hnRNPK-IN-1

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hnRNPK-IN-1  纯度: 97.11%

hnRNPK-IN-1 是一种异质核糖核蛋白 K (hnRNPK) 结合配体，用 SPR 和 MST 测量的 Kd 值分别为 4.6 μM 和 2.6 μM。hnRNPK-IN-1 通过破坏 hnRNPK 和 c-myc 启动子的结合来抑制 c-myc 转录。hnRNPK-IN-1诱导 Hela 细胞凋亡 (apoptosis)，并具有很强的抗肿瘤活性。

hnRNPK-IN-1

hnRNPK-IN-1 Chemical Structure

CAS No. : 2313528-04-8

规格 价格 是否有货 数量
5 mg ￥5500 In-stock
10 mg ￥8800 In-stock
25 mg ￥18000 In-stock
50 mg ￥30000 In-stock
100 mg ￥46000 In-stock
200 mg   询价  
500 mg   询价  

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hnRNPK-IN-1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Glutamine Metabolism Compound Library
  • Transcription Factor Targeted Library

生物活性

hnRNPK-IN-1 is a heterogeneous nuclear ribonucleoprotein K (hnRNPK) binding ligand with Kd values of 4.6 μM and 2.6 μM measured with SPR and MST, respectively. hnRNPK-IN-1 inhibits c-myc transcription by disrupting the binding of hnRNPK and c-myc promoter. hnRNPK-IN-1 induces Hela cells apoptosis and has strongly anti-tumor activities[1].

IC50 & Target

Kd: 4.6 μM (hnRNPK; SPR assay) and 2.6 μM (hnRNPK; MST assay)[1]
体外研究
(In Vitro)

hnRNPK-IN-1 (Compound 25; 1.25-5 μM; 24 hours) treatment induces Hela cells apoptosis could be due to its repression of cmyc transcription[1].
hnRNPK-IN-1 (1.25-5 μM; 48 hours) treatment down-regulates c-myc gene transcription and expression in Hela cells in a dose-dependent manner[1].
hnRNPK-IN-1 shows a selective anti-proliferative effect on human cancer cell lines (Siha, A549, Hela, U2OS, A375, HuH7 and HEK293 cells) with IC50 values ranged from 1.36 to 3.59 μM[1].
hnRNPK-IN-1 could selectively bind to hnRNP K without significant interaction with c-myc promoter DNA. The binding of hnRNPK-IN-1 to hnRNP K could disrupt the interaction between hnRNP K and c-myc promoter DNA in vitro and in cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: Hela cells
Concentration: 1.25 μM, 2.5 μM, 5 μM
Incubation Time: 24 hours
Result: Induced Hela cells apoptosis and apoptosis-related protein expressions.

RT-PCR[1]

Cell Line: Hela cells
Concentration: 1.25 μM, 2.5 μM, 5 μM
Incubation Time: 48 hours
Result: Caused a reduction of c-myc mRNA in a dose-dependent manner in Hela cells.

Western Blot Analysis[1]

Cell Line: Hela cells
Concentration: 1.25 μM, 2.5 μM, 5 μM
Incubation Time: 48 hours
Result: The expression levels of c-MYC also decreased in a dose-dependent manner.

体内研究
(In Vivo)

hnRNPK-IN-1 (Compound 25; 6.7-20 mg/kg; i.p.; once a day; for three weeks) exhibits good tumor growth inhibition in a Hela xenograft tumor model[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c female nude mice (five weeks old) bearing Hela cells[1]
Dosage: 6.7 mg/kg, 20 mg/kg
Administration: Intraperitoneal injection; once a day; for three weeks
Result: Inhibited tumor growth in a Hela cervical xenograft.

分子量

419.43

Formula

C23H21N3O5
CAS 号

2313528-04-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 5 mg/mL (11.92 mM; ultrasonic and warming and heat to 80°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3842 mL 11.9209 mL 23.8419 mL
5 mM 0.4768 mL 2.3842 mL 4.7684 mL
10 mM 0.2384 mL 1.1921 mL 2.3842 mL

*

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。-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。
参考文献

  • [1]. Bing Shu, et al. Syntheses and evaluation of new Quinoline derivatives for inhibition of hnRNP K in regulating oncogene c-myc transcription. Bioorg Chem. 2019 Apr;85:1-17.

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