GlpBio

COH29

目录号: GC19110纯度: >98.00%同义词: RNR Inhibitor COH29
COH29是一种强效的核糖核苷酸还原酶（RNR）抑制剂，对RNR的α和β亚基的IC50为16μM。
COH29
Cas No.: 1190932-38-7
规格价格库存数量操作
5mg¥1,610.00现货
1
10mg¥2,380.00现货
1
10mM (in 1mL DMSO)¥1,771.00现货
1
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产品描述 Description

COH29 is a potent ribonucleotide reductase (RNR) inhibitor with an IC50 of 16μM against the α and β subunits of RNR[1]. RNR is an important enzyme that converts ribonucleotides into deoxyribonucleotides and plays a key role in DNA synthesis and repair[2]. COH29 is usually used in cancer research[3].

In vitro, COH29 (10μM; 72h) induced significant DNA damage and cell cycle arrest with an IC50 of 7.25μM in HCC1937 cells[4]. COH29 (10μM; 24h) significantly enhanced the chemosensitivity of estrogen receptor-negative MDA-MB-231 cells to doxorubicin[5].

In vivo, COH29 (400mg/kg/day; p.o; 21 days) significantly suppressed tumor growth and prolonged survival in an atypical teratoid/rhabdoid tumor (ATRT) orthotopic mouse model[6]. COH29 (50mg/kg and 100mg/kg/day; p.o.; 24 days) significantly reduced tumor volume and weight in KYSE30 and KYSE450 cell line-derived xenograft (CDX) mice models[7].

References:
[1] Zhou B, Su L, Hu S, et al. A small-molecule blocking ribonucleotide reductase holoenzyme formation inhibits cancer cell growth and overcomes drug resistance. Cancer Res. 2013;73(21):6484-6493.
[2] Shao J, Liu X, Zhu L, Yen Y. Targeting ribonucleotide reductase for cancer therapy. Expert Opin Ther Targets. 2013;17(12):1423-1437.
[3] Bothou C, Sharma A, Oo A, et al. Novel Insights into the Molecular Regulation of Ribonucleotide Reductase in Adrenocortical Carcinoma Treatment. Cancers (Basel). 2021;13(16):4200.
[4] Chen MC, Zhou B, Zhang K, et al. The Novel Ribonucleotide Reductase Inhibitor COH29 Inhibits DNA Repair In Vitro. Mol Pharmacol. 2015;87(6):996-1005.
[5] Zhang H, Liu X, Warden CD, et al. Prognostic and therapeutic significance of ribonucleotide reductase small subunit M2 in estrogen-negative breast cancers. BMC Cancer. 2014;14:664.
[6] Giang LH, Wu KS, Lee WC, et al. Targeting of RRM2 suppresses DNA damage response and activates apoptosis in atypical teratoid rhabdoid tumor. J Exp Clin Cancer Res. 2023;42(1):346.
[7] Li W, Shi Y, Chen X, et al. TCPTP inhibition as a novel therapeutic strategy for esophageal squamous cell carcinoma: discovery and efficacy of COH29. Biochem Pharmacol. 2025;239:116997.

COH29是一种强效的核糖核苷酸还原酶（RNR）抑制剂，对RNR的α和β亚基的IC50为16μM[1]。RNR是一种将核糖核苷酸转化为脱氧核糖核苷酸的重要酶，在DNA合成和修复中发挥关键作用[2]。COH29通常用于癌症研究[3]。

体外实验中，COH29（10μM；72小时）在HCC1937细胞中显著诱导DNA损伤和细胞周期阻滞，IC50为7.25μM[4]。COH29（10μM；24小时）显著增强了雌激素受体阴性MDA-MB-231细胞对多柔比星的化疗敏感性[5]。

体内实验中，COH29（400mg/kg/天；口服；21天）显著抑制了ATRT（非典型畸胎样/横纹肌样瘤) 原位小鼠模型中的肿瘤生长，并延长了生存期[6]。COH29（50mg/kg和100mg/kg/天；口服；24天）显著减少了KYSE30和KYSE450细胞系衍生的异种移植（CDX）小鼠模型中的肿瘤体积和重量[7]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

HCC1937 cells

Preparation Method

HCC1937 cells were maintained in RPMI 1640 medium with 10% fetal bovine serum, 2mM glutamine, and 100U of penicillin and 100mg of streptomycin per milliliter of medium at 37°C in 5% CO2. Reporter cell lines for GFP-based DNA damage repair assays were established by stable transfection with the pimEJ5GFP reporter plasmid for non-homologous end joining (NHEJ) and the pHPRT-DRGFP reporter plasmid for homologous recombination (HR), respectively, and selected with 0.3mg/ml puromycin. The resultant HCC1937-EJ5GFP cells were first pre-treated with COH29 (10μM) for 24 hours and then transiently transfected with a predetermined mixture of pCBA-Scel plasmid to express I-Scel endonuclease and a plasmid to express DsRed (red fluorescent protein) protein, which served as the control for transfection efficiency. After incubation with COH29 for another 48 hours, 5×105 cells per transfection were analyzed by fluorescence-activated cell sorting to count total GFP and DsRed protein positive cells. Each assay was performed three times, and data were presented as the ratio of GFP-positive to DsRed-positive cells among whole cells.

Reaction Conditions

10μM; 72h

Applications

COH29 induced significant DNA damage in HCC1937 cells.
Animal experiment [2]:

Animal models

NOD/SCID mice

Preparation Method

The orthotopic ATRT xenograft model was performed for this experiment. In brief, Re1-P6 cells were suspended in Dulbecco’s Modified Eagle Medium (DMEM) and MatrigelTM with a ratio of 2:1 (4×105 cells/10μL) and injected into the right cerebral hemisphere of 6-8 week-old NOD/SCID (non-obese diabetic/severe combined immunodeficiency) mice. Tumor formation confirmed by magnetic resonance imaging (MRI) was performed at day 20 after injection (pre-treatment). From day 21, the mice with tumor formation confirmed by MRI were randomly divided into control group (treated with Kolliphor HS15 in saline; n=8) and COH29 treatment group (treated with COH29 (400mg/kg) ) by oral gavage every day in 3 weeks; n=8). The post-treatment brain MRI was obtained at day 28. Mice were monitored the irreversible neurological deficits and body weight daily. Tumor volumes were calculated based on post-contrast T1-weighted sequences using Image J.

Dosage form

400mg/kg/day; p.o; 21 days

Applications

COH29 significantly suppressed tumor growth and prolonged survival in an ATRT orthotopic mouse model.

References:
[1] Chen MC, Zhou B, Zhang K, et al. The Novel Ribonucleotide Reductase Inhibitor COH29 Inhibits DNA Repair In Vitro. Mol Pharmacol. 2015;87(6):996-1005.
[2] Giang LH, Wu KS, Lee WC, et al. Targeting of RRM2 suppresses DNA damage response and activates apoptosis in atypical teratoid rhabdoid tumor. J Exp Clin Cancer Res. 2023;42(1):346.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
1190932-38-7
同义词
RNR Inhibitor COH29
SMILES
O=C(NC1=NC(C2=CC=C(O)C(O)=C2)=C(C3=CC=CC=C3)S1)C4=CC=C(O)C(O)=C4
分子式
C22H16N2O5S
分子量
420.44 g/mol
溶解性
DMSO : ≥ 31 mg/mL (73.73 mM)
保存条件
Store at -20°C
General tips
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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol