2-[[(苯甲?;被?硫代甲酰]氨基]-4,7-二氫-5,5-二甲基-5H-噻吩并[2,3-C]吡喃-3-羧酸
中文名稱 | 2-[[(苯甲?;被?硫代甲酰]氨基]-4,7-二氫-5,5-二甲基-5H-噻吩并[2,3-C]吡喃-3-羧酸 |
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中文同義詞 | 2-[[(苯甲酰基氨基)硫代甲酰]氨基]-4,7-二氫-5,5-二甲基-5H-噻吩并[2,3-C]吡喃-3-羧酸;2-(3-苯甲酰硫脲基)5,5-二甲基-5,7-二氫-4H-噻吩[2,3-C]吡喃-3-羧酸;2-(3-苯甲酰硫脲基)5,5-二甲基-5,7-二氫-4H-噻吩[2,3-C]吡喃-3-甲酸;化合物CID-1067700;化合物CID-1067700,10 MM DMSO 溶液 |
英文名稱 | CID-1067700,2-(3-benzoylthioureido)-5,5-diMethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxylic acid |
英文同義詞 | CID-1067700,2-(3-benzoylthioureido)-5,5-diMethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxylic acid;CID-1067700;2-(Benzoylcarbamothioylamino)-5,5-dimethyl-4,7-dihydrothieno[2,3-c]pyran-3-carboxylic Acid;2-[[(Benzoylamino)thioxomethyl]amino]-4,7-dihydro-5,5-dimethyl-5H-thieno[2,3-c]pyran-3-carboxylic acid;SID57578339;CS-1986;5H-Thieno[2,3-c]pyran-3-carboxylic acid, 2-[[(benzoylamino)thioxomethyl]amino]-4,7-dihydro-5,5-dimethyl-;ML282,competitively,CID1067700,brain,Rab7,ML 282,GTPase,Ras,machinery,Ras-related,CID-1067700,ML-282,inhibit,CSR,Inhibitor,CID 1067700 |
CAS號 | 314042-01-8 |
分子式 | C18H18N2O4S2 |
分子量 | 390.48 |
EINECS號 | |
相關(guān)類別 | |
Mol文件 | 314042-01-8.mol |
結(jié)構(gòu)式 | ![]() |
2-[[(苯甲?;被?硫代甲酰]氨基]-4,7-二氫-5,5-二甲基-5H-噻吩并[2,3-C]吡喃-3-羧酸 性質(zhì)
密度 | 1.410±0.06 g/cm3(Predicted) |
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儲存條件 | 2-8°C |
溶解度 | DMSO:可溶10mg/mL,澄清 |
酸度系數(shù)(pKa) | 4.25±0.40(Predicted) |
形態(tài) | 粉末 |
顏色 | 白色至淺棕色 |
穩(wěn)定性 | 自購買之日起 1 年內(nèi)保持穩(wěn)定。 DMSO 中的溶液可在 -20°C 下保存長達 2 個月。 |
Ki: 13 nM (Rab7)
CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Rab7 with a K i of 13 nM. CID-1067700 shows inhibitory activity against nucleotide binding by Rab7, with K d s of 100 nM and 40 nM for BODIPY-GTP and BODIPY-GDP, respectively. With increasing concentration, CID-1067700 causes strong inhibition on binding of the BODIPY-linked nucleotides, with EC 50 values of 11.22 ± 1.34 nM for BODIPY-GTP and 20.96 ± 1.34 nM for BODIPY-GDP and calculated K i values of 12.89 nM and 19.70 nM respectively. CID-1067700 (10 μM) has no effect on the rate of release of bound BODIPY-linked nucleotide by wild type Rab7 under equilibrium binding conditions. CID-1067700 (0-40 μM) inhibits Rab7 activity, NF-κB activation as well as AID induction in B cells. Furthermore, CID-1067700 binds Rab7 with a high affinity (EC 50 : 10-20 nM), and blocks Class switch DNA recombination (CSR) in B cells via targeting Rab7.
CID-1067700 (ML282; 16 mg/kg, i.p.) prevents disease development in lupus-prone mice by Rab7 inhibition, and reduces IgG-IC deposition in MRL/ Fas lpr/lpr mice. CID-1067700 also targets B cells and specifically impairs the CSR machinery in vivo.
安全信息
WGK Germany | 3 |
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更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
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2025/02/08 | HY-13452 | 2-[[(苯甲?;被?硫代甲酰]氨基]-4,7-二氫-5,5-二甲基-5H-噻吩并[2,3-C]吡喃-3-羧酸 CID-1067700 | 314042-01-8 | 1 mg | 310元 |
2025/02/08 | HY-13452 | 2-[[(苯甲?;被?硫代甲酰]氨基]-4,7-二氫-5,5-二甲基-5H-噻吩并[2,3-C]吡喃-3-羧酸 CID-1067700 | 314042-01-8 | 10mM * 1mLin DMSO | 601元 |