CC-930
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.
CC-930是一种强效的和选择性的JNK1/JNK2/JNK3抑制剂,IC50值分别为61 nM、7 nM 和6 nM。[1]
JNK(c-Jun N末端激酶)属于原始鉴定的激酶。JNKs与c-Jun结合,然后磷酸化位于其转录激活域的Ser-63和Ser-73。JNKs属于MAPK家族,其包含十种由JNK1、JNK2和JNK3三种基因编码的亚型。JNKs是46 kD或55 kD蛋白,在应激刺激(如热休克、细胞因子和渗透性休克)中起重要作用。JNKs对细胞凋亡途径和T细胞分化也有应答,其通过位于激酶域Thr-Pro-Tyr基序中的苏氨酸和酪氨酸残基的双磷酸化而激活。JNKs修饰在细胞核或线粒体中起作用的许多蛋白的活性。JNKs激活下游分子,包括p53、c-jun、ELK1、Smad4和HSF1,并调节若干重要的细胞功能,如细胞生长、存活、分化和凋亡。[ 2 ]
在针对所有JNK亚型的底物c-Jun磷酸化中,CC-930与ATP动力学竞争,Ki值为44±3 nm(JNK1)、6.2±0.6 nm,作用于JNK3的IC50值为5 nm。在3 (M 时,EGFR是被抑制超过50%的唯一非MAP激酶。在10 M时,CC-930对22个不同的非激酶酶类抑制不超过50%。 [ 1 ] 1 μM的 CC-930减少TGF β刺激的c-Jun的磷酸化,相当于成纤维细胞的临床相关浓度[ 3 ]。CC-930在TSK1模型中显示出强效的抗纤维化作用。CC-930剂量依赖性地减少TSK1小鼠皮下增厚达85±4%。[ 3 ] CC-930对糖尿病自发性高血压大鼠(SHR)肾脏肥大、高血压、足细胞丢失、肾小球纤维化无影响。然而,CC-930减少糖尿病肾脏中CCL2 mRNA的水平[ 4 ]。
参考文献:
[1]. Plantevin Krenitsky V, Nadolny L, Delgado M, Ayala L, Clareen SS, Hilgraf R, Albers R, Hegde S, D'Sidocky N, Sapienza J et al: Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor. Bioorg Med Chem Lett, 22(3):1433-1438.
[2]. Waetzig V, Herdegen T: Context-specific inhibition of JNKs: overcoming the dilemma of protection and damage. Trends Pharmacol Sci 2005, 26(9):455-461.
[3]. Reich N, Tomcik M, Zerr P, Lang V, Dees C, Avouac J, Palumbo K, Horn A, Akhmetshina A, Beyer C et al: Jun N-terminal kinase as a potential molecular target for prevention and treatment of dermal fibrosis. Ann Rheum Dis, 71(5):737-745.
[4]. Lim AK, Ma FY, Nikolic-Paterson DJ, Ozols E, Young MJ, Bennett BL, Friedman GC, Tesch GH: Evaluation of JNK blockade as an early intervention treatment for type 1 diabetic nephropathy in hypertensive rats. Am J Nephrol, 34(4):337-346.
Storage | Store at -20°C |
M.Wt | 448.44 |
Cas No. | 899805-25-5 |
Formula | C21H23F3N6O2 |
Synonyms | Tanzisertib;CC930;CC 930 |
Solubility | Soluble in DMSO |
Chemical Name | (1S,4r)-4-((9-((S)-tetrahydrofuran-3-yl)-8-((2,4,6-trifluorophenyl)amino)-9H-purin-2-yl)amino)cyclohexan-1-ol |
SDF | Download SDF |
Canonical SMILES | O[C@@H]1CC[C@@H](NC2=NC=C3C(N([C@@H]4COCC4)C(NC(C(F)=C5)=C(F)C=C5F)=N3)=N2)CC1 |
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。 |
质量控制和MSDS
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