2. Epigenetics PROTAC
  3. Histone Methyltransferase PROTACs
  4. MS67

MS67 是一种有效的选择性 WD40 重复域蛋白 5 (WDR5) 降解剂，Kd 为 63 nM。MS67 对其他蛋白质甲基转移酶、激酶、GPCR、离子通道和转运蛋白无活性。MS67 显示出有效的抗癌作用。

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MS67 Chemical Structure

MS67 Chemical Structure

CAS No. : 2407452-77-9

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Customer Review

MS67 相关抗体

Top Publications Citing Use of Products

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects[1].

IC50 & Target[1]

VHL

 

WDR5

63 nM (Kd)

体外研究
(In Vitro)

MS67 (0.001-1 μM) induces WDR5 degradation at a concentration as low as 1 nM. MS67 induces WDR5 depletion much more effectively in all six mixed lineage leukemia (MLL)-r acute myeloid leukemia (AML) and four pancreatic ductal adenocarcinoma (PDAC) cell lines without a hook effect and in a concentration-dependent manner in PDAC cells[1].
MS67 decreases H3K4me2/3 in both MV4;11 and MIA PaCa-2 cells, whereas other examined histone methylation marks such as H3K9me3, H3K27me3, and H3K36me3 are not affected . MS67 is effective in suppressing both WDR5-related gene expression programs and WDR5/MLL-induced H3K4 methylations on chromatin[1].
The GI50 values of MS67 in the two most sensitive AML lines, MV4;11 and EOL-1, are 15 nM and 38 nM, respectively. MLL-r acute leukemia cell lines including MV4;11, EOL-1, MOLM13, KOPN8, RS4;11, and THP-1 are sensitive to MS67, whereas leukemia cell lines that did not harbor MLL-r (including K562, HL60, and a murine AML line transformed by Hoxa9 plus Meis1) are insensitive to MS67[1].
. MS67 binds to VCB (VHL-Elongin C-Elongin B ternary complex), with a Kd of 140 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

MS67 相关抗体:

Western Blot Analysis[1]

Cell Line: MV4;11 cells
Concentration: 0.001 μM, 0.005 μM, 0.01 μM, 0.05 μM, 0.1 μM, 0.5 μM, 1 μM
Incubation Time: 18 hours
Result: Induced WDR5 degradation at a concentration as low as 1 nM with DC50 of 3.7 nM.
体内研究
(In Vivo)

MS67 (75 mg/kg; i.p.; twice daily; 5 days a week; for 20 days) significantly inhibits tumor growth in vivo and prolongs survival of the treated mice[1].
After a single intraperitoneal (i.p.) injection of MS67 at a dose of 75 mg/kg, the Cmax reached at about 4.2 μM, and the concentration of MS67 retained above 0.5 μM over 12 hours[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MV4;11 MLL-r AML xenograft mouse[1]
Dosage: 75 mg/kg
Administration: i.p.; twice daily; 5 days a week; for 20 days
Result: Inhibited tumor growth in vivo.
分子量

1030.14

Formula

C52H59F4N9O7S
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (97.07 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9707 mL 4.8537 mL 9.7074 mL
5 mM 0.1941 mL 0.9707 mL 1.9415 mL
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 98.73%

COA (290 KB) HNMR (260 KB) LCMS (117 KB)

产品使用指南 (1538 KB)
参考文献

MS67 相关分类

完整储备液配制表

* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9707 mL 4.8537 mL 9.7074 mL 24.2685 mL
5 mM 0.1941 mL 0.9707 mL 1.9415 mL 4.8537 mL
10 mM 0.0971 mL 0.4854 mL 0.9707 mL 2.4269 mL
15 mM 0.0647 mL 0.3236 mL 0.6472 mL 1.6179 mL
20 mM 0.0485 mL 0.2427 mL 0.4854 mL 1.2134 mL
25 mM 0.0388 mL 0.1941 mL 0.3883 mL 0.9707 mL
30 mM 0.0324 mL 0.1618 mL 0.3236 mL 0.8090 mL
40 mM 0.0243 mL 0.1213 mL 0.2427 mL 0.6067 mL
50 mM 0.0194 mL 0.0971 mL 0.1941 mL 0.4854 mL
60 mM 0.0162 mL 0.0809 mL 0.1618 mL 0.4045 mL
80 mM 0.0121 mL 0.0607 mL 0.1213 mL 0.3034 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MS672407452-77-9MS 67MS-67Histone MethyltransferasePROTACsWDR5degraderProtacacticanceracutemyeloidleukemiaH3K4me2/3Inhibitorinhibitorinhibit

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