1. Protein Tyrosine Kinase/RTK Autophagy Epigenetics PI3K/Akt/mTOR Apoptosis
  2. FAK ULK AMPK Apoptosis Autophagy
  3. ULK1-IN-2

ULK1-IN-2 (化合物 3s) 是一种有效的 ULK1 抑制剂。ULK1-IN-2 对癌细胞具有最高的细胞毒作用,A549 中 IC50 值为 1.94 μM。ULK1-IN-2 可诱导细胞凋亡同时阻断自噬,可用于研究非小细胞肺癌。

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ULK1-IN-2 Chemical Structure

ULK1-IN-2 Chemical Structure

CAS No. : 2497409-01-3

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ULK1-IN-2 (compound 3s) is a potent ULK1 inhibitor. ULK1-IN-2 shows highest cytotoxic effect against cancer cell lines, with IC50 of 1.94 μM in A549. ULK1-IN-2 can induce apoptosis and simultaneously block autophagy, and can be used to study NSCLC (Non-small cell lung cancer)[1].

IC50 & Target

ULK1

 

体外研究
(In Vitro)

ULK1-IN-2 (compound 3s) (10 μM, 24 h) shows strong anti-proliferative activity against A549, U937, HL60, MDA-MB-468 and MCF-7[1].
ULK1-IN-2 (0-8 μM, 24 h) blocks autophagy via inhibiting ULK1 in A549 cells[1].
ULK1-IN-2 (0-8 μM, 24 h) induces apoptosis via the mitochondrial pathways in A549 cells in dose department manner[1].
ULK1-IN-2 (0-8 μM, 24 h) inhibits ULK1 and p-ULK1ser317 expression in a concentration-dependent manner, remarkably decreases Bcl-2 expression, increases Bax and the active form of Caspase-3 expression.[1].

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

Cell Proliferation Assay

Cell Line: Human cancer cell lines A549, U937, HL60, MDA-MB-468 and MCF-7[1]
Concentration: 10 μM
Incubation Time: 24 h
Result: Significantly improved anti-proliferative activity against A549, U937, HL60, MDA-MB-468 and MCF-7, with kinase inhibitory activity of 99.15% and IC50 values of 1.94, 12.92, 10.89, 16.83, and 19.60 μM, respectively.

Cell Autophagy Assay

Cell Line: A549 cells[1]
Concentration: 0, 2, 4, 8 μM
Incubation Time: 24 h
Result: Blocked autophagy of A549 cells via inhibiting ULK.

Western Blot Analysis

Cell Line: A549 cells[1]
Concentration: 0, 2, 4, 8 μM
Incubation Time: 24 h
Result: Inhibited expression of ULK1 and p-ULK1ser317 in a concentration-dependent manner. Increased the autophagy substrate P62, reduced LC3-I conversion to LC3-II, and decreased the levels of Beclin1. Remarkably decreased Bcl-2 expression, increased Bax and the active form of Caspase-3 expression.
分子量

495.26

Formula

C19H16BrFN4O6

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

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

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 33.33 mg/mL (67.30 mM; 超声助溶; 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 2.0191 mL 10.0957 mL 20.1914 mL
5 mM 0.4038 mL 2.0191 mL 4.0383 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 and light)。-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

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
参考文献

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 and light)。-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 2.0191 mL 10.0957 mL 20.1914 mL 50.4785 mL
5 mM 0.4038 mL 2.0191 mL 4.0383 mL 10.0957 mL
10 mM 0.2019 mL 1.0096 mL 2.0191 mL 5.0479 mL
15 mM 0.1346 mL 0.6730 mL 1.3461 mL 3.3652 mL
20 mM 0.1010 mL 0.5048 mL 1.0096 mL 2.5239 mL
25 mM 0.0808 mL 0.4038 mL 0.8077 mL 2.0191 mL
30 mM 0.0673 mL 0.3365 mL 0.6730 mL 1.6826 mL
40 mM 0.0505 mL 0.2524 mL 0.5048 mL 1.2620 mL
50 mM 0.0404 mL 0.2019 mL 0.4038 mL 1.0096 mL
60 mM 0.0337 mL 0.1683 mL 0.3365 mL 0.8413 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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产品名称:
ULK1-IN-2
目录号:
HY-143466
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