BML-277
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.
BML-277是新型的\有效的和高选择性的Chk2抑制剂,其IC50值为15 ± 6.9 nM[1].
BML-277对Chk2具有ATP竞争性抑制作用,其Ki值为37 nM.BML-277也是Chk2抑制剂,IC50值为15 ± 6.9 nM,并从辐射诱导的细胞凋亡中呈浓度依赖性地解救各种T细胞,其EC50值为3 ~ 7.6 μM.Chk2的ATP Km值为99 μM,胞内ATP浓度为10 mM.此外,BML-277通过对接Chk2 ATP结合位点的同源性模型来发挥其抑制作用[1].
参考文献:
[1]Arienti KL1, Brunmark A, Axe FU, McClure K, Lee A, Blevitt J, Neff DK, Huang L, Crawford S, Pandit CR, Karlsson L, Breitenbucher JG. Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. J Med Chem. 2005 Mar 24;48(6):1873-85.
- 1. Zheng K, Ma J, et al. "Sulforaphane Inhibits Autophagy and Induces Exosome-Mediated Paracrine Senescence via Regulating mTOR/TFE3." Mol Nutr Food Res. 2020;e1901231. PMID:32476238
- 2. Sarkar R, Patra U, et al. "Rotavirus activates a noncanonical ATM-Chk2 branch of DNA damage response during infection to positively regulate viroplasm dynamics." Cell Microbiol. 2019 Dec 17:e13149. PMID:31845505
- 3. N. Sanjib Banerjee, Dianne Moore, et al. "Targeting DNA Damage Response as a Strategy to Treat HPV Infections." Int. J. Mol. Sci. 2019, 20(21), 5455.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 363.8 |
Cas No. | 516480-79-8 |
Formula | C20H14ClN3O2 |
Solubility | insoluble in H2O; ≥18.2 mg/mL in DMSO; ≥2.72 mg/mL in EtOH with ultrasonic |
Chemical Name | 2-[4-(4-chlorophenoxy)phenyl]-3H-benzimidazole-5-carboxamide |
SDF | Download SDF |
Canonical SMILES | C1=CC(=CC=C1C2=NC3=C(N2)C=C(C=C3)C(=O)N)OC4=CC=C(C=C4)Cl |
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。 |
激酶实验 [1]: | |
抑制纯化的chk2 |
将BML-277,重组全长chk2:5 nM重组人类Chk2,50 mM HEPES (pH 7.4),100 mM NaCl,10 mM MgCl2,25 μM合成多肽底物(生物素-SSLYRSPSMPENLNRPR),1 μM ATP,50 μCi/mL [γ-33P] ATP以及蛋白酶抑制剂混合物。将上述混合物置于37 °C下孵育3小时。多肽底物与琼脂糖珠上的链霉亲和素结合。使用0.1% Tween-20(溶于磷酸盐缓冲液中,pH 7.4)反复洗涤琼脂糖珠。通过闪烁计数器,测定与底物多肽结合的放射性磷酸盐量,从而评估在不同BML-277浓度下的酶活性。在动力学实验中,ATP浓度发生变化,未标记ATP与[γ-33P]标记ATP的比例保持不变。加入50 mM冰冻ATP,在不同的时间点终止反应。将样品置于冰上,用于后续试验。 |
细胞实验 [1]: | |
细胞系 |
人类T细胞 |
制备方法 |
在DMSO中的溶解度大于18.2 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
反应条件 |
25小时 |
实验结果 |
BML-277呈浓度依赖性地有效减少辐射诱导的T细胞凋亡,其EC50值范围为3 ~ 7.6 μM。 |
References: [1]. Arienti KL1, Brunmark A, Axe FU, McClure K, Lee A, Blevitt J, Neff DK, Huang L, Crawford S, Pandit CR, Karlsson L, Breitenbucher JG. Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles. J Med Chem. 2005 Mar 24;48(6):1873-85. |
质量控制和MSDS
- 批次: