Rabbit anti-MEK1(S218/222) Polyclonal Antibody

Rabbit anti-MEK1(S218/222) Polyclonal Antibody描述别名宿主特异性反应种属预测反应种属应用分子量类型同种型储存/保存方法存储溶液研究领域背景说明细胞定位UniProt参考文献

概述
描述
Peptide Affinity Purified Rabbit Polyclonal Antibody (Pab)
别名
MEK1抗体;Dual specificity mitogen-activated protein kinase kinase 1; MAP kinase kinase 1; MAPKK 1; MKK1; ERK activator kinase 1; MAPK/ERK kinase 1; MEK 1; MAP2K1; MEK1; PRKMK1
宿主
Rabbit
特异性
This MEK1 antibody is generated from rabbits immunized with a KLH conjugated synthetic peptide between 199-234 amino acids from human MEK1.
反应种属
Human
预测反应种属
D, Ha, M, Rb, R, X, C
应用
WB~~1:1000
分子量
Predicted molecular weight: 43kD
Disclaimer note: The observed molecular weight of the protein may vary from the listed predicted molecular weight due to post translational modifications, post translation cleavages, relative charges, and other experimental factors.
性能
类型
Polyclonal Antibody
同种型
Rabbit Ig
储存/保存方法
Maintain refrigerated at 2-8°C for up to 2 weeks. For long term storage store at -20°C in small aliquots to prevent freeze-thaw cycles.
存储溶液
Purified polyclonal antibody supplied in PBS with 0.09% (W/V) sodium azide. This antibody is purified through a protein A column, followed by peptide affinity purification.
研究领域
Developmental Biology;Signal Transduction
靶标
背景说明
Dual specificity protein kinase which acts as an essential component of the MAP kinase signal transduction pathway. Binding of extracellular ligands such as growth factors, cytokines and hormones to their cell-surface receptors activates RAS and this initiates RAF1 activation. RAF1 then further activates the dual-specificity protein kinases MAP2K1/MEK1 and MAP2K2/MEK2. Both MAP2K1/MEK1 and MAP2K2/MEK2 function specifically in the MAPK/ERK cascade, and catalyze the concomitant phosphorylation of a threonine and a tyrosine residue in a Thr-Glu-Tyr sequence located in the extracellular signal-regulated kinases MAPK3/ERK1 and MAPK1/ERK2, leading to their activation and further transduction of the signal within the MAPK/ERK cascade. Depending on the cellular context, this pathway mediates diverse biological functions such as cell growth, adhesion, survival and differentiation, predominantly through the regulation of transcription, metabolism and cytoskeletal rearrangements. One target of the MAPK/ERK cascade is peroxisome proliferator- activated receptor gamma (PPARG), a nuclear receptor that promotes differentiation and apoptosis. MAP2K1/MEK1 has been shown to export PPARG from the nucleus. The MAPK/ERK cascade is also involved in the regulation of endosomal dynamics, including lysosome processing and endosome cycling through the perinuclear recycling compartment (PNRC), as well as in the fragmentation of the Golgi apparatus during mitosis.
细胞定位
Cytoplasm, cytoskeleton, microtubule organizing center, centrosome. Cytoplasm, cytoskeleton, microtubule organizing center, spindle pole body. Cytoplasm Nucleus. Note=Localizes at centrosomes during prometaphase, midzone during anaphase and midbody during telophase/cytokinesis
UniProt
Q02750
参考文献
参考文献
Zheng, B., et al., Blood 102(3):1019-1027 (2003).
Li, S.P., et al., Cancer Res. 63(13):3473-3477 (2003).
Zhu, X., et al., J. Neurochem. 86(1):136-142 (2003).
Fringer, J., et al., J. Biol. Chem. 278(23):20612-20617 (2003).
Witowsky, J.A., et al., J. Biol. Chem. 278(3):1403-1406 (2003).

实验结果图

Rabbit anti-MEK1(S218/222) Polyclonal Antibody

Western blot analysis of lysate from rat C6 cell line, using MEK1 Antibody (S218/222)(Cat. #JP111450). JP111450 was diluted at 1:1000. A goat anti-rabbit IgG H&L(HRP) at 1:5000 dilution was used as the secondary antibody. Lysate at 35ug.

Rabbit anti-MEK1(S218/222) Polyclonal Antibody

Western blot analysis of anti-MEK1 Antibody (S218/222) (Cat.#JP111450) in A2058, A375 cell line lysates (35ug/lane). MEK1 (arrow) was detected using the purified Pab.

PD0325901

PD0325901

货号:
IP1310

品牌:
Jinpan

PD0325901

暂无详情
产品简介
EC EINECS 687-152-7
别名 N-[(2R)-2,3-二羟基丙氧基]-3,4-二氟-2-[(2-氟-4-碘苯)氨基]苯甲酰胺
英文名称 PD0325901
CAS 391210-10-9
分子式 C16H14F3IN2O4
分子量 482.19
纯度 ≥98%
单位
生物活性 PD0325901是选择性,可渗透细胞的 MEK 抑制剂, IC50为0.33 nM。[1-2]
IC50 MEK1:0.33 nM
In Vitro PD0325901对于纯化的MEK具有极好的特异性和高效性,显示出针对活化的MEK1和MEK2的1nM的Kiapp。就其对ERK1和ERK2的磷酸化的细胞作用而言,PD0325901的效力比CI-1040大约高500倍,显示亚纳摩尔活性。 PD0325901可防止黑素瘤细胞系的生长。 PD0325901抑制TPC-1细胞和K2细胞的生长,GC50分别为11 nM和6.3 nM。 PD0325901显著阻止具有极低浓度(10nM)的BRAF突变的PTC细胞的生长,并且仅在相同浓度下适度增加携带RET/PTC1重排的PTC细胞的生长。 PD0325901有效抑制多个PTC细胞系中ERK1/2的磷酸化[2]。
In Vivo PD0325901(25mg/kg,po)在给药后24小时抑制ERK的磷酸化超过50%。产生70%完全肿瘤反应(C26模型)所需的剂量为25mg/kg /天,而PD0325901和CI-1040分别为900mg/kg /天。已经证明PD 0325901的抗癌活性用于广谱的人肿瘤异种移植物。在小鼠中处理PD0325901(20-25mg/kg /天,po),显示没有接种具有BRAF突变的PTC细胞的肿瘤生长。对于具有RET/PTC1重排的PTC,与对照相比,原位肿瘤的平均肿瘤体积减少了58%。携带BRAF突变的PTC细胞对PD0325901的敏感性高于携带RET/PTC1重排的PTC细胞[2]。
激酶实验 在含有p44MAP激酶(GST-MAPK)的谷胱甘肽S-转移酶融合蛋白和含有p45MEK(GST-MEK)的谷胱甘肽S-转移酶蛋白的存在下测定32P掺入髓鞘碱性蛋白(MBP)。该测定溶液含有20mM HEPES,pH 7.4,10mM MgCl 2,1mM MnCl 2,1mM EGTA,50mM [γ-32P] ATP,10mg GST-MEK,0.5mg GST-MAPK和40mg MBP。体积为100毫升。 20分钟后,通过加入三氯乙酸终止反应,并通过GF/C过滤垫过滤。保留在过滤垫上的32P使用1205 Betaplate测定。在各种剂量范围评估PD0325901以确定剂量反应曲线。
SMILES O=C(C1=CC=C(C(F)=C1NC2=CC=C(I)C=C2F)F)NOC[C@H](O)CO
靶点 MEK
动物实验 将用表达荧光素酶的逆转录病毒(5μLRPMI1640培养基中的5×10 5个细胞)稳定感染的K2和TPC-1细胞接种到甲状腺中,并使用Living Image 3.0软件每周监测小鼠的Xenogen肿瘤生长。接种一周后,通过超声处理将PD0325901溶解于80mM柠檬酸缓冲液(pH7)中,并通过口服强饲法(20-25mg/kg)每天给予小鼠3周(连续5天/周)。对照小鼠单独给予80mM柠檬酸缓冲液(pH 7)。所有体内实验至少进行两次。
细胞实验 将PTC细胞(1×104)接种在含有1mL培养基的24孔板中,在37℃培养箱中培养4天。在第0天将不同浓度的MEK抑制剂PD0325901一式三份加入细胞中。在第2天将溶于0.8%NaCl溶液中的5mg/mL MTT加入到每个孔(0.2mL)中以测试GC50或每天用于细胞生长曲线。
数据来源文献 [1]. Barrett SD, et al. The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6501-4.
[2]. Henderson YC, et al. MEK inhibitor PD0325901 significantly reduces the growth of papillary thyroid carcinoma cells in vitro and in vivo. Mol Cancer Ther. 2010 Jul;9(7):1968-76.
规格 10mg 50mg 100mg

PD0325901是选择性的 MEK 抑制剂。

BIX 02189

BIX 02189

货号:
IB0970

品牌:
Jinpan

BIX 02189

暂无详情

BIX 02189

暂无详情
产品简介
别名 MEK5/ERK5抑制剂
英文名称 BIX 02189
CAS 1094614-85-3
分子式 C27H28N4O2
分子量 440.54
纯度 ≥99%
单位
生物活性 BIX02189是一种选择性的MEK5抑制剂,无细胞试验中IC50为1.5 nM,也抑制ERK5催化活性,IC50为59 nM,且不抑制密切相关的激酶MEK1,MEK2,ERK2,和JNK2。[1]
IC50 MEK5: 1.5 nM [1]
In Vitro BIX02189抑制MEK5和ERK5催化活性,IC50分别为1.5 nM和59 nM。BIX02189抑制CSF1R(FMS),IC50为46 nM,但是作用于相关激酶MEK1,MEK2,ERK1,p38α,JNK2,EGFR,和STK16没有活性,IC50 >3.7 μM。用BIX02189预处理HeLa细胞,抑制山梨醇诱导的ERK5磷酸化,这种作用存在剂量依赖性,但是不会抑制ERK1/2,p38,和JNK1/2 MAPKs磷酸化。BIX02189单独处理HeLa或HEK293细胞24小时,没有毒性。BIX02189作用于HeLa和HEK293细胞,抑制MEK5/ERK5/MEF2C驱动的萤光素酶表达,IC50分别为 0.53 μM和0.26 μM。[1]
SMILES O=C(C1=CC(NC/2=O)=C(C=C1)C2=C(NC3=CC=CC(CN(C)C)=C3)/C4=CC=CC=C4)N(C)C
靶点 MEK inhibitor
数据来源文献 [1] Tatake RJ, et al. Biochem Biophys Res Commun, 2008, 377(1), 120-125.
规格 5mg 10mg 50mg

BIX02189是一种选择性的MEK5抑制剂。

BIX 02188

BIX 02188

货号:
IB0960

品牌:
Jinpan

BIX 02188

暂无详情

BIX 02188

暂无详情
产品简介
MDL MFCD14584538
别名 MEK5抑制剂
英文名称 BIX 02188
CAS 1094614-84-2
分子式 C25H24N4O2
分子量 412.48
纯度 ≥99%
单位
生物活性 BIX 02188是一种选择性的MEK5抑制剂,IC50为4.3 nM,也抑制ERK5催化活性,IC50为810 nM,且不抑制与其密切相关的激酶MEK1, MEK2, ERK2,和JNK2。[1-2]
IC50 MEK5: 4.3 nM [1]
In Vitro BIX02188明显抑制MEK5催化活性,IC50为4.3 nM, 轻微抑制ERK5催化活性,IC50为0.83 μM,作用于关系密切的激酶MEK1,MEK2,ERK1,p38α,JNK2,TGFβR1,EGFR,和STK16没有活性,作用于TGFβR1时IC50为1.8 μM,作用于p38α时IC50为3.9 μM,作用于其他激酶IC50值都大于6.3 μM。用BIX02188预处理HeLa细胞,抑制山梨醇诱导的ERK5磷酸化,这种作用存在剂量依赖性,但是不会抑制ERK1/2,p38,和JNK1/2 MAPKs磷酸化。BIX02188单独处理HeLa或HEK293细胞24小时,没有毒性。 BIX02188作用于HeLa和HEK293细胞,通过在持续激活的MEK5/ERK5/MEF2C驱动的萤光素酶表达系统中的MEK5/ERK5信号级联反应抑制MEF2C转录激活,IC50分别为 1.15 μM 和0.82 μM。[1] BIX02188作用于 300 μM H2O2刺激的牛肺微血管内皮细胞(BLMECs),抑制BMK1磷酸化,这种作用存在剂量依赖性,IC50为0.8 μM, 尤其通过抑制MEK5 信号通路。[2]
SMILES O=C(C1=CC(NC/2=O)=C(C=C1)C2=C(NC3=CC=CC(CN(C)C)=C3)/C4=CC=CC=C4)N
靶点 MEK inhibitor
数据来源文献 [1] Tatake RJ, et al. Biochem Biophys Res Commun, 2008, 377(1), 120-125.
[2] Li L, et al. Biochem Biophys Res Commun, 2008, 370(1), 159
规格 5mg 10mg 50mg

BIX 02188是一种选择性的MEK5抑制剂。

Refametinib;瑞法替尼

Refametinib;瑞法替尼

货号:
IR0430

品牌:
Jinpan

Refametinib;瑞法替尼

暂无详情
产品简介
别名 BAY86-9766;RDEA119
英文名称 Refametinib
CAS 923032-37-5
分子式 C19H20F3IN2O5S
分子量 572.34
纯度 Purity≥98%
单位
生物活性 Refametinib 是一种有效的选择性 MEK1/MEK2 抑制剂,IC50 分别为 19 nM 和 47 nM[1]。
IC50 MEK1:19 nM ; MEK2:47 nM [1]
In Vitro Refametinib选择性地直接结合MEK1 / 2酶中的变构袋。 Refametinib以非ATP竞争性方式(MEK1 IC 50 = 19 nM,MEK2 IC 50 = 47 nM)有效抑制酶抑制测定中的MEK活性,通过将来自ATP的放射性磷酸盐掺入ERK作为底物来确定。 Refametinib有效抑制MEK活性,如通过ERK1 / 2在不同组织来源的几种人癌细胞系和BRAF突变状态的磷酸化所测量的,EC50值范围为2.5至15.8nM。 Refametinib抑制具有功能获得性V600E BRAF突变体的人癌细胞系的贴壁依赖性生长,GI50值范围为67至89nM。相比之下,Refametinib对具有野生型BRAF(A431细胞)或携带BRAF突变G464V的MDA-MB-231细胞的细胞系具有显著较低的生长抑制效力,其显示出固有激酶活性的最小(<2倍增加)增强。 。在不依赖锚定的条件下,所测试的所有细胞系的GI 50值相似(40-84nM)。在锚定非依赖性条件下,MDA-MB-231和A431细胞对Refametinib显著更敏感[1]。
In Vivo Refametinib是一种口服,有效,非ATP竞争性,高选择性MEK1/2抑制剂,在人肿瘤异种移植模型中具有活性,在动物的治疗暴露范围内具有良好的耐受性。发现黑素瘤A375肿瘤异种移植物对Refametinib治疗敏感,在每日一次×14时间表上以25和50mg/kg/d口服给予54%和68%肿瘤生长抑制(TGI)。在这种每日一次的时间表中,在A375肿瘤中也观察到显著的肿瘤生长延迟(TGD)和消退。例如,观察到五到八个完全或部分反应(CR/PR)和多达六个无肿瘤幸存者(TFS)。每隔一天以100mg/kg给予Refametinib的效果不如每日给药25或50mg/kg。当Refametinib按每日两次的时间表给药时,它比每日一次的时间表更有效[1]。
SMILES O=S(C1(C[C@H](O)CO)CC1)(NC(C(NC(C(F)=C2)=CC=C2I)=C3F)=C(OC)C=C3F)=O
靶点 MEK
动物实验 小鼠[1]雌性无胸腺裸鼠用于所有功效研究,除了使用雄性小鼠的Colo205研究2。小鼠皮下注射1×106个肿瘤细胞(Colo205和A431)或~1mm3肿瘤碎片(A375和HT-29)。通过卡尺测量监测肿瘤体积。对于功效分析,当肿瘤为80至185mm 3时开始治疗。 Refametinib(25和50 mg/kg/d)通过口服强饲法每日一次或每日两次,持续14 d,或每2 d一次,共14次[1]。
细胞实验 对于贴壁依赖性生长抑制实验,将A375,SK-Mel-28,A431,Colo205,HT-29,MDA-MB-231和BxPC3细胞系以1,000 /20μL/孔接种于白色384孔板中或白色96孔微孔板,4,000 /100μL/孔。在37℃,5%CO 2和100%湿度下孵育24小时后,将Refametinib在37℃温育48小时并使用CellTiter-Glo进行测定。
数据来源文献 [1]. Iverson C, et al. RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer. Cancer Res. 2009 Sep 1;69(17):6839-47
规格 5mg 10mg

Refametinib 是一种有效的选择性 MEK1/MEK2 抑制剂

Rabbit anti-MEK1 Polyclonal Antibody(Center S217/221)

Rabbit anti-MEK1 Polyclonal Antibody(Center S217/221)别名宿主特异性反应种属预测反应种属应用分子量类型同种型储存/保存方法背景说明参考文献

概述
别名
MEK1抗体;Dual specificity mitogen-activated protein kinase kinase 1; MAP kinase kinase 1; MAPKK 1; MKK1; ERK activator kinase 1; MAPK/ERK kinase 1; MEK 1; MAP2K1; MEK1; PRKMK1
宿主
Rabbit
特异性
This MEK1 antibody is generated from rabbits immunized with a KLH conjugated synthetic peptide between 200-227 amino acids from the Central region of human MEK1.
反应种属
Human, Mouse, Rat
预测反应种属
Drosophila, C.Elegans, Hamster, Rabbit, Rat, Xenopus, Chicken
应用
WB
分子量
Predicted molecular weight: 43kD
Disclaimer note: The observed molecular weight of the protein may vary from the listed predicted molecular weight due to post translational modifications, post translation cleavages, relative charges, and other experimental factors.
性能
类型
Polyclonal Antibody
同种型
Rabbit Ig
储存/保存方法
Maintain refrigerated at 2-8°C for up to 2 weeks. For long term storage store at -20°C in small aliquots to prevent freeze-thaw cycles.
靶标
背景说明
The protein encoded by this gene is a member of the dual
specificity protein kinase family, which acts as a
mitogen-activated protein (MAP) kinase kinase. MAP kinases, also
known as extracellular signal-regulated kinases (ERKs), act as an
integration point for multiple biochemical signals. This protein
kinase lies upstream of MAP kinases and stimulates the enzymatic
activity of MAP kinases upon wide variety of extra- and
intracellular signals. As an essential component of MAP kinase
signal transduction pathway, this kinase is involved in many
cellular processes such as proliferation, differentiation,
transcription regulation and development.
参考文献
参考文献
Liang, Q., et al. J. Immunol. 185(10):5704-5713(2010)
Yokoyama, T., et al. Blood 116(15):2768-2775(2010)
Klemke, M., et al. EMBO J. 29(17):2915-2929(2010)
Shang, C., et al. Med. Sci. Monit. 16 (6), BR168-BR173 (2010) :
Sasaki, H., et al. J Thorac Oncol 5(皪Ỵ皫㟹皩腙癹