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网站主页 2-Thiophenecarboxamide, N-[(1S)-1-cyclopropyl-2,2,2-trifluoroethyl]-4-[6-(4-fluorophenyl)pyrazolo[1,5-a]pyrimidin-3-yl]- 化合物 ULK-101
  • 化合物 ULK-101|T5403|TargetMol

化合物 ULK-101|T5403|TargetMol

ULK-101
2443816-45-1
828 1mg 起订
1270 2mg 起订
2790 5mg 起订
上海 更新日期:2024-12-12

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产品详情:

中文名称:
化合物 ULK-101
英文名称:
ULK-101
CAS号:
2443816-45-1
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格:
99.66%
产品类别:
抑制剂
货号:
T5403

Product Introduction

Bioactivity

名称ULK-101
描述ULK-101 is a potent and selective ULK1 inhibitor ( IC50s: 8.3/30 nM for ULK1/ULK2). It can suppress autophagy.
细胞实验Cells (U2OS or NSCLC) were seeded on tissue culture treated 96-well plates at 1,000 cells per well in RPMI-1640 media supplemented with 10% FBS. Twenty-four hours later, media was aspirated, wells rinsed with 1x DPBS, and replaced with full media (FM) or Optistarve (OS) with a concentration gradient of ULK-101 (final concentrations of 100 μM, 50 μM, 25 μM, 12.5 μM, 6.25 μM, 3.1 μM, 1.6 μM, 0.8 μM, 0.4 μM, or 0 μM). Two days later, media (and ULK-101) was aspirated, wells were rinsed with 1x DPBS, and all wells replaced with FM. Five days later, relative ATP levels were measured using a luminescent CellTiter-Glo assay.
激酶实验IC50 data for ULK1 and ULK2 was generated using 10-point IC50Profiler assays with half-log dilutions from top concentrations of 10 μM (4 replicates) and 1 μM (4 replicates), giving 8 data points for most concentrations in the curve. For selectivity profiling, KinaseProfiler assays with wild-type human kinase panels were performed in duplicate using 500 nM SBI-0206965, 40 nM ULK-101, or 15 nM ULK-100. For each kinase reaction, the Km concentration of ATP was used. The percent activity remaining and percent inhibition were calculated from negative control wells. For selectivity profiling, relative inhibition was calculated by dividing the percent inhibition of each kinase by the percent inhibition of ULK1. GraphPad Prism 7 was used for IC50 determinations by fitting curves with variable slope (four-parameter) non-linear regression models using top and bottom constraints of 100% and 0%, respectively.
体外活性U2OS cells were treated with AZD8055 for 2.5 hr, a catalytic mTOR inhibitor that strongly induces autophagy in U2OS cells and observed that the abundance of DFCP1-positive puncta increased over 3-fold. Co-treatment of cells with 5 μM ULK-101 completely abrogated the formation of DFCP1-positive structures induced by AZD8055 treatment, consistent with the loss of Beclin 1 phosphorylation.
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 5 mg/mL (10.86 mM), Sonication is recommended.
H2O : Insoluble
关键字Unc-51 like kinase | ULK-101 | ULK | ULK 101 | Inhibitor | inhibit | ULK101
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相关库抑制剂库 | 经典已知活性库 | 已知活性化合物库 | 自噬库 | 激酶抑制剂库 | NO PAINS 化合物库 | 表型筛选靶点鉴定库
ULK-101|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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