1. Autophagy Apoptosis
  2. ULK Autophagy Apoptosis
  3. LYN-1604

LYN-1604 是一种有效的 UNC-51 样激酶 1 (ULK1) 激活剂,EC50 值为 18.94 nM。LYN-1604 可用于三阴性乳腺癌 (TNBC) 的研究。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 LYN-1604 dihydrochloride 通常具有更好的水溶性和稳定性。

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LYN-1604 Chemical Structure

LYN-1604 Chemical Structure

CAS No. : 2088939-99-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC)[1].

IC50 & Target[1]

ULK1

18.94 nM (EC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MDA-MB-231 IC50
1.66 μM
Compound: 8; LYN-1604
Antiproliferative activity against human MDA-MB-231 cells by MTT assay
Antiproliferative activity against human MDA-MB-231 cells by MTT assay
[PMID: 29509411]
体外研究
(In Vitro)

LYN-1604 is a potential ULK1 agonist (enzymatic activity=195.7% at 100 nM and IC50=1.66 μM against MDA-MB-231 cells) [1].
LYN-1604 binds to wild-type ULK1 with a binding affinity in the nanomole range (KD=291.4 nM) [1].
LYN-1604 (0.5, 1.0 and 2.0 μM) induces cell death via the ULK complex in MDA-MB-231 cells[1].
LYN-1604 (0.5-2 μM, 24 hours) induces remarkable up-regulation of Beclin-1 and degradation of p62, as well as transformation of LC3-I to LC3-II in MDA-MB-231 cells[1].
LYN-1604 induces ATG5-dependent autophagy via the ULK complex[1].
LYN-1604 can also increase cleavage of caspase3 and induce apoptosis[1].

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

Cell Viability Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5, 1.0 and 2.0 μM
Incubation Time:
Result: Induced cell death. Autophagy ratio was increased in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0, 0.5, 1, and 2 μM
Incubation Time: 24 hours
Result: Induced remarkable up-regulation of Beclin-1 and degradation of p62, as well as transformation of LC3-I to LC3-II.
体内研究
(In Vivo)

LYN-1604 (low dose, 25 mg/kg; median dose, 50 mg/kg; high dose, 100 mg/kg; intragastric administration once a day for 14 days) inhibits the growth of xenograft TNBC by targeting ULK1-modulated cell death[1].

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

Animal Model: 24 female nude mice (BALB/c, 6-8 weeks, 20-22 g)[1]
Dosage: Low dose, 25 mg/kg; median dose, 50 mg/kg; high dose, 100 mg/kg
Administration: Intragastric administration; once a day for 14 days
Result: Significantly inhibited the growth of xenograft MDA-MB-231 cells. The body weights of mice were stable. By the end of the experiment, the liver and spleen weight indexes of mice were slightly increased in parts of the groups, while the kidney weight index was not affected in all dose groups.
分子量

584.62

Formula

C33H43Cl2N3O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (171.05 mM; 超声加热助溶; 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 1.7105 mL 8.5526 mL 17.1051 mL
5 mM 0.3421 mL 1.7105 mL 3.4210 mL
查看完整储备液配制表
  • 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

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7105 mL 8.5526 mL 17.1051 mL 42.7628 mL
5 mM 0.3421 mL 1.7105 mL 3.4210 mL 8.5526 mL
10 mM 0.1711 mL 0.8553 mL 1.7105 mL 4.2763 mL
15 mM 0.1140 mL 0.5702 mL 1.1403 mL 2.8509 mL
20 mM 0.0855 mL 0.4276 mL 0.8553 mL 2.1381 mL
25 mM 0.0684 mL 0.3421 mL 0.6842 mL 1.7105 mL
30 mM 0.0570 mL 0.2851 mL 0.5702 mL 1.4254 mL
40 mM 0.0428 mL 0.2138 mL 0.4276 mL 1.0691 mL
50 mM 0.0342 mL 0.1711 mL 0.3421 mL 0.8553 mL
60 mM 0.0285 mL 0.1425 mL 0.2851 mL 0.7127 mL
80 mM 0.0214 mL 0.1069 mL 0.2138 mL 0.5345 mL
100 mM 0.0171 mL 0.0855 mL 0.1711 mL 0.4276 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:
LYN-1604
目录号:
HY-101923
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