 
        
        
        TTP 22是一种高亲和力、ATP竞争性的酪蛋白激酶2(CK2)抑制剂,IC50/Ki为0.1 μM/40 nM,表现出对CK2的选择性,相较于JNK3、ROCK1和MET(IC50 > 10 μM)。
 
                                 
                                
                            

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| 产品名称 | CK1 ↓ ↑ | CK2 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| PF-670462 2HCl | ++++ CK1δ, IC50: 13 nM CK1ε, IC50: 90 nM | 99%+ | |||||||||||||||||
| D4476 | ++ CK1 from Schizosaccharomyces pombe, IC50: 200 nM CK1δ, IC50: 300 nM | 99% | |||||||||||||||||
| SR-3029 | +++ CK1δ, IC50: 44 nM CK1ε, IC50: 260 nM | 99%+ | |||||||||||||||||
| IWP-2 | +++ M82FCK1δ, IC50: 40 nM | Wnt | 99% | ||||||||||||||||
| LY364947 | ++ CK1δ, IC50: 0.22 μM | 98% | |||||||||||||||||
| TA-01 | ++++ CK1δ, IC50: 6.8 nM CK1ε, IC50: 6.4 nM | p38 MAPK | 99%+ | ||||||||||||||||
| IC261 | + CK1, IC50: 16 μM | 98% | |||||||||||||||||
| PF-4800567 | +++ casein kinase 1 epsilon, IC50: 32 nM casein kinase 1 delta, IC50: 711 nM | 99%+ | |||||||||||||||||
| CK1-IN-1 | ++++ CK1δ, IC50: 15 nM CK1ε, IC50: 16 nM | 99% | |||||||||||||||||
| Longdaysin | + CKIα, IC50: 5.6 μM CKIδ, IC50: 8.8 μM | 99%+ | |||||||||||||||||
| Silmitasertib | ++++ CK2, IC50: 1 nM | 99%+ | |||||||||||||||||
| Ellagic acid (hydrate) | +++ CK2, IC50: 0.04 μM | PKA | 95+% | ||||||||||||||||
| DMAT | +++ CK2, Ki: ~40 nM | 99% | |||||||||||||||||
| Hematein | ++ CK2, IC50: 0.55 μM | 40% | |||||||||||||||||
| Silmitasertib sodium salt | ++++ CK2α', IC50: 1 nM CK2α, IC50: 1 nM | 99%+ | |||||||||||||||||
| LY294002 | +++ CK2, IC50: 98 nM | 99%+ | |||||||||||||||||
| A-3 HCl | + CK1, Ki: 80 μM | ++ CK2, Ki: 5.1 μM | PKA,MLCK,PKC | 98+% | |||||||||||||||
| TBB | + CK1, Ki: 47 μM | ++ CK2, Ki: 0.4 μM | 98% | ||||||||||||||||
| TTP 22 | ++ CK2, IC50: 100 nM | 98%+ | |||||||||||||||||
| DRB | ✔ | 99%+ | |||||||||||||||||
| BioE-1115 | + CK2α, IC50: 10 μM | 99%+ | |||||||||||||||||
| (E/Z)-GO289 | ++++ CK2, IC50: 7 nM | 99%+ | |||||||||||||||||
| 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。 | |||||||||||||||||||
| 靶点 | 
 | 
| 描述 | Protein kinase CK2 (formerly known as casein kinase 2) is a constitutively-active kinase that is expressed ubiquitously in eukaryotes. CK2 is critical in embryonic development, differentiation, immunity, cell survival, epithelial homeostasis and circadian rhythms and is abnormally elevated in many cancers[2]. TTP 22 is a potent and ATP-competitive CK2 inhibitor, with an IC50 of 100 nM and a Ki of 40 nM. It shows selectivity for CK2 over other kianses such as Jnk3, Rock1, Tie2, Ask1, Met and FGFR1 at 10 μM[3]. | 
| Concentration | Treated Time | Description | References | |
| Plasmodium falciparum NF54 parasites | 50 µM | To test the inhibitory effect of TTP 22 on parasite proliferation, results showed TTP 22 performed poorly (IC50 > 50 µM) | Commun Biol. 2021 Mar 12;4(1):336. | |
| Plasmodium falciparum NF54 parasites | 50 µM | Test the inhibitory effect of TTP 22 on parasite proliferation, results showed IC50 > 50 µM | Commun Biol. 2021 Mar 12;4(1):336. | |
| HeLa cells | 1 µM | 4 h | Inhibits CK2 activity, increases nuclear localization of mVenus-α-TAT1 | J Cell Biol. 2022 Nov 7;221(11):e202202100. | 
[2]Silva-Pavez E, Tapia JC. Protein Kinase CK2 in Cancer Energetics. Front Oncol. 2020 Jun 18;10:893
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 3.03mL 0.61mL 0.30mL | 15.13mL 3.03mL 1.51mL | 30.26mL 6.05mL 3.03mL | |
| CAS号 | 329907-28-0 | 
| 分子式 | C16H14N2O2S2 | 
| 分子量 | 330.42 | 
| SMILES Code | O=C(O)CCSC1=C(C(C2=CC=C(C)C=C2)=CS3)C3=NC=N1 | 
| MDL No. | MFCD02654497 | 
| 别名 | |
| 运输 | 蓝冰 | 
| InChI Key | RAOULLCLLOGTDA-UHFFFAOYSA-N | 
| Pubchem ID | 1536915 | 
| 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, store in freezer, under -20°C | 
| 溶解方案 | DMSO: 50 mg/mL(151.32 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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 
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