5.31711

DOT1L Inhibitor, SYC-522

• Synonym(e): DOT1L Inhibitor, SYC-522, Histone methyltransferase DOT1L Inhinitor, SYC-522
• Empirische Formel (Hill-System): C₂₇H₄₀N₈O₄
• CAS-Nummer: 1381761-52-9
• Molekulargewicht: 540.66
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Qualitätsniveau: 100
• Form: solid
• Wirksamkeit: 500 pM K_i
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: white to light yellow
• Löslichkeit: DMSO: 50 mg/mL
• Lagertemp.: −20°C

Beschreibung

Allgemeine Beschreibung

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. Wirkung

Cell permeable: yes

Primary Target
DOT1L

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable