PD98059

PD98059 是一種有效的選擇性的 MEK 抑制劑，IC50 為 5 μM。PD98059 與 MEK 的無(wú)活性形式結(jié)合，從而阻止上游激酶ji活 MEK1 (IC50 為 2-7 μM) 和 MEK2 (IC50 為 50 μM)。PD98059 是一種 ERK1/2 信號(hào)的抑制劑。PD98059 是一種芳烴受體 (AHR) 的配體，可抑制細(xì)胞中 TCDD 結(jié)合 (IC50 為 4 μM) 和 AHR 轉(zhuǎn)化 (IC50 為 1 μM)。PD98059 還可抑制細(xì)胞自噬 (autophagy)。

貨號(hào)：HY-12028
CAS：167869-21-8

參數(shù)品牌：MCE

產(chǎn)品參數(shù)

品牌：MCE

型號(hào)：HY-12028

起訂量：1

規(guī)格:：5mg

價(jià)格:：￥750

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PD98059

PD98059 是一種有效的選擇性的 MEK 抑制劑，IC₅₀ 為 5 μM。PD98059 與 MEK 的無(wú)活性形式結(jié)合，從而阻止上游激酶ji活 MEK1 (IC₅₀ 為 2-7 μM) 和 MEK2 (IC₅₀ 為 50 μM)。PD98059 是一種 ERK1/2 信號(hào)的抑制劑。PD98059 是一種芳烴受體 (AHR) 的配體，可抑制細(xì)胞中 TCDD 結(jié)合 (IC₅₀ 為 4 μM) 和 AHR 轉(zhuǎn)化 (IC₅₀ 為 1 μM)。PD98059 還可抑制細(xì)胞自噬 (autophagy)。

生物活性

PD98059 is a potent and selective MEK inhibitor with an IC₅₀ of 5 μM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC₅₀ of 2-7 μM) and MEK2 (IC₅₀ of 50 μM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC₅₀ of 4 μM) and AHR transformation (IC₅₀ of 1 μM). PD98059 also inhibits autophagy

體外研究(In Vitro)

PD98059 (20 μM; 24 hours) causes G1-phase cell cycle arrest in OCI-AML-3 cells^[4].

PD98059 (10 μM; 22 hours) results in concentration-dependent reductions in the dually phosphorylated forms of ERK1 and ERK2^[1]. PD98059 both prevents ERK activation and blocks formation of TDP-43 and HuR-positive SGs^[7].

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

Cell Cycle Analysis^[4]

Cell Line:	OCI-AML-3 cells
Concentration:	20 μM
Incubation Time:	24 hours
Result:	Caused G1-phase cell cycle arrest.

體內(nèi)研究(In Vivo)

PD98059 (10 mg/kg; i.p.; 1 and 6 hours after Zymosan) significantly reduces the level of p-ERK1/2 in zymosan-injected mice^[3].

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

Animal Model:	Male CD mice^[3]
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; 1 and 6 hours after Zymosan
Result:	Significantly reduced the level of p-ERK1/2.

分子量：267.28

Formula：C₁₆H₁₃NO₃

CAS 號(hào)：167869-21-8

運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式：

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數(shù)據(jù)

DMSO : 33.33 mg/mL (124.70 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	3.7414 mL	18.7070 mL	37.4139 mL
5 mM	0.7483 mL	3.7414 mL	7.4828 mL
10 mM	0.3741 mL	1.8707 mL	3.7414 mL

*

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。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

以下溶解方案都請(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
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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

1.

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (7.78 mM); Suspended solution; Need ultrasonic

參考文獻(xiàn)

[1]. Reiners JJ Jr, et al. PD98059 is an equipotent antagonist of the aryl hydrocarbon receptor and inhibitor of mitogen-activated protein kinase kinase. Mol Pharmacol. 1998 Mar;53(3):438-45.

[2]. Alessi DR, et al. PD 098059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo. J Biol Chem, 1995, 270(46), 27489-27494.

[3]. Jia Luo, et al. DUSP5 (dual-specificity protein phosphatase 5) suppresses BCG-induced autophagy via ERK 1/2 signaling pathway.

[4]. Di Paola R, et al. PD98059, a specific MAP kinase inhibitor, attenuates multiple organ dysfunction syndrome/failure (MODS) induced by zymosan in mice. Pharmacol Res. 2010 Feb;61(2):175-87.

[5]. Kojima K, et al. Mitogen-activated protein kinase kinase inhibition enhances nuclear proapoptotic function of p53 in acute myelogenous leukemia cells. Cancer Res. 2007 Apr 1;67(7):3210-9.

[6]. Kim KY, et al. Inhibition of Autophagy Promotes Salinomycin-Induced Apoptosis via Reactive Oxygen Species-Mediated PI3K/AKT/mTOR and ERK/p38 MAPK-Dependent Signaling in Human Prostate Cancer Cells. Int J Mol Sci. 2017 May 18;18(5). pii: E1088.

[7]. Sarah J Parker, et al. Inhibition of TDP-43 accumulation by bis(thiosemicarbazonato)-copper complexes. PLoS One. 2012;7(8):e42277.

PD98059

PD98059 是一種有效的選擇性的 MEK 抑制劑，IC50 為 5 μM。PD98059 與 MEK 的無(wú)活性形式結(jié)合，從而阻止上游激酶ji活 MEK1 (IC50 為 2-7 μM) 和 MEK2 (IC50 為 50 μM)。PD98059 是一種 ERK1/2 信號(hào)的抑制劑。PD98059 是一種芳烴受體 (AHR) 的配體，可抑制細(xì)胞中 TCDD 結(jié)合 (IC50 為 4 μM) 和 AHR 轉(zhuǎn)化 (IC50 為 1 μM)。PD98059 還可抑制細(xì)胞自噬 (autophagy)。

貨號(hào)：HY-12028
CAS：167869-21-8

品牌：MCE

型號(hào)：HY-12028

起訂量：1

規(guī)格:：5mg

價(jià)格:：￥750

15906629305

在線(xiàn)客服

客服一

產(chǎn)品詳情

PD98059

PD98059 是一種有效的選擇性的 MEK 抑制劑，IC₅₀ 為 5 μM。PD98059 與 MEK 的無(wú)活性形式結(jié)合，從而阻止上游激酶ji活 MEK1 (IC₅₀ 為 2-7 μM) 和 MEK2 (IC₅₀ 為 50 μM)。PD98059 是一種 ERK1/2 信號(hào)的抑制劑。PD98059 是一種芳烴受體 (AHR) 的配體，可抑制細(xì)胞中 TCDD 結(jié)合 (IC₅₀ 為 4 μM) 和 AHR 轉(zhuǎn)化 (IC₅₀ 為 1 μM)。PD98059 還可抑制細(xì)胞自噬 (autophagy)。

生物活性

PD98059 is a potent and selective MEK inhibitor with an IC₅₀ of 5 μM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC₅₀ of 2-7 μM) and MEK2 (IC₅₀ of 50 μM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC₅₀ of 4 μM) and AHR transformation (IC₅₀ of 1 μM). PD98059 also inhibits autophagy

體外研究(In Vitro)

PD98059 (20 μM; 24 hours) causes G1-phase cell cycle arrest in OCI-AML-3 cells^[4].

PD98059 (10 μM; 22 hours) results in concentration-dependent reductions in the dually phosphorylated forms of ERK1 and ERK2^[1]. PD98059 both prevents ERK activation and blocks formation of TDP-43 and HuR-positive SGs^[7].

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

Cell Cycle Analysis^[4]

Cell Line:	OCI-AML-3 cells
Concentration:	20 μM
Incubation Time:	24 hours
Result:	Caused G1-phase cell cycle arrest.

體內(nèi)研究(In Vivo)

PD98059 (10 mg/kg; i.p.; 1 and 6 hours after Zymosan) significantly reduces the level of p-ERK1/2 in zymosan-injected mice^[3].

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

Animal Model:	Male CD mice^[3]
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; 1 and 6 hours after Zymosan
Result:	Significantly reduced the level of p-ERK1/2.

分子量：267.28

Formula：C₁₆H₁₃NO₃

CAS 號(hào)：167869-21-8

運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式：

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數(shù)據(jù)

DMSO : 33.33 mg/mL (124.70 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	3.7414 mL	18.7070 mL	37.4139 mL
5 mM	0.7483 mL	3.7414 mL	7.4828 mL
10 mM	0.3741 mL	1.8707 mL	3.7414 mL

*

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。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

以下溶解方案都請(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
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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶