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瀏覽器自帶分享功能也很好用哦~貨號：HY-10182
CAS：252917-06-9
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Laduviglusib
Laduviglusib (CHIR-99021) 是一種有效的選擇性 GSK-3α/β 抑制劑，IC50 為 10 nM 和 6.7 nM。Laduviglusib 對 GSK-3 的選擇性比 CDC2，ERK2 和其他蛋白激酶高 500 倍以上。Laduviglusib 還是一種有效的 Wnt/β-catenin 信號通路ji活劑。CHIR-99021 可增強小鼠和人類胚胎干細胞的自我更新。Laduviglusib 能誘導(dǎo)細胞自噬 (autophagy)。
生物活性
Laduviglusib (CHIR-99021) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib enhances mouse and human embryonic stem cells self-renewal. Laduviglusib induces autophagy[1][2][3].
體外研究(In Vitro)
Laduviglusib (CHIR-99021) inhibits human GSK-3β with Ki values of 9.8 nM[1]. Laduviglusib is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites.In vitro kinase assays reveal that Laduviglusib specifically inhibits GSK3β (IC50=~5 nM) and GSK3α (IC50=~10 nM), with little effect on other kinases[4]. In the presence of Laduviglusib the viability of the ES-D3 cells is reduced by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM Laduviglusib with an IC50 of 4.9 μM[2].
體內(nèi)研究(In Vivo)
In ZDF rats, a single oral dose of Laduviglusib (16 mg/kg or 48 mg/kg) rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration[1]. Laduviglusib (2 mg/kg) given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). Laduviglusib treatment significantly blocks crypt apoptosis and accumulation of p-H2AX+ cells, and improves crypt regeneration and villus height. Laduviglusib treatment increases Lgr5+ cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h[5].
分子量：465.34
Formula：C22H18Cl2N8
CAS 號：252917-06-9
運輸條件：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 : 16.67 mg/mL (35.82 mM; Need ultrasonic)
| 濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1490 mL | 10.7448 mL | 21.4897 mL |
| 5 mM | 0.4298 mL | 2.1490 mL | 4.2979 mL |
| 10 mM | 0.2149 mL | 1.0745 mL | 2.1490 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，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用； 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
貨號：HY-10182
CAS：252917-06-9
在線客服客服一Laduviglusib
Laduviglusib (CHIR-99021) 是一種有效的選擇性 GSK-3α/β 抑制劑，IC50 為 10 nM 和 6.7 nM。Laduviglusib 對 GSK-3 的選擇性比 CDC2，ERK2 和其他蛋白激酶高 500 倍以上。Laduviglusib 還是一種有效的 Wnt/β-catenin 信號通路ji活劑。CHIR-99021 可增強小鼠和人類胚胎干細胞的自我更新。Laduviglusib 能誘導(dǎo)細胞自噬 (autophagy)。
生物活性
Laduviglusib (CHIR-99021) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib enhances mouse and human embryonic stem cells self-renewal. Laduviglusib induces autophagy[1][2][3].
體外研究(In Vitro)
Laduviglusib (CHIR-99021) inhibits human GSK-3β with Ki values of 9.8 nM[1]. Laduviglusib is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites.In vitro kinase assays reveal that Laduviglusib specifically inhibits GSK3β (IC50=~5 nM) and GSK3α (IC50=~10 nM), with little effect on other kinases[4]. In the presence of Laduviglusib the viability of the ES-D3 cells is reduced by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM Laduviglusib with an IC50 of 4.9 μM[2].
體內(nèi)研究(In Vivo)
In ZDF rats, a single oral dose of Laduviglusib (16 mg/kg or 48 mg/kg) rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration[1]. Laduviglusib (2 mg/kg) given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). Laduviglusib treatment significantly blocks crypt apoptosis and accumulation of p-H2AX+ cells, and improves crypt regeneration and villus height. Laduviglusib treatment increases Lgr5+ cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h[5].
分子量：465.34
Formula：C22H18Cl2N8
CAS 號：252917-06-9
運輸條件：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 : 16.67 mg/mL (35.82 mM; Need ultrasonic)
| 濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1490 mL | 10.7448 mL | 21.4897 mL |
| 5 mM | 0.4298 mL | 2.1490 mL | 4.2979 mL |
| 10 mM | 0.2149 mL | 1.0745 mL | 2.1490 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，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用； 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
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