5.31711

DOT1L Inhibitor, SYC-522

• Synonim(y): DOT1L Inhibitor, SYC-522, Histone methyltransferase DOT1L Inhinitor, SYC-522
• Wzór empiryczny (zapis Hilla): C₂₇H₄₀N₈O₄
• Numer CAS: 1381761-52-9
• Masa cząsteczkowa: 540.66
• Kod UNSPSC: 12352200

Właściwości

• Próba: ≥98% (HPLC)
• Poziom jakości: 100
• Postać: solid
• siła działania: 500 pM K_i
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: white to light yellow
• rozpuszczalność: DMSO: 50 mg/mL
• temp. przechowywania: −20°C

Opis

Opis ogólny

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)

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
DOT1L

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable