96 Well Format Sample Storage Tube With Screw Cap and Optional 2D Barcode

MAPK Inhibitor Library

A unique collection of 61 MAPK signaling pathway inhibitors

规格 价格  
预溶于DMSO
100uL/well (10mM solution) RMB 13738.73
2x100uL/well (10mM solution) RMB 20251.24
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产品详情

产品描述及优势

    A unique collection of 61 small molecule inhibitors used for MAPK signaling research.
    Targets MEK,Raf,p38 MAPK,JNK,ERK, etc.
    • Structurally diverse, medicinally active, and cell permeable.
    • Rich documentation with structure, IC50, and customer reviews.
    NMR and HPLC validated to ensure high purity.

产品详细信息

配制: A unique collection of 61 MAPK signaling pathway inhibitors supplied as pre-dissolved DMSO solutions
96-孔板: 96 Well Format Sample Storage Tube With Screw Cap and Optional 2D Barcode
稳定性:
1年 -20°C 溶于DMSO
2年 -80°C 溶于DMSO
发货: 蓝冰物流
包装: 惰性气体

化合物库组成成份

Chemical Library Composition

客户使用Selleck产品的实验数据 (10)

AS-605240 Review
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数据来源 Nature,2015, 520(7547), 368-72. Vemurafenib (PLX4032, RG7204) purchased from Selleck
方法 Animal studies
细胞系 A375 tumours
浓度 10 mg/kg
处理时间 4, 5 days
结果 Although vemurafenib treatment decreased the volume of sensitive tumours (A375 alone)(b), Green fluorescent protein (GFP) staining confirmed increased numbers of resistant cells in regressing tumours, and EdU or BrdU staining confirmed their increased proliferation rate compared to the vehicletreated controls (c). Tumours comprising only resistant cells showed no growth difference when treated with vehicle or vemurafenib (d), indicating that the growth advantage of resistant cells in regressing tumours was not caused by direct effects of vemurafenib on cancer or stromal cells. In line with these findings, A375R cells co-implanted with other vemurafenib-sensitive melanoma cell lines (Colo800, LOX and UACC62) also showed an up toeightfold growthincreasecompared to vehicle-treated control groups (e). Local growth acceleration of resistant cells in the regressing subcutaneous tumours resulted in higher lung metastatic burden (f).
Axitinib and PF2341066(Crizotinib) Reviews
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数据来源 Nature 2015, 520(7547), 368-72. Vemurafenib (PLX4032, RG7204) purchased from Selleck
方法 Immunofluorescence staining
细胞系 A375/A375R tumours
浓度 0.1-1 uM
处理时间 5 days
结果 This analysis highlighted FRA1 (also known FOSL1), a member of the AP1 transcription factor complex and effector of the ERK pathway27, as one of the putative upstream regulators of the TIS .FRA1 was downregulated in all drug-sensitive cells, but not in resistan cells, treated with vemurafenib, crizotinib and erlotinib (c, d).
Axitinib and PF2341066(Crizotinib) Reviews
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数据来源 Nature 2015, 517(7534), 391-5. PD0325901 purchased from Selleck
方法 Western blot
细胞系 Metabolic
浓度 10 mg/kg
处理时间 5 days
结果 PD0325901 caused a decrease in PPARc phosphorylation at S112 and S273, confirming the established role of ERKs in regulating S112 and strongly suggesting a new role in regulating S273 (refs 22-24).
Axitinib and PF2341066(Crizotinib) Reviews
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数据来源 Nature 2014, 510(7504), 283-7. Trametinib (GSK1120212) purchased from Selleck
方法 HE staining, IHC
细胞系 Smyd3 mutant mice
浓度 1 mg/kg
处理时间 7 days
结果 Administration of Kras and Kras;Smyd3 mutant mice with a normal dose of Trametinib blocked tumorigenesis in both strains, though phosphorylation of ERK1/2 was still lower in mice depleted of SMYD3. Notably, a low dose Trametinib regimen, which only partially inhibited pERK1/2 levels and the formation of neoplastic lesions in Kras mutant mice, was sufficient to block tumorigenesis and ERK1/2 activation in Smyd3 knockouts.
Axitinib and PF2341066(Crizotinib) Reviews
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数据来源 Nature 2010, 468, 968-972. Selumetinib (AZD6244) purchased from Selleck
方法 Immunoblotting
细胞系 A375 cells
浓度 1 μM
处理时间
结果 Ectopic COT expression in A375 and SKMEL28 cells also conferred decreased sensitivity to the MEK inhibitors CI-1040 and AZD6244, suggesting that COT expression alone was sufficient to induce this phenotype. In the setting of ectopic COT expression, exposure to AZD6244 or CI-1040 in combination with PLX470 (1 μM each) reduced cell growth and pERK expression more effectively than did single-agent PLX4720, even at concentrations of 10 μM.
Axitinib and PF2341066(Crizotinib) Reviews
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数据来源 Nature 2010, 468, 973-977. Selumetinib (AZD6244) purchased from Selleck
方法 Survival Assay
细胞系 isogenic cell
浓度 0.01-10 μM
处理时间 72 h
结果 The growth of M249 R4 and Pt55 R was sensitive to MEK inhibition in the presence of PLX4032
Axitinib and PF2341066(Crizotinib) Reviews
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数据来源 Science 2011, 331, 912-916. PD184352 (CI-1040) purchased from Selleck
方法 Immunohistochemistry
细胞系 Hand2d/d mice
浓度
处理时间 24h
结果 The epithelia of vehicle-treated horn showed prominent expression of p-FRS2 and p-ERK1/2(Fig.A,a and c). However, the levels of both p -FRS2 and p -ERK1/2 were reduced in the epithelia of PD173074-treated horn on day 4 of pregnancy (Fig. A, b and d). We also observed a marked decline in the proliferative activity of Hand2-null uterine epithelia, as indicated by decreased Ki-67 staining (Fig. A, e and f) . In parallel experiments, administration of PD184352, an inhibitor of the ERK1/2 pathway, to uterine horns of Hand2 d/d mice suppressed the level of pERK1/2 (Fig.B, a and b) , as well as luminal epithelial proliferation ( Fig. B, c and d).The ERK1/2-dependent phosphorylation of epithelial ERα at Ser118 is critical for the transcriptional activation of ERα. Administration of either PD173074 (Fig. C, a to d) or PD184352 (Fig. C, e to h) to Hand2-null uterine horns blocked the phosphorylation of epithelial ERα at Ser118 and the expression of Muc -1.
Axitinib and PF2341066(Crizotinib) Reviews
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数据来源 Cell 2012, 149(3), 656-70. AZD8330 purchased from Selleck
方法 Western blotting
细胞系 iKras p53L/+ cells
浓度 50 nM
处理时间 18 h
结果 As shown in Figure, the expression of several glycolytic genes (Glut1, Hk1, Eno1, Ldha), the rate-limiting HBP gene (Gfpt1), as well as a nonoxidative PPP gene (Rpia) are significantly decreased by MEK inhibition (AZD8330) at a dose that exerts a similar effect on ERK phosphorylation as that observed upon doxy withdrawal.
Axitinib and PF2341066(Crizotinib) Reviews
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数据来源 Cancer Discov 2014, 4(2), 232-45. Trametinib (GSK1120212) purchased from Selleck
方法 Immunofluorescence
细胞系 5XMYC cells
浓度 100 nM
处理时间 4, 24, 48 h
结果 Treatment of 5XMYC cells with a MEK inhibitor (GSK1120212/trametinib) resulted in the formation of polarized normal acini, as observed by immunofluorescence for basal (CK5, vimentin), luminal (CK8, e-cadherin), and a tight-junction marker (ZO-1).
Axitinib and PF2341066(Crizotinib) Reviews
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数据来源 Cancer Discov 2013, 3, 350-62. PLX-4720 purchased from Selleck
方法 Western blot
细胞系 A375 cells
浓度 1 uM
处理时间 16 h
结果 Associated with the increased RAS-GTP, it's observed a concomitant increase in C-RAF activation, as measured by phosphorylation of Ser338. Under conditions of combined C-RAF/NF1 knockdown, ERK phosphorylation was inhibited more effectively compared to knockdown of NF1 alone. Moreover, whereas cyclin D1 levels were inhibited by PLX4720 in A375 cells, but NF1 silencing partially alleviated this effect.

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