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Tocris Bioscience™ AS 99
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Produktkod. 18765955
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Kvantitet:
5 mg
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18765955 5 mg
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Produktkod. 18765955 Leverantör Tocris Bioscience™ Leverantörsnummer 7648/5

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Beskrivning

Selective ASH1L histone methyltransferase inhibitor

AS 99 is a selective ASH1L histone methyltransferase inhibitor (IC50 = 0.79 μM); it binds to the autoinhibitory loop region in the SET domain (Kd = 0.89 μM). AS 99 exhibits >100-fold selectivity for ASH1L over a range of lysine methyltransferases; no significant inhibition is observed at 50 μM against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2. In leukemia cells, AS 99 blocks H3K36 methylation, and causes a dose-dependent downregulation of MLL fusion target genes; it also induces apoptosis and differentiation and inhibits cell proliferation. AS 99 reduces leukemia burden in the xenotransplantation mouse model of MLL leukemia without affecting blood count in normal mice.
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Specifikationer

Kemiskt namn eller material N-[[3-[3-(Aminothioxomethyl)phenyl]-1-[1-[(trifluoromethyl)sulfonyl]-4-piperidinyl]-1 H-indol-6-yl]methyl]-1-methyl-3-azetidinecarboxamide
CAS 2323623-93-2
Kvantitet 5 mg
Mål Lysine Methyltransferase Inhibitors
Molekylformel C27H30F3N5O3S2
Renhet 0.98
Produkttitel
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