Active-mono-sulfone-PEG8-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
IC50 & Target
PEGs
体外研究 (In Vitro)
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
767.88
Formula
C37H53NO14S
CAS 号
2055048-45-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562
GSK2983559 active metabolite 是 GSK2983559 的活性代谢物。GSK2983559 active metabolite 是一种受体相互作用蛋白-2 (RIP2) 激酶抑制剂,详细信息请参考专利 WO/2014043446 A1 中的化合物 example 1。
GSK2983559 active metabolite Chemical Structure
CAS No. : 1423186-80-4
规格
价格
是否有货
数量
10 mM * 1 mL in DMSO
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100 mg
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GSK2983559 active metabolite 相关产品
•相关化合物库:
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Clinical Compound Library
生物活性
GSK2983559 active metabolite is an active metabolite of GSK2983559. GSK2983559 active metabolite is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.
IC50 & Target
RIP2 Kinase[1]
体外研究 (In Vitro)
GSK2983559 active metabolite is a novel prodrug of a quinazolyl amine that inhibits RIP2 kinase. Receptor interacting protein-2 (RIP2) kinase, which is also referred to as CARD3, RICK, CARDIAK, or RIPK2, is a TKL family serine/threonine protein kinase involved in innate immune signaling. RIP2 kinase is composed of an N-terminal kinase domain and a C-terminal caspase-recruitment domain (CARD) linked via an intermediate (IM) region. The CARD domain of RIP2 kinase mediates interaction with other CARD-containing proteins, such as NODI and NOD2. NODI and NOD2 are cytoplasmic receptors which play a key role in innate immune surveillance. They recognize both gram positive and gram negative bacterial pathogens and are activated by specific peptidoglycan motifs, diaminopimelic acid (i.e., DAP) and muramyl dipeptide[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
458.55
Formula
C21H22N4O4S2
CAS 号
1423186-80-4
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Linda N. Casillas, et al. Prodrugs of amino quinazoline kinase inhibitor. PCT Int. Appl. (2014), WO 2014043446 A1 20140320.
Animal Administration [1]
Rats[1] Rats are orally pre-dosed with RIP2 kinase inhibitor 1, at a dose of 2 mg/kg (8 rats) and with Prednisolone (8 rats, used as a positive control), followed by dosing with L18-MDP (50 μg/rat) 0.25 h/min after pre-dosing. Combined cytokine levels (IL8, TNFa, IL6 and IL-Ιβ) in whole blood samples taken from the rats in this study are measured using an antibody based detection. The combined cytokine response is calculated as the averaged response for the 4 cytokines measured relative to the response observed in the vehicle-treated mice, and are depicted as the mean±standard error of the mean (n=8 rats/group).
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Linda N. Casillas, et al. Prodrugs of amino quinazoline kinase inhibitor. PCT Int. Appl. (2014), WO 2014043446 A1 20140320.