Sigma-Aldrich Dot1l Inhibitor, Syc-522

Assay

≥98% (HPLC)

Quality Level

100

Form

solid

Potency

500 pM K_i

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

white to light yellow

Solubility

DMSO: 50 mg/mL

Storage Temp.

−20°C

General Description

A cell permeable S-adenosyl-L-methionine (SAM) derivative that acts as a highly potent and selective inhibitor of histone 3-lysine79 (H3K79) methyltransferase DOT1L (K_i= 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.A cell permeable S-adenosyl-L-methionine (SAM) derivative that acts as a highly potent and selective inhibitor of histone 3-lysine79 (H3K79) methyltransferase DOT1L (K_i= 500 pM ) and inhibits H3K79 methylation. Does not affect the activity of PRMT1, CARM1 and SUV39H1 (IC_{50>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%.} A cell permeable S-adenosyl-L-methionine (SAM) derivative that acts as a highly potent and selective inhibitor of histone 3-lysine79 (H3K79) methyltransferase DOT1L (K_i= 500 pM)

Biochem/Physiol Actions

Cell permeable: yesPrimary Target
DOT1L

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

Liu, W., et al. 2014.PLoS One. 9,e98270.
Anglin, J.L., et al. 2012.J. Med. Chem. 55,8066.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany