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

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Product Use Citation

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Product Description

Description & Advantages

    • A unique collection of 378 kinase inhibitors for high throughput screening (HTS) and high content screening (HCS)
    • Bioactivity and safety confirmed by preclinical research and clinical trials
    • Some inhibitors have been approved by the FDA
    • Targets kinases such as RTKs, PI3K, Aurora Kinase, CDK, and MEK
    • Most are ATP competitive
    • Structurally diverse, medicinally active, and cell permeable
    • Rich documentation with structure, IC50, and customer reviews
    • NMR and HPLC validated to ensure high purity

Product Details

Formulation: A collection of 378 kinase inhibitors supplied as pre-dissolved DMSO solutions
Container: 96 Well Format Sample Storage Tube With Screw Cap and Optional 2D Barcode
Stability:
3 months -20°C in DMSO
6 months -80°C in DMSO
Shipping: Blue ice
Packaging: Inert gas

Kinase Inhibitor Library Contents

Download the Kinase Inhibitor Library - XLSX Download the Kinase Inhibitor Library - SDF

Contents are for reference only and are subject to change without notice.

Kinase Inhibitor Library Composition

Kinase Inhibitor Library Composition

Customer Product Validation (10)

AS-605240 Review
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Rating
Source Nature,2015, 520(7547), 368-72. Vemurafenib (PLX4032, RG7204) purchased from Selleck
Method Animal studies
Cell Lines A375 tumours
Concentrations 10 mg/kg
Incubation Time 4, 5 days
Results 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).

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Source Nature, 2015, 520(7547), 368-72. Vemurafenib (PLX4032, RG7204) purchased from Selleck
Method Immunofluorescence staining
Cell Lines A375/A375R tumours
Concentrations 0.1-1 uM
Incubation Time 5 days
Results 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).

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Source Nature, 2015, 517(7534), 391-5. PD0325901 purchased from Selleck
Method Western blot
Cell Lines Metabolic
Concentrations 10 mg/kg
Incubation Time 5 days
Results 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).

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Source Nature, 2014, 510(7504), 283-7. Trametinib (GSK1120212) purchased from Selleck
Method HE staining, IHC
Cell Lines Smyd3 mutant mice
Concentrations 1 mg/kg
Incubation Time 7 days
Results 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.

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Source Nature, 2014, 508(7494), 118-22. Barasertib (AZD1152-HQPA) purchased from Selleck
Method Long-term cell proliferation assays
Cell Lines A375-SOX10KD cells
Concentrations 0.5 uM
Incubation Time 4 weeks
Results Compared with controls, treatment of A375-SOX10KD cells with a combination of both vemurafenib and GDC0941 lead to proliferation arrest.

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Rating
Source Nature, 2011, 478(7369):349-55. Sunitinib Malate purchased from Selleck
Method Immunofluorescent staining
Cell Lines Mouse pancreatic stem cells
Concentrations 12 uM
Incubation Time 2 days
Results Compared to vehicle-exposed controls, juvenile islets exposed to PDGF-AA had a sixfold increase of β-cell BrdU incorporation, an effect eliminated by simultaneous exposure to Sunitinib or U0126.

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Source Nature, 2011, 478(7369):349-55. Sunitinib Malate purchased from Selleck
Method Western immunoblots
Cell Lines Mouse pancreatic stem cells
Concentrations 12 uM
Incubation Time 2 days
Results Increased Ezh2 expression and β-cell BrdU incorporation were eliminated by simultaneous treatment with the receptor tyrosine kinase inhibitors Sunitinib.

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Rating
Source Nature, 2010, 468, 968-972. Selumetinib (AZD6244) purchased from Selleck
Method Immunoblotting
Cell Lines A375 cells
Concentrations 1 μM
Incubation Time
Results 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.

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Source Nature, 2010, 468, 973-977. Selumetinib (AZD6244) purchased from Selleck
Method Survival Assay
Cell Lines isogenic cell
Concentrations 0.01-10 μM
Incubation Time 72 h
Results The growth of M249 R4 and Pt55 R was sensitive to MEK inhibition in the presence of PLX4032

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Source Science, 2011, 331, 912-916. PD184352 (CI-1040) purchased from Selleck
Method Immunohistochemistry
Cell Lines Hand2d/d mice
Concentrations
Incubation Time 24h
Results 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.

Product Use Citation (32)

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Tags: phosphatase inhibitor library
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