2. Metabolic Enzyme/Protease Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. Aminoacyl-tRNA Synthetase Apoptosis Caspase PARP c-Myc
  4. NCP26

NCP26 是一种 ATP 竞争性的 ProRS 抑制剂 (在无 Proline 条件下 KD 为 271 nM，在 100 μM Proline 存在下其 KD 达 0.35 nM)。NCP26 可激活 AAR，诱导 G0/G1 期阻滞、细胞凋亡 (Apoptosis)、Caspase 切割、PARP 切割。NCP26 可下调 MYC、TCF3 及 CCND1。NCP26 可抑制多发性骨髓瘤细胞生长。NCP26 可用于多发性骨髓瘤的研究。

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NCP26

NCP26 Chemical Structure

CAS No. : 2396683-89-7

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NCP26 相关抗体

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NCP26 is an ATP-competitive ProRS inhibitor (with a KD of 271 nM in the absence of proline, and a KD of 0.35 nM in the presence of 100 μM proline). NCP26 activates AAR, induces G0/G1 phase arrest, Apoptosis, Caspase cleavage, and PARP cleavage. NCP26 downregulates MYC, TCF3, and CCND1. NCP26 inhibits the growth of multiple myeloma cells. NCP26 can be used for the research of multiple myeloma[1][2].

IC50 & Target[1]

Caspase 8

 

Caspase 9

 

Caspase 3

 

体外研究
(In Vitro)

NCP26 是重组人源 ProRS 的 ATP 竞争性抑制剂，在 100 μM proline 存在下其结合亲和力提升超过 750 倍，KD 达 0.35 nM[1]。
NCP26 (0.5 μM; 48 h) 在 0 至 20 mM 脯氨酸浓度范围内对 AMO1 和 RPMI 8226 多发性骨髓瘤 (MM) 细胞保持抗增殖活性，在高脯氨酸水平下其效力未出现降低[1]。
NCP26 (0.01-10 μM; 96 h) 对 AMO1 多发性骨髓瘤 (MM) 细胞的效力比健康供者外周血单个核细胞 (PBMCs) 高 10 倍，前者处理 96 h 后的 EC50 为 0.1 μM，后者处理 96 h 后的 EC50 约为 1 μM[1]。
NCP26 可强效抑制大多数多发性骨髓瘤 (MM) 细胞系的生长，其 EC50 值范围为 135 nM 至 1.1 μM[1]。
NCP26 (0.5 μM; 6-48 h) 可在 AMO1 和 RPMI 8226 多发性骨髓瘤 (MM) 细胞中诱导 G0/G1 期细胞周期阻滞及半胱天冬酶依赖性细胞凋亡[1]。

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

NCP26 相关抗体:

Cell Cycle Analysis[1]

Cell Line: AMO1, RPMI 8226 MM cell lines
Concentration: 0.5 μM
Incubation Time: 6 h, 24 h, 48 h
Result: Induced G0/G1 cell cycle arrest in both cell lines at 6 h, with enhanced arrest observed at 24 h.
Induced apoptotic cell death, evidenced by increased Annexin-V+ cells, sub-G1 populations, and mitochondrial damage.
Induced time- and dose-dependent cleavage of caspases-3, -8, -9, and PARP.

Western Blot Analysis[1]

Cell Line: AMO1, RPMI 8226 MM cell lines
Concentration: 0-1 μM
Incubation Time: 6 h
Result: Dose-dependently reduced protein levels of MYC, PIM2, CCND1, and TCF3 in both cell lines.
Mirrored the effects of EPRS shRNA knockdown on MYC, PIM2, CCND1, and TCF3 protein levels.
体内研究
(In Vivo)

NCP26 (2.5-10 mg/kg；腹腔注射；每日 1 次；连续 21 天) 可显著抑制荷 AMO1 异种移植物的 CB17 SCID 小鼠的多发性骨髓瘤肿瘤生长，并延长其总生存期，且未导致显著的体重下降[1]。
NCP26 (10 mg/kg；每日一次) 可显著抑制 AMO1 异种移植小鼠模型中的多发性骨髓瘤肿瘤生长并延长宿主生存期，且不会导致体重下降[2]。

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

Animal Model: CB17 SCID (5-week-old female, subcutaneously inoculated with AMO1 cells)[1]
Dosage: 2.5 mg/kg; 10 mg/kg
Administration: i.p.; once daily; 21 days
Result: Significantly inhibited AMO1 tumour growth compared to vehicle control (control vs.
2.5 mg/kg, P = 0.01; control vs.
10 mg/kg, P < 0.001).
Resulted in greater tumour growth inhibition at 10 mg/kg dose than 2.5 mg/kg dose.
Caused no significant body weight loss in either treatment cohort.
Significantly prolonged overall survival compared to vehicle control (control vs.
2.5 mg/kg, P = 0.01; control vs.
10 mg/kg, P < 0.001).
Downregulated MYC, CCND1, and TCF3, and induced p-GCN2 and DDIT3 in treated tumours.
分子量

365.44

Formula

C20H23N5O2
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

NCP26 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

NCP262396683-89-7NCP 26NCP-26Aminoacyl-tRNA SynthetaseApoptosisCaspasePARPc-MyctRNA Synthetase, aaRSpoly ADP ribose polymerase MycISRAMO1ProRSATF4GCN2EPRSeIF2αDDIT3AARmultiple myelomaInhibitorinhibitorinhibit

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