SGC-iMLLT

An inhibitor of MLLT1 and MLLT3 YEATS domains

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库存: 现货

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数量
5mg

￥1100.00

880.00

- +
10mg

￥1737.00

1390.00

- +
50mg

￥5937.00

4750.00

- +
100mg

￥9175.00

7340.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajce53798
CAS: 2255338-25-9
别名:
分子式: C22H24N6O
分子量: 388.47
纯度: >98%
溶解度: DMSO : 83.33 mg/mL (214.51 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

SGC-iMLLT is an inhibitor of the YEATS domain-containing proteins MLLT1 and MLLT3.¹ It binds to the MLLT1 YEATS1 and MLLT3 YEATS3 domains (K_ds = 129 and 77 nM, respectively).¹ It is selective for YEATS1 and -3 over YEATS2 and -4 (IC₅₀s = >10 ?M), as well as a panel of 48 bromodomains at 50 ?M. SGC-iMLLT inhibits the interaction of histone H3.3 with MLLT3 (IC₅₀ = 400 nM in a reporter assay) and decreases expression of the tumorigenic genes MYC and DDN in MV-4-11 leukemia cells when used at a concentration of 1 ?M.

1.Moustakim, M., Christott, T., Monteiro, O.P., et al.Discovery of an MLLT1/3 YEATS domain chemical probeAngew. Chem. Int. Ed. Engl.57(50)16302-16307(2018)