TH287 | MTH1 Inhibitor | AmBeed-信号通路专用抑制剂

TH287 {[allProObj[0].p_purity_real_show]}

货号：A600790

TH287是一种选择性的MTH1抑制剂，IC50值为0.8 nM。

TH287 化学结构
CAS号：1609960-30-6

TH287 3D分子结构
CAS号：1609960-30-6

规格	价格	会员价	库存	数量
{[ item.pr_size ]} {[ size_append(item.pr_size_append, item.pr_am, item.pr_size) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]}	现货	1周咨询	- +

购物车0 收藏询单

sales@ambeed.cn tech@ambeed.cn 400-920-2911 产品手册产品订购技术咨询
快速发货顺丰冷链运输，1-2 天到达

品质保证

技术支持

免费溶解

TH287 质控信息

DNA 亚型比较

MTH1 亚型比较

产品名称	DNA synthesis ↓ ↑	helicase ↓ ↑	RdRp ↓ ↑	ribonucleotide reductase ↓ ↑	tRNA synthetase ↓ ↑	YB-1 ↓ ↑	其他靶点	纯度
Fexinidazole	✔							98%
Daptomycin	✔							98%
Blasticidin S·HCl	✔							98%
Metronidazole	✔							98%
Daunorubicin HCl	+++ DNA synthesis, Ki: 20 nM							98%
Triglycidyl isocyanurate	✔						p53	98+%
Nedaplatin	✔							99%+
Oxolinic acid	✔							98+%
Bendamustine	✔							98+%
Trifluridine	✔							98%
Robinetin	✔							99%+
Carboplatin	✔							99%
Cidofovir	✔							99%
Cisplatin	✔							99%
Cytarabine	++++ DNA synthesis, IC50: 16 nM							98%
Acelarin	++++ DNA synthesis, EC50: 0.2 nM							99%+
Oxaliplatin	✔							98%
YK-4-279		✔						99%+
ML216		+ BLM^full-length, IC50: 2.98 μM BLM^636-1298, IC50: 0.97 μM						99%+
RK-33		✔						98%
Brr2-IN-3		✔						99%+
Phen-DC3 Trifluoromethanesulfonate		✔						98%
Favipiravir			✔					99%
Suramin sodium salt			++ RdRp, IC50: 0.26 μM					99%+
Clofarabine				++ Ribonucleotide reductase, IC50: 65 nM				97%
Didox				✔				98%
(E)-3-AP				✔				99%
Halofuginone					+++ prolyl-tRNA synthetase, Ki: 18.3nM			99%+
BC-LI-0186					+++ Leucyl-tRNA synthetase, Kd: 42.1 nM Leucyl-tRNA synthetase, IC50: 46.11 nM			98%
SU056						+ YB-1, IC50: 1.73 μM		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	MTH1 ↓ ↑	纯度
TH588	+++ MTH1, IC50: 5 nM	99%+
TH287	++++ MTH1, IC50: 0.8 nM	99%
(S)-Crizotinib	++ MTH1, IC50: 72 nM	98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

TH287 生物活性

靶点

MTH1

MTH1, IC50:0.8 nM

描述

The nucleotide-sanitizing enzyme MutT homolog 1 (MTH1) can hydrolyze oxidized nucleotides and is required for cancer survival. TH287 is a potent inhibitor of MTH1 with an IC50 value of 0.8 nM and causes incorporation of oxidized dNTPs in cancer cells, leading to DNA damage, cytotoxicity and therapeutic responses. TH287 at 10uM significantly induced 3.2-fold increases in apoptosis level in human non-small cell lung cancer cell line H23 but showed no affect on A549 cells. TH287 alone showed no obvious effect on the human tongue squamous cell carcinoma cell line CAL27 cancer suppression in the xenograft model.

作用机制

TH287 inhibits MTH1 by occupying the recognition site of 8-oxodGTP in MTH1.

TH287 细胞实验

Cell Line PC3 H1563 A549 H23 U2OS Glioblastoma cells (U251MG) MCF-7 cells U2OS cells HT1080 cells MRC-5 (normal lung fibroblasts) A549 (wildtype p53) H522 (p53-mutated) H23 (p53-mutated) HeLa cells	Concentration	Treated Time	Description	References
PC3	20 μmol/L	1 hour	Evaluate the inhibitory effect of TH287 on 8-oxodGTPase activity	Mol Cancer Ther. 2020 Feb;19(2):432-446.
H1563	20 μmol/L	1 hour	Evaluate the inhibitory effect of TH287 on 8-oxodGTPase activity	Mol Cancer Ther. 2020 Feb;19(2):432-446.
A549	20 μmol/L	1 hour	Evaluate the inhibitory effect of TH287 on 8-oxodGTPase activity	Mol Cancer Ther. 2020 Feb;19(2):432-446.
H23	20 μmol/L	1 hour	Evaluate the inhibitory effect of TH287 on 8-oxodGTPase activity	Mol Cancer Ther. 2020 Feb;19(2):432-446.
U2OS	20 μmol/L	1 hour	Evaluate the inhibitory effect of TH287 on 8-oxodGTPase activity	Mol Cancer Ther. 2020 Feb;19(2):432-446.
Glioblastoma cells (U251MG)	0.5–15 nM	30 minutes	Evaluate the binding affinity of [3H]TH287 to MTH1, showing Kd of 1.97±0.18 nM and Bmax of 2676±122 fmol/mg protein.	Int J Mol Sci. 2020 Nov 23;21(22):8860.
MCF-7 cells	10 μM	24 hours	Induced M arrest and mitochondrial oxidative stress	Oncogene. 2022 Jan;41(3):427-443.
U2OS cells	10 μM	24 hours	Induced M arrest and mitochondrial oxidative stress	Oncogene. 2022 Jan;41(3):427-443.
HT1080 cells	10 μM	24 hours	Induced M arrest and mitochondrial oxidative stress	Oncogene. 2022 Jan;41(3):427-443.
MRC-5 (normal lung fibroblasts)	10 μM	24 hours	TH287 did not significantly induce apoptosis in MRC-5 cells	2018 Apr 16;18(1):423. doi: 10.1186/s12885-018-4332-7.
A549 (wildtype p53)	10 μM	24 hours	TH287 did not significantly induce apoptosis in A549 cells	2018 Apr 16;18(1):423. doi: 10.1186/s12885-018-4332-7.
H522 (p53-mutated)	10 μM	24 hours	TH287 induced apoptosis in H522 cells but did not significantly increase oxidative DNA damage levels	2018 Apr 16;18(1):423. doi: 10.1186/s12885-018-4332-7.
H23 (p53-mutated)	10 μM	24 hours	TH287 induced apoptosis in H23 cells and significantly increased oxidative DNA damage levels	2018 Apr 16;18(1):423. doi: 10.1186/s12885-018-4332-7.
HeLa cells	3 μM	18 hours	Proteomic profiling to investigate the modes of action of TH287, revealing its similarity to tubulin-targeting agents rather than other MTH1 inhibitors	Sci Rep. 2016 May 23;6:26521.

Cell Line

Concentration

Treated Time

Description

References

PC3

20 μmol/L

1 hour

Evaluate the inhibitory effect of TH287 on 8-oxodGTPase activity