ST 2825
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.
ST2825是MyD88二聚化的特异性抑制剂[1]。
ST2825是模仿MyD88-TIR结构域BB-环的7肽结构而合成的化合物,抑制MyD88的同源二聚化。ST 2825特异性抑制MyD88 TIR结构域的同源二聚化,而对死亡结构域(death domains)的同源二聚化不起作用。在转染Flag-MyD88和Myc-MyD88的HEK293T细胞中,ST 2825在10 μM浓度时抑制了80% 的MyD88相互作用,从而影响了随后IRAK1和IRAK4的募集。此外,在小鼠中,ST 2825以100和200 mg/kg的剂量给药后显著抑制IL-1β刺激的IL-6的生产。而且,8 μM ST 2825完全阻止TLR9诱导的B细胞增殖。ST2825也可以剂量依赖地抑制CpG诱导的浆细胞的产生[1]。
参考文献:
[1] Loiarro M, Capolunghi F, Fantò N, et al. Pivotal Advance: Inhibition of MyD88 dimerization and recruitment of IRAK1 and IRAK4 by a novel peptidomimetic compound. Journal of leukocyte biology, 2007, 82(4): 801-810.
- 1. Katia Beider, Valeria Voevoda-Dimenshtein, et al. "CXCL13 chemokine is a novel player in multiple myeloma osteolytic microenvironment, M2 macrophage polarization, and tumor progression." J Hematol Oncol. 2022 Oct 10;15(1):144. PMID: 36217194
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- 5. Janda J, Burkett NB, et al. "Resatorvid-based Pharmacological Antagonism of Cutaneous TLR4 Blocks UV-induced NF-κB and AP-1 Signaling in Keratinocytes and Mouse Skin." Photochem Photobiol. 2016 Nov;92(6):816-825. PMID: 27859308
- 6. Wang SH, Wang SC, et al. "Induction of cyclooxygenase-2 gene by Candida albicans through EGFR, ERK, and p38 pathways in human urinary epithelium." Med Mycol. 2016 Sep 23. PMID: 27664170
- 7. Hu LT, et al. "Role of TREM-1 in response to Aspergillus fumigatus infection in corneal epithelial cells.." Int Immunopharmacol.2014 Sep 18. pii:S1567-5769(14)00363-4. PMID: 25242387
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 591.51 |
Cas No. | 894787-30-5 |
Formula | C27H28Cl2N4O5S |
Synonyms | ST2825;ST-2825 |
Solubility | Soluble in DMSO |
Chemical Name | (4R,7R,8aR)-1'-[2-[4-[[2-(2,4-dichlorophenoxy)acetyl]amino]phenyl]acetyl]-6-oxospiro[3,4,8,8a-tetrahydro-2H-pyrrolo[2,1-b][1,3]thiazine-7,2'-pyrrolidine]-4-carboxamide |
SDF | Download SDF |
Canonical SMILES | C1CC2(CC3N(C2=O)C(CCS3)C(=O)N)N(C1)C(=O)CC4=CC=C(C=C4)NC(=O)COC5=C(C=C(C=C5)Cl)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。 |
细胞实验[1]: | |
细胞系 |
HEK 293T和HeLa细胞[1],B细胞和浆细胞样树突细胞[1]。 |
溶解方法 |
在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
6-7 h(HEK 293T细胞)、15 min(HeLa细胞)、5天(B细胞培养)[1] |
应用 |
在HEK293T细胞中,ST2825特异性地抑制MyD88 TIR结构域的同源二聚化,在5 μM和10 μM时分别获得40%和80%的抑制。该效应对TIR结构域的同源二聚化是特异性的,而对死亡结构域的同源二聚化不起作用。而且,ST2825干扰MyD88对IRAK1和IRAK4的募集,从而抑制IL-1介导的NF-κB转录活性的激活[1]。CpG诱导TLR9的激活,从而诱导B细胞增殖和分化形成浆细胞,而ST2825(> 8 μM)可以抑制该反应。这些结果表明,ST2825通过干扰MyD88的同源二聚化,从而阻断IL-1R/TLR信号。ST2825可能具有治疗慢性炎性疾病的潜力[1]。在来自SLE患者的外周血单核细胞中,ST2825阻断TLR9诱导的浆细胞(PC)的生成[3]。 |
动物实验[2]: | |
动物模型 |
雌性C57BL小鼠[1] |
剂量 |
100或200 mg/kg/day;口服给药[1];25 mg/kg/day,注射[2] |
准备方法 |
ST2825溶于0.5%羧甲基纤维素[1] |
应用 |
在治疗小鼠中,ST2825(100或200 mg/kg/day)剂量依赖地抑制IL-1β诱导的IL-6的产生[1]。在非再灌注急性心肌梗塞小鼠模型中,ST2825(25 mg/kg)防止左心室扩张和肥厚,而梗死面积没有显著减少[2]。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1]. Loiarro M, Capolunghi F, Fantò N et al. Pivotal advance: inhibition of MyD88 dimerization and recruitment of IRAK1 and IRAK4 by a novel peptidomimetic compound. Journal of Leukocyte Biology (2007), 82(4), 801-810. [2]. Van Tassell BW, Seropian IM, Toldo S et al. Pharmacologic Inhibition of Myeloid Differentiation Factor 88 (MyD88) Prevents Left Ventricular Dilation and Hypertrophy After Experimental Acute Myocardial Infarction in the Mouse. Journal of Cardiovascular Pharmacology (2010), 55(4), 385-390. [3]. Capolunghi F1, Rosado MM, Cascioli S et al., Pharmacological inhibition of TLR9 activation blocks autoantibody production in human B cells from SLE patients. Rheumatology (Oxford). 2010 Dec;49(12):2281-9. |
描述 | ST2825是MyD88抑制剂。 | |||||
靶点 | MyD88 | |||||
IC50 |