TMP269
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.
TMP269是一种新型选择性的IIa类组蛋白去乙酰化酶(HDAC)抑制剂,作用于HDAC 4、5、7和9,IC50值分别为126、80、36和9 nM[1]。
组蛋白去乙酰化酶(HDAC)是一系列酶,从组蛋白ε-N-乙酰赖氨酸残基上去除乙酰基,使组蛋白更紧密地包裹住DNA,阻止其转录。
TMP269是一种新型选择性的IIa类HDAC抑制剂。在MM细胞系中,TMP269以剂量依赖的方式诱导中度的细胞毒性,IC50范围介于22-38 μM之间,这与caspase-3、-8、-9和PARP的切割相关。TMP269也增强CFZ诱导的细胞凋亡,增加激活转录因子4(ATF4)和促凋亡转录因子C/EBP同源蛋白(CHOP)的表达。在BMSCs或IL-6存在时,TMP269和CFZ也显示显著的细胞毒性[2]。在IEC-18肠上皮细胞中,TMP269抑制G蛋白偶联受体/蛋白激酶D1(PKD1)激活所诱导的细胞增殖、细胞周期进程和DNA合成[3]。
参考文献:
[1]. Lobera M, Madauss KP, Pohlhaus DT, et al. Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group. Nat Chem Biol, 2013, 9(5): 319-325.
[2]. Kikuchi S, Suzuki R, Ohguchi H, et al. Class IIa HDAC inhibition enhances ER stress-mediated cell death in multiple myeloma. Leukemia, 2015.
[3]. Sinnett-Smith J, Ni Y, Wang J, et al. Protein kinase D1 mediates class IIa histone deacetylase phosphorylation and nuclear extrusion in intestinal epithelial cells: role in mitogenic signaling. Am J Physiol Cell Physiol, 2014, 306(10): C961-71.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 514.52 |
Cas No. | 1314890-29-3 |
Formula | C25H21F3N4O3S |
Synonyms | TMP 269;TMP-269 |
Solubility | ≥23 mg/mL in DMSO; insoluble in H2O; ≥21 mg/mL in EtOH with ultrasonic |
Chemical Name | (Z)-N-((4-(4-phenylthiazol-2-yl)tetrahydro-2H-pyran-4-yl)methyl)-3-(5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl)benzimidic acid |
SDF | Download SDF |
Canonical SMILES | FC(F)(F)C1=NC(C2=CC(/C(O)=N/CC3(C4=NC(C5=CC=CC=C5)=CS4)CCOCC3)=CC=C2)=NO1 |
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。 |
细胞实验 [1]: | |
细胞系 |
IEC-18细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于23 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
4 μM, 18 h, 37°C |
应用 |
在IEC-18肠上皮细胞中,TMP269有效抑制ANG II诱导的[3H]胸苷掺入,EC50大约为1.5 μM。TMP269完全防止了ANG II刺激的G0/G1到G2/M转变。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Sinnett-Smith J, Ni Y, Wang J, et al. Protein kinase D1 mediates class IIa histone deacetylase phosphorylation and nuclear extrusion in intestinal epithelial cells: role in mitogenic signaling[J]. American Journal of Physiology-Cell Physiology, 2014, 306(10): C961-C971. |
描述 | TMP269是一种有效的和选择性的IIa类HDAC抑制剂,作用于HDAC4、HDAC5、HDAC7和HDAC9,IC50值分别为157 nM、97 nM、43 nM和23 nM。 | |||||
靶点 | HDAC9 | HDAC7 | HDAC5 | HDAC4 | ||
IC50 | 23 nM | 43 nM | 97 nM | 157 nM |