2. Autophagy Immunology/Inflammation Apoptosis
  3. ULK Beclin1 Autophagy MHC Caspase Apoptosis
  4. SBP-5147

SBP-5147 是一种具有口服活性的 ULK1/ULK2 抑制剂，其对 ULK1 的 IC50 为 2 nM，对 ULK2 的 IC50 为 53 nM。SBP-5147 可抑制 Beclin-1 和 Vps34 的磷酸化，减少自噬 (autophagy) 流，下调 ATG13 和 ATG101 的表达，上调 MHC-I 的表达，诱导半胱天冬酶 (caspase) 依赖性细胞凋亡 (apoptosis)，并降低非小细胞肺癌细胞的存活率。SBP-5147 可用于非小细胞肺癌的相关研究[1][2]。

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SBP-5147

SBP-5147 Chemical Structure

CAS No. : 1884222-37-0

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SBP-5147 相关抗体

Top Publications Citing Use of Products

查看 ULK 亚型特异性产品:

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ULK1 ULK2

查看 MHC 亚型特异性产品:

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MHC I MHC II

查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SBP-5147 is an orally active ULK1/ULK2 inhibitor, with an IC50 of 2 nM against ULK1 and an IC50 of 53 nM against ULK2. SBP-5147 inhibits the phosphorylation of Beclin-1 and Vps34, reduces autophagy flux, downregulates the expression of ATG13 and ATG101, upregulates the expression of MHC-I, induces caspase-dependent apoptosis, and decreases the viability of non-small cell lung cancer cells. SBP-5147 is applicable to research related to non-small cell lung cancer[1][2].

IC50 & Target

ULK2

53 nM (IC50)

ULK1

2 nM (IC50)

体外研究
(In Vitro)

SBP-5147 (Compound 5) 在 NanoBRET 实验中可与 HEK293T 细胞内的 ULK1 结合，其 IC50 为 47 nM[1]。
SBP-5147 (10 μM; 1 h) 在转染的 HEK293T 细胞中可将 ULK1 下游底物 Beclin-1 (Ser15) 和 Vps34 (Ser249) 的磷酸化水平抑制约 80%[1]。
SBP-5147 (10 μM; 18 h) 可抑制营养饥饿状态下 A549 细胞中的自噬流，减少高自噬流细胞群体[1]。
SBP-5147 (72 h) 可降低 A549、HCC827、H1373、H1975 细胞的活力，IC50 分别为91、49、40、35 nM[1]。
SBP-5147 (1 μM; 8-24 h) 可诱导 A549 细胞发生 caspase 依赖性凋亡[1]。
SBP-5147 (15-30 nM; 72 h) 可显著上调 H1373、HCC827 和 A549 细胞中总 MHC-I 蛋白的表达[1]。
SBP-5147 可在生化 ADP-Glo 实验中强效抑制 ULK1 激酶活性 (IC50 = 2 nM) 和 ULK2 激酶活性 (IC50 = 53 nM)[2]。
SBP-5147 (48 h) 可诱导 A549 非小细胞肺癌 (NSCLC) 细胞中 ATG13 降解，IC50 为 4.5 μM[2]。

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

SBP-5147 相关抗体:

Western Blot Analysis[1]

Cell Line: HEK293T cells transfected with Myc-tagged WT ULK1 and Flag-tagged Beclin-1 or Vps34
Concentration: 10 μM
Incubation Time: 1 h
Result: Inhibited phosphorylation of Beclin-1 at Ser15 by roughly 80% relative to DMSO-treated cells.
Inhibited phosphorylation of Vps34 at Ser249 by roughly 80% relative to DMSO-treated cells.

Cell Autophagy Assay[1]

Cell Line: A549 NSCLC cells expressing mCherry-GFP-LC3 reporter
Concentration: 10 μM
Incubation Time: 18 h
Result: Reduced the percentage of cells exhibiting high autophagic flux, shifting populations to intermediate and low flux relative to EBSS-only treated cells.

Apoptosis Analysis[1]

Cell Line: A549, H1975 NSCLC cells
Concentration: 1 μM
Incubation Time: 24 h (imaging); 8 h (Western blot)
Result: Induced caspase-dependent apoptotic cell death in A549 cells, with cell death abrogated by Emricasan and partially inhibited by zVAD-fmk.
Induced cleavage of PARP and caspase-3, blocked by apoptosis inhibitors.

Western Blot Analysis[1]

Cell Line: H1373, HCC827, A549, H1975 NSCLC cell lines
Concentration: 15 nM, 30 nM
Incubation Time: 72 h
Result: Significantly increased total MHC-I protein expression at 30 nM in H1373, HCC827, and A549 cells.
Increased expression in H1373 and HCC827 cells also at 15 nM.
Had no significant effect on H1975 cells.
药代动力学
(Parmacokinetics)
Species Dose Route Tmax Cmax T1/2
Mice[1] 10 mg/kg p.o. 0.25 h 664 nM 2.5 h
体内研究
(In Vivo)

SBP-5147 (10 mg/kg；灌胃；单次给药) 可使 C57BL/6J 小鼠肝脏和肺组织中的 ATG13 与 ATG101 蛋白水平降低，表明其可持久地靶向抑制自噬[1]。

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

Animal Model: C57BL/6J (8-week-old female)[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose
Result: Caused progressive, significant decrease in ATG13 and ATG101 protein levels in liver and lung tissues.
Maintained significantly reduced ATG13 and ATG101 levels at 24 hours postdosing (plasma SBP-5147 almost completely eliminated) compared to vehicle-treated samples.
Confirmed statistically significant reductions in both proteins at 4, 8, and 24 hours postdosing relative to vehicle controls.
分子量

349.35

Formula

C17H18F3N5
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.
纯度 & 产品资料
参考文献

SBP-5147 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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.

Keywords:

SBP-51471884222-37-0SBP5147SBP 5147ULKBeclin1AutophagyMHCCaspaseApoptosisUnc-51 like kinaseAtg6Major Histocompatibility ComplexULK1/ULK2 inhibitorHEK293T cellsA549 cellsHCC827 cellsH1373 cellsH1975 cellsC57BL/6J miceautophagyapoptosisInhibitorinhibitorinhibit

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