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531711 DOT1L Inhibitor, SYC-522 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₇H₄₀N₈O₄

Products

Catalog NumberPackaging Qty/Pack
5.31711.0001 Glass bottle 5 mg
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
Global Trade Item Number
Catalog Number GTIN
5.31711.0001 04055977287080

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

Title
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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 Protect from light
-20°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
ReferencesLiu, W., et al. 2014. PLoS One. 9, e98270.
Anglin, J.L., et al. 2012. J. Med. Chem. 55, 8066.