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  2. Epigenetics Apoptosis NF-κB Immunology/Inflammation
  3. Histone Methyltransferase Apoptosis NF-κB TNF Receptor Interleukin Related
  4. MM-102

MM-102 (HMTase Inhibitor IX) 是一種具有細(xì)胞滲透性并緊密結(jié)合的 MLL1-WDR5 相互作用抑制劑 (IC50=2.4 nM)。MM-102 能特異性抑制含有 MLL1 融合蛋白的白血病細(xì)胞的生長和誘導(dǎo)細(xì)胞凋亡 (apoptosis)，并減輕缺血再灌注損傷小鼠腎臟纖維化和炎癥反應(yīng)。此外，MM-102 也作為 H3K4 組蛋白甲基轉(zhuǎn)移酶抑制劑來改善豬體細(xì)胞核移植 (SCNT) 胚胎發(fā)育。

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MM-102 Chemical Structure

MM-102 Chemical Structure

CAS No. : 1417329-24-8

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規(guī)格 價格 是否有貨 數(shù)量
2 mg ￥750
In-stock
5 mg ￥1540
In-stock
10 mg ￥2520
In-stock
50 mg 現(xiàn)貨 詢價
100 mg   詢價  
200 mg   詢價  

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Other Forms of MM-102:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

MM-102 (HMTase Inhibitor IX) is a cell-permeable and tightly binding inhibitor of MLL1-WDR5 interaction (IC50=2.4 nM). MM-102 can specifically inhibit the growth and induce apoptosis of leukemia cells containing MLL1 fusion protein, and reduce renal fibrosis and inflammation in mice with ischemia-reperfusion injury. In addition, MM-102 also acts as an H3K4 histone methyltransferase inhibitor to improve the development of porcine somatic cell nuclear transfer (SCNT) embryos[1][2][3][4][5].

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
K562 IC50
37.8 μM
Compound: MM-102
Growth inhibition of human K562 cells after 7 days by MTS assay
Growth inhibition of human K562 cells after 7 days by MTS assay
[PMID: 27598236]
K562 IC50
37.8 μM
Compound: MM-102
Antiproliferative activity against human K562 cells harboring BCR-ABL assessed as inhibition of cell viability after 72 hrs by CCK8-based colorimetric assay
Antiproliferative activity against human K562 cells harboring BCR-ABL assessed as inhibition of cell viability after 72 hrs by CCK8-based colorimetric assay
[PMID: 27720555]
MV4-11 IC50
20.7 μM
Compound: MM-102
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 fusion protein after 72 hrs by CCK8 assay
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 fusion protein after 72 hrs by CCK8 assay
[PMID: 27598236]
MV4-11 IC50
20.7 μM
Compound: MM-102
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as inhibition of cell viability after 72 hrs by CCK8-based colorimetric assay
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 assessed as inhibition of cell viability after 72 hrs by CCK8-based colorimetric assay
[PMID: 27720555]
MV4-11 IC50
25 μM
Compound: MM-102
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 fusion protein by CellTiter-Glo assay
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 fusion protein by CellTiter-Glo assay
[PMID: 27598236]
MV4-11 IC50
25 μM
Compound: MM-102
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 after 7 days by CellTiter-Glo luminescent cell viability Assay
Antiproliferative activity against human MV4-11 cells harboring MLL-AF4 after 7 days by CellTiter-Glo luminescent cell viability Assay
[PMID: 27720555]
體外研究
(In Vitro)

MM-102 (40 μM; 4 d) 處理 MLL1-AF9 轉(zhuǎn)化的小鼠白血病細(xì)胞可特異性地誘導(dǎo)具有 MLL1 易位的白血病細(xì)胞生長停滯和細(xì)胞死亡，但不會干擾正常骨髓的生長[2]。
MM-102 (2、10 和 50 μM) 以濃度依賴的方式破壞了 WDR5 和 RbBP5 與 GSTMLL1 的關(guān)聯(lián)。在 2 μM 的劑量下，輕度破壞 WDR5 與 MLL1 的關(guān)聯(lián)，在 10 μM 劑量下中度破壞，在 50 μM 劑量下完全破壞[2]。
MM-102特異性地抑制 MLL1 復(fù)合物的甲基轉(zhuǎn)移酶活性，IC50 值為 0.32 μM[2]。
MM-102 (50 μM; 48 h) 可以顯著抑制 TFK1 和 RBE 細(xì)胞的增殖、遷移和化療耐藥[3]。
MM-102 (50 μM; 1 h) 不僅顯著降低 TGF-b1刺激的 NRK-49F 細(xì)胞中的 MLL1、WDR5 和 H3K4me3 的表達(dá)，還抑制 p16INK4a 的表達(dá)[4]。
MM-102 (50-100 μM; 48 h) 提高了豬 SCNT 胚胎的發(fā)育能力并改善了 SCNT 胚胎發(fā)育的關(guān)鍵基因表達(dá)模式[5]。

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

Cell Viability Assay[3]

Cell Line: TFK1 and RBE cells
Concentration: 50 μM
Incubation Time: 48 h
Result: Inhibited the expression of ABCB1, but had no effect on the expression of MBD2 and WDR5.
體內(nèi)研究
(In Vivo)

MM-102 (15 mg/kg；i.p.；每日 1 次，持續(xù) 7 天) 抑制原代 CCA 模型小鼠體內(nèi)腫瘤的進(jìn)展[3]。
MM-102 (15 mg/kg；i.p.；每日 1 次，持續(xù) 7 天) 抑制 p16INK4a 基因在 IRI 小鼠體內(nèi)表達(dá)，并減輕 IRI 小鼠的腎纖維化和腎臟炎癥[4]。

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

Animal Model: Ischemia-reperfusion injury in mice[4]
Dosage: 15 mg/kg
Administration: i.p.; Once daily for 7 days
Result: Inhibited a-SMA protein expression.
Inhibited p-NF-kB (p65), IL-1b, TNF-a, and IL-6 mRNA expression.
分子量

669.80

Formula

C35H49F2N7O4
CAS 號
性狀

固體

顏色

White to off-white

運(yùn)輸條件

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

Sealed storage, away from moisture and light, under nitrogen

Powder -80°C 2 years
-20°C 1 year

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

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 125 mg/mL (186.62 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.4930 mL 7.4649 mL 14.9298 mL
5 mM 0.2986 mL 1.4930 mL 2.9860 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)。-80°C儲存時，請?jiān)?個月內(nèi)使用，-20°C儲存時，請?jiān)?個月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計(jì)算器
請輸入動物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)。-80°C儲存時，請?jiān)?個月內(nèi)使用，-20°C儲存時，請?jiān)?個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4930 mL 7.4649 mL 14.9298 mL 37.3246 mL
5 mM 0.2986 mL 1.4930 mL 2.9860 mL 7.4649 mL
10 mM 0.1493 mL 0.7465 mL 1.4930 mL 3.7325 mL
15 mM 0.0995 mL 0.4977 mL 0.9953 mL 2.4883 mL
20 mM 0.0746 mL 0.3732 mL 0.7465 mL 1.8662 mL
25 mM 0.0597 mL 0.2986 mL 0.5972 mL 1.4930 mL
30 mM 0.0498 mL 0.2488 mL 0.4977 mL 1.2442 mL
40 mM 0.0373 mL 0.1866 mL 0.3732 mL 0.9331 mL
50 mM 0.0299 mL 0.1493 mL 0.2986 mL 0.7465 mL
60 mM 0.0249 mL 0.1244 mL 0.2488 mL 0.6221 mL
80 mM 0.0187 mL 0.0933 mL 0.1866 mL 0.4666 mL
100 mM 0.0149 mL 0.0746 mL 0.1493 mL 0.3732 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.

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產(chǎn)品名稱：
MM-102
目錄號：
HY-12220
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