      Brand Family Calbiochem®
      SynonymsHistone methyltransferase DOT1L Inhinitor, SYC-522
      References
      ReferencesLiu, W., et al. 2014. PLoS One. 9, e98270.
      Anglin, J.L., et al. 2012. J. Med. Chem. 55, 8066.
      Product Information
      FormLight yellow solid
      Hill FormulaC₂₇H₄₀N₈O₄
      Chemical formulaC₂₇H₄₀N₈O₄
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetDOT1L
      Primary Target K<sub>i</sub>500 pM
      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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°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

      Documentation

      DOT1L Inhibitor, SYC-522 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Liu, W., et al. 2014. PLoS One. 9, e98270.
      Anglin, J.L., et al. 2012. J. Med. Chem. 55, 8066.

      Technical Info

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      White Paper - The Message in the Marks: Deciphering Cancer Epigenetics
      White Paper: Further considerations of antibody validation and usage.
      Data Sheet

      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.

      Revision27-March-2015 JSW
      SynonymsHistone methyltransferase DOT1L Inhinitor, SYC-522
      DescriptionA cell permeable S-adenosyl-L-methionine (SAM) derivative that acts as a highly potent and selective inhibitor of histone 3-lysine79 (H3K79) methyltransferase DOT1L (Ki = 500 pM ) and inhibits H3K79 methylation. Does not affect the activity of PRMT1, CARM1 and SUV39H1 (IC50 > 100 µM). Blocks cell cycle at the G0/G1 phase. Although it does not induce apoptosis, it sensitizes MLL rearranged leukemia cells to chemotherapeutic agents (mitoxantrone, etoposide, cytarabine) to cause apoptotic cell death. Shown to down-regulate the expression of HOXA9 and MEIS1, leukemia-relevant genes, by over 50%.
      FormLight yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₇H₄₀N₈O₄
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage -20°C
      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.
      Toxicity Standard Handling
      ReferencesLiu, W., et al. 2014. PLoS One. 9, e98270.
      Anglin, J.L., et al. 2012. J. Med. Chem. 55, 8066.