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Adezmapimod抑制劑

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  • 型號

    HY-10256

  • 品牌

    MCE

  • 廠商性質(zhì)

    代理商

  • 所在地

    杭州市

規(guī)格

10 mM * 1 mL in DMSO 660元 10000可售

10 mg 600元 10000可售

50 mg 1400元 10000可售

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更新時間:2023-05-25 17:13:47瀏覽次數(shù):476次

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CAS號 152121-47-6 產(chǎn)地 進口
級別 其他
Adezmapimod抑制劑
Adezmapimod (SB 203580) 是一種選擇性的,ATP 競爭性的 p38 MAPK 抑制劑,對 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。

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 競爭性的 p38 MAPK 抑制劑,對 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




IC50 & Target[1]




p38

50 nM (IC50)

p38β2

500 nM (IC50)

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].
SB203580 blocks PKB phosphorylation (IC50 3-5 μM). SB203580 inhibitsthe phosphorylation of Ser473 in a dose-dependent manner in both CT6 and activated human T cells and IL-2-responsive BA/F3 F7 B cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line:CT6, BA/F3 cell line F7, and PBMC/T cells
Concentration:0-30 μM
Incubation Time:Preincubated with 0-30 μM SB203580 for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2
Result:Prevented 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.
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.

Animal Model:Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors[1]
Dosage:5 mg/kg/day
Administration:Intra peritoneal injected daily for 16 consecutive days
Result:After 2 weeks treatment, CAL27 p38WT tumors were significantly smaller; CAL27 p38TM tumors were not affected by the p38 inhibitor (n=10).
分子量

377.43

性狀

Solid

Formula

C21H16FN3OS

CAS 號

152121-47-6

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month
溶解性數(shù)據(jù)
In Vitro: 

DMSO : 20 mg/mL (52.99 mM; ultrasonic and warming and heat to 60°C)

配制儲備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM2.6495 mL13.2475 mL26.4950 mL
5 mM0.5299 mL2.6495 mL5.2990 mL
10 mM0.2649 mL1.3247 mL2.6495 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。

In Vivo:

請根據(jù)您的實驗動物和給藥方式選擇適當?shù)娜芙夥桨浮R韵氯芙夥桨付颊埾劝凑?nbsp;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

  • 1.


    請依序添加每種溶劑: 0.5% CMC-Na/saline water

    Solubility: 16.67 mg/mL (44.17 mM); Suspended solution; Need ultrasonic


  • 2.


    請依序添加每種溶劑: 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution


  • 3.


    請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2 mg/mL (5.30 mM); Clear solution; Need ultrasonic


  • 4.


    請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2 mg/mL (5.30 mM); Clear solution; Need ultrasonic


  • 5.


    請依序添加每種溶劑: 10% DMSO    90% corn oil

    Solubility: 2 mg/mL (5.30 mM); Clear solution; Need ultrasonic



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