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Stattic 是一種有效的 STAT3 抑制劑,可以抑制 STAT3 磷酸化 (磷酸化位點為 Y705 和 S727)。Stattic 抑制高親和力磷酸肽與 STAT3 的 SH2 域結(jié)合。Stattic 可改善 Alport 綜合征 (AS) 小鼠的腎功能不全。
生物活性
Stattic is a potent STAT3 inhibitor and inhibits STAT3 phosphorylation (at Y705 and S727)[1]. Stattic inhibits the binding of a high affinity phosphopeptide for the SH2 domain of STAT3[2]. Stattic ameliorates the renal dysfunction in Alport syndrome (AS) mice[3].
STAT3
體外研究(In Vitro)
Stattic (20 μM; 24 hours) inhibits STAT3 phosphorylation (Y705) and selectively inhibits P-STAT3 as demonstrated by the lack of inhibition of P-ERK1/2 in ALDH+ and D44+/CD24+ subpopulations of Panc-1 and HPAC pancreatic cancer cell lines[1].
Stattic (2.5, 5, 10 μM; for 4 h) significantly reduces the nuclear level of pSTAT3 and survivin in PC3M-1E8 cells at 10 μM. Stattic (2.5-10 μM; for 24 h) inhibits IL-6-induced STAT3 activation in a dose-dependent manner[2].
Stattic (2.5, 5, 10 μM; for 48 h) suppresses both the growth and induces apoptosis prostate cancer cells (PC3M-1E8 cells) with 10 μM. Stattic does not induce significant cell apoptosis with 2.5 μM, 5 μM[2].
Stattic (2.5, 5, 10 μM; for 48 h) shows significant S phase accumulation[2].
Stattic can not lead to significant morphological changes or apoptosis and has little STAT3 phosphorylation in A2780 cells and HUVECs[2].
體內(nèi)研究(In Vivo)
Stattic (10 mg/kg; i.p.; three times per week for 10 week) ameliorates the renal dysfunction in Alport syndrome (AS) mice[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | Age-matched wild-type (WT) C57BL/6 mice[3] |
Dosage: | 10 mg/kg |
Administration: | IP; three timesper week for 10 week |
Result: | Increased levels of proteinuria, BUN and serum creatinine. Significantly suppressed the gene expression levels of renal injury markers (Lcn2, Kim-1), pro-inflammatory cytokines (Il-6, KC), pro-fibrotic genes (Tgf-β, Col1a1, α-Sma) and Mmp9. |
分子量:211.19
Formula:C8H5NO4S
CAS 號:19983-44-9
運(yùn)輸條件:Room temperature in continental US; may vary elsewhere.
儲存方式:
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 50 mg/mL (236.75 mM; Need ultrasonic)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 4.7351 mL | 23.6754 mL | 47.3507 mL |
5 mM | 0.9470 mL | 4.7351 mL | 9.4701 mL |
10 mM | 0.4735 mL | 2.3675 mL | 4.7351 mL |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲存時,請在 6 個月內(nèi)使用,-20°C 儲存時,請在 1 個月內(nèi)使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶
參考文獻(xiàn)
[2]. John S McMurray, et al. A new small-molecule Stat3 inhibitor. Chem Biol. 2006 Nov;13(11):1123-4.
Stattic 是一種有效的 STAT3 抑制劑,可以抑制 STAT3 磷酸化 (磷酸化位點為 Y705 和 S727)。Stattic 抑制高親和力磷酸肽與 STAT3 的 SH2 域結(jié)合。Stattic 可改善 Alport 綜合征 (AS) 小鼠的腎功能不全。
生物活性
Stattic is a potent STAT3 inhibitor and inhibits STAT3 phosphorylation (at Y705 and S727)[1]. Stattic inhibits the binding of a high affinity phosphopeptide for the SH2 domain of STAT3[2]. Stattic ameliorates the renal dysfunction in Alport syndrome (AS) mice[3].
STAT3
體外研究(In Vitro)
Stattic (20 μM; 24 hours) inhibits STAT3 phosphorylation (Y705) and selectively inhibits P-STAT3 as demonstrated by the lack of inhibition of P-ERK1/2 in ALDH+ and D44+/CD24+ subpopulations of Panc-1 and HPAC pancreatic cancer cell lines[1].
Stattic (2.5, 5, 10 μM; for 4 h) significantly reduces the nuclear level of pSTAT3 and survivin in PC3M-1E8 cells at 10 μM. Stattic (2.5-10 μM; for 24 h) inhibits IL-6-induced STAT3 activation in a dose-dependent manner[2].
Stattic (2.5, 5, 10 μM; for 48 h) suppresses both the growth and induces apoptosis prostate cancer cells (PC3M-1E8 cells) with 10 μM. Stattic does not induce significant cell apoptosis with 2.5 μM, 5 μM[2].
Stattic (2.5, 5, 10 μM; for 48 h) shows significant S phase accumulation[2].
Stattic can not lead to significant morphological changes or apoptosis and has little STAT3 phosphorylation in A2780 cells and HUVECs[2].
體內(nèi)研究(In Vivo)
Stattic (10 mg/kg; i.p.; three times per week for 10 week) ameliorates the renal dysfunction in Alport syndrome (AS) mice[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | Age-matched wild-type (WT) C57BL/6 mice[3] |
Dosage: | 10 mg/kg |
Administration: | IP; three timesper week for 10 week |
Result: | Increased levels of proteinuria, BUN and serum creatinine. Significantly suppressed the gene expression levels of renal injury markers (Lcn2, Kim-1), pro-inflammatory cytokines (Il-6, KC), pro-fibrotic genes (Tgf-β, Col1a1, α-Sma) and Mmp9. |
分子量:211.19
Formula:C8H5NO4S
CAS 號:19983-44-9
運(yùn)輸條件:Room temperature in continental US; may vary elsewhere.
儲存方式:
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 50 mg/mL (236.75 mM; Need ultrasonic)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 4.7351 mL | 23.6754 mL | 47.3507 mL |
5 mM | 0.9470 mL | 4.7351 mL | 9.4701 mL |
10 mM | 0.4735 mL | 2.3675 mL | 4.7351 mL |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲存時,請在 6 個月內(nèi)使用,-20°C 儲存時,請在 1 個月內(nèi)使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶
參考文獻(xiàn)
[2]. John S McMurray, et al. A new small-molecule Stat3 inhibitor. Chem Biol. 2006 Nov;13(11):1123-4.