注:本產(chǎn)品僅用于科研,不可用于臨床
Adezmapimod抑制劑
Adezmapimod (SB 203580) 是一種選擇性的,ATP 競(jìng)爭(zhēng)性的 p38 MAPK 抑制劑,對(duì) SAPK2a/p38 和 SAPK2b/p38β2 的 IC50 分別為 50 nM 和 500 nM。Adezmapimod 抑制 LCK,GSK3β 和 PKBα,IC50 比 SAPK2a/p38 高 100-500 倍。Adezmapimod 不抑制 JNK 活性,是一種自噬 (autophagy) 和線粒體自噬 (mitophagy) 激活劑。
Adezmapimod抑制劑 生物活性
Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator
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| 體外研究 (In Vitro) | Adezmapimod (SB 203580) (preincubated with 0-30 μM for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2) prevents the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3-5 μM[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation Assay[1]
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| 體內(nèi)研究 (In Vivo) | Adezmapimod (SB 203580) (5 mg/kg/day; intra peritoneal injected daily for 16 consecutive days, in female atymic Nu/Nu mice) treatment, p38WT tumors show a significantly smaller tumor burden when compared with p38TM tumors that were treated in parallel[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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| 分子量 | 377.43 | ||||||||||||||||
| 性狀 | Solid | ||||||||||||||||
| Formula | C21H16FN3OS | ||||||||||||||||
| CAS 號(hào) | 152121-47-6 | ||||||||||||||||
| 運(yùn)輸條件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
| 儲(chǔ)存方式 |
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| 溶解性數(shù)據(jù) | In Vitro: DMSO : 20 mg/mL (52.99 mM; ultrasonic and warming and heat to 60°C) 配制儲(chǔ)備液
* 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。 In Vivo: 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮R韵氯芙夥桨付颊?qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑: ——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)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
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