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应用
药物靶标
激酶
CMGC：包含CDK，MAPK，GSK3，CLK家族
2-氨基-5-[(5-硝基-2-噻唑基)硫代]-1,3,4-噻二唑

2-氨基-5-[(5-硝基-2-噻唑基)硫代]-1,3,4-噻二唑

选择性JNK抑制剂

规格或纯度: 96%

CAS编号: 40045-50-9
分子式: C₅H₃N₅O₂S₃
分子量: 261.29
MDL号: MFCD01927019
PubChem编号: 11837140

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货号 (SKU)	包装规格	是否现货
A151167-10mg	10mg	现货
A151167-50mg	50mg	现货
A151167-250mg	250mg	现货
A151167-1g	1g	现货

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mitogen-activated protein kinase 8 Inhibitor

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基本描述

规格或纯度	96%
英文名称	2-Amino-5-[(5-nitro-2-thiazolyl)thio]-1,3,4-thiadiazole
别名	5-((5-硝基噻唑-2-基)硫基)-1,3,4-噻二唑-2-胺
英文别名	40045-50-9\|SU 3327\|halicin\|SU3327\|5-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3,4-thiadiazol-2-amine\|SU-3327\|Y4KQC5P9B2\|2-Amino-5-[(5-nitro-2-thiazolyl)thio]-1,3,4-thiadiazole\|5-((5-Nitrothiazol-2-yl)thio)-1,3,4-thiadiazol-2-amine\|5-(5-Nitrothiazol-2-ylthio)
生化机理	c-Jun N末端激酶（JNK）的选择性抑制剂（IC50 =0.7μM）。抑制JNK和JIP之间的蛋白质-蛋白质相互作用（IC50 = 239 nM）。显示对p38 MAPK和Akt的选择性。恢复2型糖尿病小鼠模型的胰岛素敏感性。对多种细菌，包括金黄色葡萄球菌，鲍曼不动杆菌，艰难梭菌和结核分枝杆菌显示抗生素活性。
储存温度	避光,-20°C储存,充氩
运输条件	超低温冰袋运输
产品介绍	产品介绍： SU3327 是一种有效的，选择性的且具有底物竞争性的 JNK 抑制剂，IC50 为 0.7 μM。SU3327 还以 IC50 值为 239 nM 抑制 JNK 和 JIP 之间的蛋白相互作用。SU3327 对 p38α 和 Akt 激酶的活性较低。 Product description： SU3327 is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. SU3327 also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. SU3327 shows less active against p38α and Akt kinase.

名称和标识符

IUPAC Name	5-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3,4-thiadiazol-2-amine
INCHI	InChI=1S/C5H3N5O2S3/c6-3-8-9-5(14-3)15-4-7-1-2(13-4)10(11)12/h1H,(H2,6,8)
InChi Key	NQQBNZBOOHHVQP-UHFFFAOYSA-N
Canonical SMILES	C1=C(SC(=N1)SC2=NN=C(S2)N)[N+](=O)[O-]
分子式	C₅H₃N₅O₂S₃
PubChem CID	11837140
分子量	261.29

数据库链接

PubChem CID	11837140
CAS Registry No.	40045-50-9
ChEMBL Ligand	CHEMBL510038
BindingDB Ligand	29315

化学和物理性质

溶解性	溶于DMSO, 最高浓度 (mg/mL): 26.13, 最高浓度(mM): 100；溶于ethanol, 最高浓度 (mg/mL): 2.61, 最高浓度(mM): 10
敏感性	对热敏感；对光线敏感
熔点	160 °C(dec.)

安全信息

象形图	Harmful
信号词	Warning
危险声明	H315: Causes skin irritation H319: Causes serious eye irritation
预防措施声明	P305+P351+P338,P280,P302+P352,P321,P264,P362+P364,P264+P265,P337+P317,P332+P317
Reaxy-Rn	1139980

靶标

Target ID

1496

名称

mitogen-activated protein kinase 8

缩写名

JNK1

家族

JNK subfamily

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	2	427	10q11.22	MAPK8	mitogen-activated protein kinase 8
Mouse	2	384	14 B	Mapk8	mitogen-activated protein kinase 8
Rat	2	411	16p16	Mapk8	mitogen-activated protein kinase 8

Ensembl Gene

ENSG00000107643 (Hs) , ENSMUSG00000021936 (Mm) , ENSRNOG00000020155 (Rn)

Entrez Gene

26419 (Mm) , 116554 (Rn) , 5599 (Hs)

OMIM

601158 (Hs)

Protein GI

293354099 (Rn) , 20986523 (Hs) , 7710060 (Mm)

UniProtKB

P45983 (Hs) , P49185 (Rn) , Q91Y86 (Mm)

RefSeq Nucleotide

NM_002750 (Hs) , NM_016700 (Mm) , NM_053829 (Rn)

RefSeq Protein

NP_002741 (Hs) , NP_057909 (Mm) , NP_446281 (Rn)

ChEMBL Target

CHEMBL5718 (Rn) , CHEMBL1795174 (Mm) , CHEMBL2276 (Hs)

关联配体

Ligand ID	10703
名称	SU-3327
别名	SU3327
类别	Synthetic organic
学名	5-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3,4-thiadiazol-2-amine
生物活性评价	The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价	SU3327 was originally identified as an inhibitor of the serine/threonine c-Jun N-terminal kinases (JNKs) . It is substrate competitive (inhibiting the protein-protein interaction between JNK and the substrate JIP-1), and selective for JNK vs. p38 MAPK and Akt. SU3327 was shown to restore insulin sensitivity in mouse models of diabetes. In the search for new antibacterials, artificial intelligence algorithms were used to identify novel chemotypes that were likely to have novel mechanisms of antibacterial activity. SU3327 (re-named as halicin) was identified by this process and in vitro and in vivo follow-up showed that it potently killed a wide range of diffucult to treat, antibacterial-resistant bacterial strains . Halicin appears to disrupt the ability of bacteria to maintain an electrochemical gradient across their cell membranes which blocks their production of ATP for energy.

参考文献

1. De SK, Stebbins JL, Chen LH, Riel-Mehan M, Machleidt T, Dahl R, Yuan H, Emdadi A, Barile E, Chen V et al.. (2009) Design, synthesis, and structure-activity relationship of substrate competitive, selective, and in vivo active triazole and thiadiazole inhibitors of the c-Jun N-terminal kinase.. J Med Chem, 52 (7): (1943-52). [PMID:19271755]
2. Stokes JM, Yang K, Swanson K, Jin W, Cubillos-Ruiz A, Donghia NM, MacNair CR, French S, Carfrae LA, Bloom-Ackerman Z et al.. (2020) A Deep Learning Approach to Antibiotic Discovery.. Cell, 180 (4): (688-702.e13). [PMID:32084340]