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  1. PI3K/Akt/mTOR Epigenetics Apoptosis
  2. AMPK Apoptosis
  3. EB-3D

EB-3D 是有效的選擇性膽堿激酶 α (ChoKα) 抑制劑,對 ChoKα1 的 IC50 值為 1 μM。EB-3D 對 ChoKα 表達、AMPK 激活、細胞凋亡 (apoptosis)、內(nèi)質(zhì)網(wǎng)應(yīng)激和脂質(zhì)代謝有影響。EB-3D 在一組T-白血病細胞系中顯示出強大的抗增殖活性。具有抗癌活性。

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EB-3D Chemical Structure

EB-3D Chemical Structure

CAS No. : 1839150-63-8

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity[1][2][3].

IC50 & Target

IC50: 1 μM; Kd: 0.7 μM[3]

體外研究
(In Vitro)

EB-3D 顯示 (0-100 μM;72 小時) 對廣泛的 T 白血病細胞系具有出色的抗增殖活性,GI GI50s 13 值在納摩爾范圍內(nèi)[1]。
EB-3D (1.25-5 μM;24小時) 誘導白血病細胞系凋亡[1]。
EB-3D (0.5-1 μM;24 小時) 誘導導致細胞凋亡的 G0/G1 期阻滯[1]。
EB-3D (0.3 μM;48 小時) 在 30 分鐘后顯示 AMPKα 激活的第一個尖峰以及隨后 T172[1] 的磷酸化增加。
EB-3D (1-40 μM;48 小時) 抑制 HepG2 細胞的細胞生長,GI50 14.55 μM[2]。
EB-3D 誘導 AMPK-mTOR 通路失調(diào)和白血病 T 細胞凋亡[1]。

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

Cell Proliferation Assay[1]

Cell Line: JURKAT, CCRF-CEM, HSB-2, MOLT-16, DNA-41, LOUCY, PEER, ALL-SIL cells
Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 72 hours
Result: Inhibited JURKAT, CCRF-CEM, HSB-2, MOLT-16, DNA-41, LOUCY, PEER, and ALL-SIL cells growth with GI50s of 136.2, 478.8, 17.7, 0.9, 60.6, 200, 265, and 132 nM, respectively.

Apoptosis Analysis[1]

Cell Line: Jurkat, CCRF-CEM and HSB-2 cells
Concentration: 1.25, 2.5, 5 μM
Incubation Time: 24 hours
Result: Induced apoptosis in leukemia cell lines.

Cell Cycle Analysis[1]

Cell Line: Jurkat, CCRF-CEM and HSB-2 cells
Concentration: 0.5, 1 μM
Incubation Time: 24 hours
Result: Induces cell cycle arrest in G0/G1 phase.

Western Blot Analysis[1]

Cell Line: Jurkat cells
Concentration: 0.3 μM
Incubation Time: 48 hours
Result: Showed a first spike of activation of AMPKα after 30 minutes of treatment and a later increase in the phosphorylation of T172. The increase in S79 phosphorylation of its main target ACC (acetyl-coenzyme A (CoA) carboxylase), followed the same pattern. This rapid activation of AMPK, in turn induced a consequent reduction in mTOR phosphorylation that is visible already at 30’ and that becomes amplified at longer time probably due to the interruption of feedback loops that are characteristic of mTOR connecting pathways.
體內(nèi)研究
(In Vivo)

EB-3D (1 mg/kg;腹腔注射;每隔一天) 在同源原位 E0771-C57BL/6 小鼠模型中抑制乳腺腫瘤的生長[4]。
EB-3D (2.5 mg /kg;每隔一天,持續(xù) 4 周) 顯示自發(fā)性肺大轉(zhuǎn)移和微轉(zhuǎn)移的數(shù)量減少[4]。

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

Animal Model: E0771-C57BL/6 mice[4]
Dosage: I.p.; every other day for 4 weeks
Administration: 2.5 mg/kg
Result: A reduction of the number of spontaneous lung macro- and micrometastasis.
分子量

644.44

Formula

C30H36Br2N4O2

CAS 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, sealed storage, away from moisture

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

溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : 50 mg/mL (77.59 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)

H2O 中的溶解度 : ≥ 9.09 mg/mL (14.11 mM)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.5517 mL 7.7587 mL 15.5173 mL
5 mM 0.3103 mL 1.5517 mL 3.1035 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)。-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。

* 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

  • 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

純度: 99.57%

參考文獻

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)。-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
H2O / DMSO 1 mM 1.5517 mL 7.7587 mL 15.5173 mL 38.7934 mL
5 mM 0.3103 mL 1.5517 mL 3.1035 mL 7.7587 mL
10 mM 0.1552 mL 0.7759 mL 1.5517 mL 3.8793 mL
DMSO 15 mM 0.1034 mL 0.5172 mL 1.0345 mL 2.5862 mL
20 mM 0.0776 mL 0.3879 mL 0.7759 mL 1.9397 mL
25 mM 0.0621 mL 0.3103 mL 0.6207 mL 1.5517 mL
30 mM 0.0517 mL 0.2586 mL 0.5172 mL 1.2931 mL
40 mM 0.0388 mL 0.1940 mL 0.3879 mL 0.9698 mL
50 mM 0.0310 mL 0.1552 mL 0.3103 mL 0.7759 mL
60 mM 0.0259 mL 0.1293 mL 0.2586 mL 0.6466 mL

* 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

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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Inquiry Information

產(chǎn)品名稱:
EB-3D
目錄號:
HY-115463
需求量: