7648/5 | Tocris Bioscience 7648/5 product information

product summary

company name :

Tocris Bioscience

product type :

chemical

product name :

7648/5

catalog :

7648/5

quantity :

5 mg

price :

349 USD

more info or order :

Tocris Bioscience product webpage

image

image 1 :

Selective ASH1L histone methyltransferase inhibitor

product information

master code :

7648

SKU :

7648/5

product name :

AS 99

unit size :

5 mg

description :

Selective ASH1L histone methyltransferase inhibitor

target :

Lysine Methyltransferase Inhibitors

category :

Small Molecules

purity :

98%

observed molecular weight :

593.68

url print :

?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules

details of functionality :

AS 99 is a selective ASH1L histone methyltransferase inhibitor (IC50 = 0.79 it binds to the autoinhibitory loop region in the SET domain (Kd = 0.89 M). AS 99 exhibits 100-fold selectivity for ASH1L over a range of lysine methyltransferases; no significant inhibition is observed at 50 M 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.

top caption :

Selective ASH1L histone methyltransferase inhibitor

extended description :

Selective ASH1L histone methyltransferase inhibitor

chemical name text :

N-[[3-[3-(Aminothioxomethyl)phenyl]-1-[1-[(trifluoromethyl)sulfonyl]-4-piperidinyl]-1H-indol-6-yl]methyl]-1-methyl-3-azetidinecarboxamide

formula :

C27H30F3N5O3S2

formula text :

C27H30F3N5O3S2

cas num :

2323623-93-2

USD :

349 USD

product details :

Selective ASH1L histone methyltransferase inhibitor

storage :

Store at -20░C

more info or order :

Tocris Bioscience product webpage