ERCC1-XPF-IN-2是一种高效的 ERCC1-XPF 核酸内切酶抑制剂,IC50 值为 0.6 μM。该化合物在核苷酸切除修复、顺铂增强疗效及 γH2AX 测定中表现出活性,适用于癌症和 DNA 损伤修复的研究。
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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 |
+
BLMfull-length, IC50: 2.98 μM BLM636-1298, IC50: 0.97 μM |
99%+ | |||||||||||||||||
RK-33 | ✔ | 98% | |||||||||||||||||
Brr2-IN-3 | ✔ | 99%+ | |||||||||||||||||
Phen-DC3 Trifluoromethanesulfonate | ✔ | 95% | |||||||||||||||||
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, IC50: 46.11 nM Leucyl-tRNA synthetase, Kd: 42.1 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。 |
描述 | ERCC1-XPF-IN-2 is an effective ERCC1-XPF endonuclease inhibitor, exhibiting an IC50 of 0.6 µM. It is active in nucleotide excision repair, enhances cisplatin efficacy, and is involved in γH2AX assays[1]. |
体外研究 | ERCC1-XPF-IN-2, at concentrations between 0 and 100 µM, displays activities for FEN-1 and DNase I with IC50 values exceeding 100 µM for both[1]. ERCC1-XPF-IN-2 exhibits slow binding kinetics with a dissociation constant (Kd) of approximately 30 µM[1]. ERCC1-XPF-IN-2 is non-toxic to Hep-G2 cells at 10 µM and has short microsomal half-lives in mice and humans, with t1/2 values of 23 minutes and 28 minutes, respectively. Additionally, ERCC1-XPF-IN-2 (0-60 µM; 24 h) inhibits nucleotide excision repair (NER) in A375 cells with an IC50 of 15.6 µM[1]. ERCC1-XPF-IN-2 enhances cisplatin efficacy without causing toxicity at concentrations ranging from 0 to 60 µM[1]. ERCC1-XPF-IN-2 (10 µM; 6h) delays DNA repair, as indicated by an increase in the number of γH2AX foci per cell[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.07mL 0.61mL 0.31mL |
15.33mL 3.07mL 1.53mL |
30.66mL 6.13mL 3.07mL |
CAS号 | 1808986-37-9 |
分子式 | C15H13Cl2NO3 |
分子量 | 326.17 |
SMILES Code | O=C(NCC1=CC=C(O)C(O)=C1)CC2=CC=C(Cl)C=C2Cl |
MDL No. | MFCD34676435 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, sealed in dry, 2-8°C |
溶解方案 |
DMSO: 250 mg/mL(766.46 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |