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160807-49-8

中文名稱(chēng) 靛玉紅-3' -單肟
英文名稱(chēng) INDIRUBIN-3'-MONOXIME
CAS 160807-49-8
分子式 C16H11N3O2
分子量 277.28
MOL 文件 160807-49-8.mol
更新日期 2024/12/15 19:35:21
160807-49-8 結(jié)構(gòu)式 160807-49-8 結(jié)構(gòu)式

基本信息

中文別名
靛玉紅-3'-肟
靛玉紅-3' -單肟
英文別名
Indirubin-3'
Indirubin-3′
INDIRUBIN-3'-OXIME
Indirubine-3'-oxime
INDIRUBIN-3'-MONOXIME
INDIRUBIN-3’-MONOOXIME
3-[1,3-DIHYDRO-3-(HYDROXYIMINO)-2H-INDOL-2-YLIDENE]-1,3-DIHYDRO-2H-INDOL-2-ONE

物理化學(xué)性質(zhì)

熔點(diǎn)247-249°C
沸點(diǎn)532.2±50.0 °C(Predicted)
密度1.50
儲(chǔ)存條件room temp
儲(chǔ)存條件Store at RT
溶解度DMSO: >10 mg/mL
溶解度二甲基亞砜:>10 mg/mL
酸度系數(shù)(pKa)8.66±0.20(Predicted)
形態(tài)solid
顏色深紅色或棕色
穩(wěn)定性感光
CAS 數(shù)據(jù)庫(kù)160807-49-8

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H332-H335
防范說(shuō)明P261-P280-P305+P351+P338
WGK Germany3
WGK Germany3

應(yīng)用領(lǐng)域

用途1
A potent inhibitor of GSK-3脽 (IC50=22nM). Also inhibits CDK1 (IC50=180nM) and CDK (IC50=100nM). It reversibly arrests asynchronous HBL-100 cells at G2. It induces apoptosis in the mammary carcinoma cell line MCF-7 (10眉M).
靛玉紅-3' -單肟?jī)r(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2024/11/11XW16080749803靛玉紅-3’-單肟160807-49-8100MG5632元
2024/11/11XW16080749802靛玉紅-3’-單肟160807-49-825MG2055元
2024/11/11XW16080749801靛玉紅-3’-單肟160807-49-85MG549元

常見(jiàn)問(wèn)題列表

生物活性
Indirubin-3'-monoxime (Indirubin-3'-oxime)是一種選擇性的CDK抑制劑,對(duì)CDK1-cyclinB, CDK2-cyclinA, CDK2-cyclinE, CDK4-cyclinD1, CDK5-p35的IC50分別為 0.18 μM, 0.44 μM, 0.25 μM, 3.33 μM, 0.065 μM。Indirubin-3'-monoxime是一種直接、選擇性的5-lipoxygenase抑制劑,IC50為7.8-10 μM。
靶點(diǎn)
TargetValue
CDK5-P35
(Cell-free assay)
0.065 μM
CDK1-cyclinB
(Cell-free assay)
0.18 μM
CDK2-cyclinE
(Cell-free assay)
0.25 μM
CDK2-cyclinA
(Cell-free assay)
0.44 μM
CDK4-cyclinD1
(Cell-free assay)
3.33 μM
體外研究

Indirubin-3'-monoxime inhibits GSK-3β by competing with ATP, with K i of 0.85 μM, and K m of 110 μM. Indirubin-3'-monoxime also inhibits tau phosphorylation by GSK-3β, with an IC 50 value of around 100 nM. Indirubin-3'-monoxime completely inhibits the phosphorylation of the AT100 epitope. Indirubin-3'-monoxime inhibits vascular smooth muscle cell (VSMC) proliferation with IC 50 of ~2 μM. Indirubin-3'-monoxime blunts migration of VSMC stimulated with the PDGF. Indirubin-3'-monoxime interferes with the migratory response in VSMC, and also suppresses the production of pro-migratory LT in monocytes. Moreover, Indirubin-3'-monoxime inhibits 5-lipoxygenase (5-LO) product synthesis in monocytes and neutrophils, with the same potency (IC 50 =5.0±1.1 and 3.7±1.2 μM, respectively). Indirubin-3'-monoxime is an inhibitor of 5-LO, with IC 50 of 7.8-10 μM in cell-free assay.

體內(nèi)研究

Indirubin-3'-monoxime (0.1, 0.2 and 0.4 mg/kg, i.p) dose dependently reverses the cognitive impairment and combats the elevated oxidative stress markers in HFD fed mice. Indirubin-3'-monoxime also dose dependently lowers the serum glucose, TGs, TC and insulin levels, and improves the β-cell functioning in HFD fed mice. Moreover, Indirubin-3'-monoxime treatment significantly decreases HOMA-IR levels compared to HFD group. Indirubin-3'-monoxime (0.4 mg/kg) significantly attenuates the increased EL in the HFD group.

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