CAS:587841-73-4
Storage:Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:White to yellow Solid
ZCL278 是一种选择性的 Cdc42 调节剂。
Array ( [133] => Array ( [id] => 133 [name] => Inhibitors & Antagonists & Agonists [num] => [children] => Array ( [352] => Array ( [id] => 352 [name] => Protein Tyrosine Kinase/PTK ) [350] => Array ( [id] => 350 [name] => PI3K/Akt/mTOR ) [351] => Array ( [id] => 351 [name] => Endocrinology & Hormones ) [357] => Array ( [id] => 357 [name] => Angiogenesis ) [358] => Array ( [id] => 358 [name] => HIF ) [363] => Array ( [id] => 363 [name] => Immunology & Inflammation ) [364] => Array ( [id] => 364 [name] => Stem Cells ) [365] => Array ( [id] => 365 [name] => Apoptosis ) [377] => Array ( [id] => 377 [name] => Metabolic Enzyme & Protease ) [379] => Array ( [id] => 379 [name] => Autophagy ) [380] => Array ( [id] => 380 [name] => ER Stress ) [384] => Array ( [id] => 384 [name] => Cell Cycle ) [385] => Array ( [id] => 385 [name] => Cytoskeleton ) [386] => Array ( [id] => 386 [name] => DNA Damage & DNA Repai ) [387] => Array ( [id] => 387 [name] => Epigenetics ) [388] => Array ( [id] => 388 [name] => Ubiquitin ) [389] => Array ( [id] => 389 [name] => JAK/STAT ) [390] => Array ( [id] => 390 [name] => GPCR & G Protein ) [391] => Array ( [id] => 391 [name] => Neuronal Signal Pathway ) [392] => Array ( [id] => 392 [name] => MAPK ) [393] => Array ( [id] => 393 [name] => NF-κB ) [394] => Array ( [id] => 394 [name] => Membrane Transporter & Ion Channel ) [395] => Array ( [id] => 395 [name] => TGF-β/Smad ) [396] => Array ( [id] => 396 [name] => Hippo ) [775] => Array ( [id] => 775 [name] => Antibody-drug Conjugate/ADC Related ) [122] => Array ( [id] => 122 [name] => Others ) ) ) )
>
Small Molecule Compounds >
Inhibitors & Antagonists & Agonists >
Cell Cycle >
ZCL-278CAS:587841-73-4
Storage:Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:White to yellow Solid
CAS | 587841-73-4 |
English Name | ZCL-278 |
Synonyms | ZCL278;ZCL278 |
Molecular Formula | C21H19BrClN5O4S2 |
Molecular Weight | 584.89 |
Solubility | Soluble in DMSO |
Purity | ≥98% |
Appearance | White to yellow Solid |
Storage | Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC | EINECS 200-256-5 |
MDL | MFCD03623090 |
SMILES | O=C(NC(NC1=CC=C(S(=O)(NC2=NC(C)=CC(C)=N2)=O)C=C1)=S)COC3=CC=C(Br)C=C3Cl |
Target Point | Cdc42 |
Passage | Cell Cycle |
Background | ZCL278 is a selective Cdc42 modulator. |
Biological Activity | ZCL278是一种有效的,选择性的 Cdc42 调节剂,直接结合到 Cdc42,且抑制其功能,Kd 为 11.4 μM。ZCL278 可抑制基于肌动蛋白的细胞功能,包括高尔基体组织和细胞运动。[1-2] |
In Vitro | 在瑞士3T3成纤维细胞培养物中,ZCL278消除了显微镜形成并破坏了GM130对接的高尔基结构,其中两个最突出Cdc42介导的亚细胞事件。与选择性Rac抑制剂NSC23766相比,ZCL278减少了活性Cdc42的核周累积。 ZCL278在转移性前列腺癌细胞系(即PC-3)中抑制Cdc42介导的神经元分支和生长锥动力学以及基于肌动蛋白的运动和迁移,而不破坏细胞活力[1]。 ZCL278抑制Cdc42作为Junin病毒(JUNV)和水疱性口炎病毒,淋巴细胞脉络丛脑膜炎病毒和登革病毒的进入抑制剂,但不抑制无包膜脊髓灰质炎病毒。在细胞中,ZCL278显示出有效抑制化学诱导的filopodium形成,这是一种依赖于Cdc42活性的过程。剂量反应实验首先在Vero细胞中进行,而ZCL278在高达200μM的浓度下无毒,而ZCL278抑制JUNV,IC50为~14μM,通过流式细胞术测量[2]。 |
In Vivo | ZCL278使脾脏中的JUNV RNA负荷降低33倍以上,8只小鼠中的5只小鼠无法检测到JUNV RNA。这些结果与加巴喷丁治疗小鼠的结果相似,证明ZCL278可以消除JUNV复制[2]。 |
Cell Experiment | 为了确定细胞活力,将PC-3细胞与或不与Cdc42激活剂,ZCL278或NSC23766一起温育24小时。通过使用台盼蓝染料排除法,用Countess Automated Cell Counter获得活细胞和死细胞的数量。在每个实验中分配P值,并且拒绝概率水平<95%的任何零假设[1]。 |
Animal Experiment | 小鼠[2]四周龄C57BL/6小鼠静脉内注射加巴喷丁或ZCL278(100μg/ g,ip)。在处理后1小时,用27 1/2的针头针对JUNV Candid#1(1×106PFU)腹膜内接种小鼠,不超过1mL。在实验结束时,处死小鼠,用Dounce匀浆器将其脾脏匀浆并离心以产生细胞沉淀和上清液,并测定RNA表达水平。 |
Kinase Experiment | 将冻干的Cdc42蛋白质在由50mM Tris,0.5mM MgCl 2,50mM NaCl,3%(wt/vol)蔗糖和0.6%葡聚糖组成的缓冲液中重构成5mg/mL。然后将储备溶液在5mM磷酸盐缓冲液(pH 7.4)中稀释至1μM。在含有Cdc42溶液的石英比色杯中,加入等份的ZCL278并在每次荧光测量前温育5分钟。激发波长为275nm,每次添加后测量350nm处色氨酸的荧光。使用GraphPad中的等摩尔特异性结合模型拟合滴定曲线,并计算Kd [1]。 |
Data Literature Source | [1]. Friesland A,et al. Small molecule targeting Cdc42-intersectin interaction disrupts Golgi organization and suppresses cell motility. Proc Natl Acad Sci U S A. 2013 Jan 22;110(4):1261-6. [2]. Chou YY,et al. Identification and Characterization of a Novel Broad-Spectrum Virus Entry Inhibitor. J Virol. 2016 Apr 14;90(9):4494-510. |
Unit | Bottle |
Specification | 10mg 20mg 50mg |
ZCL278 是一种选择性的 Cdc42 调节剂。