ML-323
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50值：ML-323是一种高效的和选择性的USP1-UAF1抑制剂，IC50值为76 nM。
ML-323是一种高选择性的和对人类细胞具有低细胞毒性的USP1-UAF1抑制剂[1]。USP1-UAF1与DNA损伤反应密切相关，且最近将其作为抗肿瘤治疗中克服耐药性的策略[1]。
体外实验：H596细胞研究表明，ML-323通过抑制USP1–UAF1活性，阻止PCNA和FANCD2的去泛素化。据报道，ML-323强效抑制USP1-UAF1，在泛素-罗丹明(Ub-Rho)试验和正交凝胶实验中的IC50值分别为76 nM和174 nM。此外，通过靶向两种主要的DNA损伤反应信号通路TLS和FA，ML-323增加NSCLC H596细胞和骨肉瘤U2OS细胞中的顺铂毒性。而且，该药剂对人DUBs、deSUMOylase、deneddylase及不相关蛋白酶具有高选择性[1]。
体内实验：到目前为止，还未进行体内研究。
临床试验：到目前为止，还未进行临床试验。
参考文献：
[1]Liang Q, Dexheimer TS, Zhang P, Rosenthal AS, Villamil MA, You C, Zhang Q, Chen J, Ott CA, Sun H, Luci DK, Yuan B, Simeonov A, Jadhav A, Xiao H, Wang Y, Maloney DJ and Zhuang Z. A selective USP1-UAF1 inhibitor links deubiquitination to DNA damage responses. Nat Chem Biol. 2014 April; 10(4): 298–304.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 384.48 |
| Cas No. | 1572414-83-5 |
| Formula | C23H24N6 |
| Solubility | ≥12.34 mg/mL in EtOH; ≥15.05 mg/mL in DMSO; ≥2.25 mg/mL in H2O |
| Chemical Name | (E)-1-(4-(1H-1,2,3-triazol-1-yl)phenyl)-N-(2-(2-isopropylphenyl)-5-methylpyrimidin-4(3H)-ylidene)methanamine |
| SDF | Download SDF |
| Canonical SMILES | CC(C1=CC=CC=C1C2=NC=C(/C(N2)=N\CC3=CC=C(N4C=CN=N4)C=C3)C)C |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Description | ML323 is a highly potent and selective inhibitor of USP1-UAF1 with IC50 value of 76 nM. | |||||
| Targets | USP1-UAF1 | |||||
| IC50 | 76 nM | |||||
化学结构
