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SGC 0946 Sale

目录号 : GC11491

A potent inhibitor of DOT1L

SGC 0946 Chemical Structure

Cas No.:1561178-17-3

规格 价格 库存 购买数量
1mg
¥386.00
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5mg
¥891.00
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10mg
¥1,418.00
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25mg
¥2,835.00
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50mg
¥5,292.00
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Sample solution is provided at 25 µL, 10mM.

Description

SGC 0946 is a potent small-molecule inhibitor of protein methyltransferase (PMT) DOT1L, a unique protein lysine methyltransferase (PKMT) catalyzing the methylation of histone H3 on Lysine 79 (H3K79), with the half maximal inhibition concentration IC50 value of 0.3 nM [1].

As a brominated analogue of EPZ004777, SGC 0946 exhibits substantially increased cellular inhibitory potency than its predecessor, where SGC 0946 reduces the methylation of H3K79 in both MCF10A (IC50: 8.8 nM) and A431 (IC50: 2.65 nM) cells compared with EPZ004777 (IC50: 84 nM and 264 nM respectively). This greatly increased cellular inhibitory potency of SGC 0946 can be attributed to lower off-rate and to improved cell permeability [1].

Reference

References:
[1] Yu W, Chory EJ, Wernimont AK, Tempel W, Scopton A, Federation A, Marineau JJ, Qi J, Barsyte-Lovejoy D, Yi J, Marcellus R, Iacob RE, Engen JR, Griffin C, Aman A, Wienholds E, Li F, Pineda J, Estiu G, Shatseva T, Hajian T, Al-Awar R, Dick JE, Vedadi M, Brown PJ, Arrowsmith CH, Bradner JE, Schapira M. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288. doi: 10.1038/ncomms2304.

实验参考方法

Cell experiment [1]:

Cell lines

Molm13 MLL and A431 cell lines

Preparation method

The solubility of this compound in DMSO is >31 mg/ml. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0-10 μM

Applications

SGC0946 showed time- and dose-dependent reductions in the H3K79me2 mark in the Molm13 MLL cell line that has the MLL/AF9 translocation. Quantitative assessment of H3K79me2 levels as measured by automated epifluorescence microscopy in MCF10A cells showed a substantially improved DOT1L inhibitory potency of SGC0946 (IC50 8.8±1.6 nM) compared with EPZ004777 (IC50 84±20nM). A similar observation was made in A431 cells, with IC50s of 2.65 nM and 264nM for SGC0946 and EPZ004777, respectively.

References:

[1] Yu W, Chory EJ, Wernimont AK, Tempel W, Scopton A, Federation A, Marineau JJ, Qi J, Barsyte-Lovejoy D, Yi J, Marcellus R, Iacob RE, Engen JR, Griffin C, Aman A, Wienholds E, Li F, Pineda J, Estiu G, Shatseva T, Hajian T, Al-Awar R, Dick JE, Vedadi M, Brown PJ, Arrowsmith CH, Bradner JE, Schapira M. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288.

化学性质

Cas No. 1561178-17-3 SDF
Canonical SMILES CC(C)(C)C1=CC=C(NC(NCCCN(C[C@@H]2[C@@H](O)[C@@H](O)[C@H](N3C4=NC=NC(N)=C4C(Br)=C3)O2)C(C)C)=O)C=C1
分子式 C28H40BrN7O4 分子量 618.57
溶解度 ≥ 30.95 mg/mL in DMSO, ≥ 97.6 mg/mL in EtOH with ultrasonic 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.6166 mL 8.0832 mL 16.1663 mL
5 mM 0.3233 mL 1.6166 mL 3.2333 mL
10 mM 0.1617 mL 0.8083 mL 1.6166 mL
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