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

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Product Description

Description & Advantages

    • A unique collection of 355 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 355 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 Reviews (10)

AS-605240 Review
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Rating
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, 2012, 483(7387):100-3. Vemurafenib (PLX4032, RG7204) purchased from Selleck
Method Colony formation assay
Cell Lines Thyroid cancer (8505C)/CRC (OXCO-1, COLO741 and WiDr)/melanoma (A375) cells
Concentrations 0/0.15/0.31/0.63/1/25 uM
Incubation Time 10-14 days
Results Of the ten colorectal cancer cell lines examined, eight express much higher levels of EGFR, but in two (COLO-741 and OXCO-1) EGFR levels were as low as those seen in melanoma. All three thyroid cancer cell lines expressed EGFR at significant levels. When we tested the two EGFRlow CRC cell lines for their response to PLX4032, we found them to be almost as sensitive as the melanoma cell line A375 in both short-term assays and long-term assays.

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Rating
Source Nature, 2012, 483(7387):100-3. Vemurafenib (PLX4032, RG7204) purchased from Selleck
Method Western blot
Cell Lines PC9GR4/WZR10 cells
Concentrations 1 uM
Incubation Time 72 h
Results Co-treatment of these cells with a combination of PLX4032 and either cetuximab or gefitinib prevented this feedback activation of EGFR. PLX4032 treatment inhibited MEK and ERK activation downstream of BRAF but activated AKT, which acts downstream of EGFR in a pathway parallel to BRAF. We note that in all three cell lines treatment with BRAF and EGFR inhibitors caused a more complete inhibition of AKT, MEK and ERK signalling as compared to PLX4032 monotherapy, providing a rationale for the observed synergy in growth assays.

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Rating
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, 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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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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Rating
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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Rating
Source Cell , 2010, 142, 444–455. VX-680 (Tozasertib, MK-0457) purchased from Selleck
Method Immunofluorescence Microscopy
Cell Lines HeLa cells
Concentrations
Incubation Time
Results Inhibition of Aurora kinases with VX-680 sharply reduced kinetochore-localized pT422 signal (Figure G). When normalized to the total level of CENP-E at the kinetochore (which is also reduced in VX-680 treated cells (Ditchfield et al. 2003)), a > 90% reduction in T422 phosphorylation was seen following VX-680 treatment ( Figure H).

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Rating
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.

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Source Nat Genet, 2014, 46(4), 364-70. Rapamycin (Sirolimus) purchased from Selleck
Method Western blot
Cell Lines Persister cells
Concentrations 10 nM
Incubation Time 3 days
Results While added with a specific mTOR inhibitor, rapamycin(Rapa), it inhibitied endogenous mTOR activity, showed that markedly reduced MYC protein levels in persister cells but not in naive T-ALL cells.

Product Citations (21)

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Tags: phosphatase inhibitor library