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  1. Epigenetics Apoptosis
  2. Histone Demethylase Apoptosis
  3. Bomedemstat

Bomedemstat (IMG-7289) 是一種具有口服活性和不可逆的 lysine-specific demethylase 1 (LSD1) 抑制劑。Bomedemstat 可以增加 H3K4 和 H3K9 的甲基化,然后改變基因表達(dá)。Bomedemstat 具有抗癌活性,可抑制癌細(xì)胞增殖并誘導(dǎo)細(xì)胞凋亡。

該游離形式化合物不穩(wěn)定,推薦具有相同生物學(xué)活性的穩(wěn)定鹽形式 Bomedemstat dihydrochloride,Bomedemstat ditosylateBomedemstat hydrochloride。

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Bomedemstat Chemical Structure

Bomedemstat Chemical Structure

CAS No. : 1990504-34-1

1.  客戶無需承擔(dān)相應(yīng)的運輸費用。

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Bomedemstat 的其他形式現(xiàn)貨產(chǎn)品:

Customer Review

Other Forms of Bomedemstat:

查看 Histone Demethylase 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis[1][2].

IC50 & Target

KDM1/LSD1

 

體外研究
(In Vitro)

Bomedemstat selectively inhibits proliferation and induces apoptosis of Jak2V617F cells by concomitantly increasing expression and methylation of p53[1].
Bomedemstat (50 nM-1 μM; 96 h) enhances survival, induces apoptosis via BCL-XL and PUMA in a TP53-dependent manner, and leads to cell cycle arrest[1].

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

Apoptosis Analysis[1]

Cell Line: SET-2 cells
Concentration: 50?nM, 100?nM, and 1?μM
Incubation Time: 96 hours
Result: Decreased levels of the antiapoptotic protein BCL-XL and increased levels of the pro-apoptotic protein PUMA.
體內(nèi)研究
(In Vivo)

Bomedemstat treatment (oral gavage; 45?mg/kg; once daily; 56 d) normalizes or improves blood cell counts, reduces spleen volumes, restores normal splenic architecture, and reduces bone marrow fibrosis[1].

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

Animal Model: Mx-Jak2V617F mice[1]
Dosage: 45?mg/kg
Administration: Oral gavage; 45?mg/kg; once daily; 56 days
Result: Reduced splenomegaly significantly with a few treated mice normalizing their spleen weight, the 56-day course led to partial restoration of lymph follicles and spleen architecture by histological examination.
Clinical Trial
分子量

519.61

Formula

C28H34FN7O2

CAS 號
性狀

油狀物

顏色

Colorless to light yellow

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Pure form -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實驗: 

DMSO 中的溶解度 : 100 mg/mL (192.45 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 1.9245 mL 9.6226 mL 19.2452 mL
5 mM 0.3849 mL 1.9245 mL 3.8490 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。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

動物溶解方案計算器
請輸入動物實驗的基本信息:

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

由于實驗過程有損耗,建議您多配一只動物的量
計算結(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。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1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 1.9245 mL 9.6226 mL 19.2452 mL 48.1130 mL
5 mM 0.3849 mL 1.9245 mL 3.8490 mL 9.6226 mL
10 mM 0.1925 mL 0.9623 mL 1.9245 mL 4.8113 mL
15 mM 0.1283 mL 0.6415 mL 1.2830 mL 3.2075 mL
20 mM 0.0962 mL 0.4811 mL 0.9623 mL 2.4057 mL
25 mM 0.0770 mL 0.3849 mL 0.7698 mL 1.9245 mL
30 mM 0.0642 mL 0.3208 mL 0.6415 mL 1.6038 mL
40 mM 0.0481 mL 0.2406 mL 0.4811 mL 1.2028 mL
50 mM 0.0385 mL 0.1925 mL 0.3849 mL 0.9623 mL
60 mM 0.0321 mL 0.1604 mL 0.3208 mL 0.8019 mL
80 mM 0.0241 mL 0.1203 mL 0.2406 mL 0.6014 mL
100 mM 0.0192 mL 0.0962 mL 0.1925 mL 0.4811 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:
Bomedemstat
目錄號:
HY-109169
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