EGFR Pathway Inhibitor Kit

Catalog No. K1030

A unique collection of 15 inhibitors for studying the EGFR signaling pathway

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  • RAF inhibitors induce dimer formation between KSR and RAF, and activate KSR by CRAF. (A) GDC0879 but not PLX4720 induces BRAF/CRAF dimers. Cells overexpressing myc-CRAF and BRAF were treated with drug for 1 h and CRAF immunoprecipitates were immunoblotted for BRAF and CRAF (epitope tagged with myc). (B) GDC0879 but not PLX4720 enhances KSR/BRAF complexes. KSR immunoprecipitates were prepared from cells overexpressing FLAG-KSR and BRAF after treatment with the indicated drug for 1 h and immunoblotted using antibodies to BRAF. (C) Both GDC0879 and PLX4720 induce KSR/CRAF complexes.KSR immunoprecipitates were prepared from cells overexpressing FLAG-KSR and myc-CRAF after treatment with the indicated drug for 1 h and immunoblotted for CRAF using myc antibodies. (D and E) Requirement of KSR for drug-induced ERK activation. Lysates fromwild-type and KSR deficient fibroblasts, transfected with RASV12, were treated with the indicated doses of either GDC-0879 (D) or PLX4720 (E) for 1 h. Lysates were immunoblotted for phospho-ERK1 and 2, ERK2, and RASV12. (F) KSR and CRAF cooperate to activate MEK. Cells expressing the indicated constructs were treated with a 50 uM PLX4720 for 2 h before cell lysates were prepared and analyzed for pMEK by immunoblotting. CRAF(TM) refers to the T421M gatekeeper mutant that cannot bind to the drug(4). (G) KSR in vitro kinase reactions. Cells were cotransfected with WT or ATP binding deficient KSR and CRAF and immunoprecipitates prepared after cells were treated with an activating dose of PLX (10 uM) for 1 h. KSR immunoprecipitates were prepared, pretreated with 50 uM PLX4720 to inhibit coprecipitating RAF activity, and then tested for kinase activity using purified MEK. MEK phosphorylation was detected using a pMEK specific antibody.

    A, ANOVA of IC50 values of the dual PI3K/mTOR inhibitor NVP-BEZ235 in 23 melanoma cell lines showing no significant difference in sensitivity to this compound in B-Raf mutant and Braf wild-type cells. B, decreases in pAkt and pP70S6K in a dose and time-dependent fashion in 2 melanoma cell lines treated with NVP-BEZ235. pP70S6K levels are undetectable at all concentrations and time points studied, whereas levels of pAkt start rising again after 4 hours of drug exposure in a dose-dependent fashion. C, clonogenic assays in 2 melanoma cell lines (YUVON and YUSIK) treated with NVP-BEZ235 at different concentrations. NVPBEZ235 was effective in inhibiting colony formation at low nanomolar concentrations.

  • Confocal microscopy images of NO formation. DAF 2 DA-loaded washed platelets (1.0109 platelets/mL) were preincubated at 378C with saline (A), and then stimulated for 1min with 0.1 (B), 1.0 (C) or 10 (D) mM AEA. In Panel (E–F–G) washed platelets were preincubated with 1 mM SR1 (E), 1 Mm MK2206 (F) or 20 mM LY294002 (G), and then stimulated for 1min with 1.0 mM AEA. In panel (H) is reported the effect of 5 mg/mL collagen, used as a positive control. All the experiments were carried out in the presence of 100 mM L-arginine. NO formation was visualized by confocal microscropy as detailed in Methods.

    Inhibition of anchorage-independent growth of lung tumor cell lines by selected inhibitors. Each selected cell line was treated with the indicated inhibitor at 0.1 μM and 1 μM concentrations for two weeks and cell colony size formation was scored under the Nikon inverted-phase microscope.

  • (a) Western blots examine the effects of WZ4002 alone or a combination of WZ4002 and ABT-263 in H1975 parental or SR cells in suspension. Cells were grown for 48 h and then treated with the indicated pharmacological agent(s) for another 24 h. The cleaved/total poly (ADP-ribose) polymerase-1 (PARP-1) ratio determined for each cell line using Image J software is also represented. The values are the means of three independent experiments. (b) Quantification of apoptotic cells assessed by PARP-1 cleavage from each cell line.

    ERK activation is increased in Il6ra2/2 mice compared with WT mice. A, Total and phosphorylated (p) Stat3 and ERK were assessed in small punch biopsy wounds collected after 30 min (Stat3) or 1 d (ERK) by Western blotting. Densitometry results for the blots are provided to the right. pp , 0.05. B, Total and p-ERKs were assessed in small wounds generated in WTand Il6ra2/2 mice treated topically with vehicle (DMSO) or with the MEK inhibitor U0126.Wounds were harvested after 1 d, and western blotting was performed on lysates. C, Wound contraction was assessed macroscopically in large wounds of WT (left panel) and Il6ra2/2 mice treated daily with vehicle (DMSO) or U0126. pp , 0.05.

  • A, effects of p38 inhibitor SB203580 (1, 5, and 10 M) on SRP72 protein expression was evaluated by WB using antibodies against human SRP72,SRP54, and GAPDH. A decreased intensity of SRP72 bands was noted when using the inhibitor at 5M concentration at 240 min (lane 6) and 10M at 120 and 240 min (lanes 8 and 9). B, results were analyzed and RUA illustrated, finding significant results at 5M, 240 versus 0 min, and 10M, 240 versus 0 and 120 versus 0 min, respectively, (p0.05).

    Inhibition of the MAPK signaling pathway results in downregulation of Plk-1 protein expression. (a) WB analysis for Plk-1 protein after treatment of human melanoma cell lines M14 and WM-115 with MEK 1/2 inhibitor PD98059 (10 mM), JNK inhibitor (16 mM), p38 inhibitor SB203580 (20 mM), and multikinase inhibitor sorafenib (10 mM) for 48 h showing significant reduction in the expression of Plk-1 protein after 48 hours. (b) Annexin V/PI staining of cells treated with MAPK inhibitors and induction of apoptosis. JNK, c-Jun N-terminal kinase; MAPK, mitogen-activated protein kinase; MEK 1/2, mitogen-activated protein kinase kinase 1/2; Plk-1, polo-like kinase 1; WB, western blot.

Product Overview

A unique collection of 15 potent and selective inhibitors for studying the EGFR signaling pathway. This kit contains the following inhibitors:

Product Details

Formulation: A unique collection of 15 inhibitors for studying the EGFR signaling pathway supplied as lyophilized powder
Container: Screw Cap Micro Tubes of WATSON
Stability: Powder -20°C 2 years
In DMSO -80°C 6 months
Shipping: Blue ice
Packaging: Inert gas

Data

Cat.No. Product Name Targets and IC50s Suggested Solvent Amount Supplied
S1078 MK-2206 dihydrochloride A highly selective inhibitor of Akt. Akt1, IC50=8 nM; Akt2, IC50=12 nM; Akt3, IC50=65 nM. DMSO 96 mg/mL
Water 96 mg/mL
5 mg
S1023 Erlotinib HCl A hydrochloride acid salt form of Erlotinib which is a HER1/EGFR tyrosine kinase inhibitor for HER1/EGFR tyrosine kinase with an IC50 of 2 nM. DMSO 3 mg/mL 100 mg
S1173 WZ4002 A novel mutant-selective EGFR kinase inhibitor of EGFRL858R and EGFRL858R/T790M with IC50s of 2 nM and 8 nM, respectively. DMSO 13 mg/mL 10 mg
S1460 SP600125 A broad-spectrum serine/threonine kinase inhibitor of JNK with an IC50 range from 40 to 90 nM. DMSO 44 mg/mL 10 mg
S1009 BEZ235 (NVP-BEZ235) A dual ATP-competitive inhibitor of PI3K and mTOR. p110α, IC50=4 nM; p110β, IC50=75 nM; p110δ, IC50=7 nM; p110γ, IC50=5 nM. DMSO 7 mg/mL 50 mg
S1102 U0126-EtOH (UO126 EtOH) A chemically synthesized and highly selective inhibitor of both MEK1 and MEK2 with IC50s of 70 nM and 60 nM, respectively. DMSO 85 mg/mL 25 mg
S2700 KX2-391 A synthetic, orally bioavailable small molecule and non-ATP competitive Src tyrosine kinase inhibitor with an IC50 of average 72 nM. DMSO 86 mg/mL 5 mg
S1076 SB 203580 A p38 MAPK inhibitor with an IC50 range of 0.3-0.5 µM and blocks PKB phosphorylation with an IC50 range of 3-5 µM. DMSO 76 mg/mL 25 mg
S1378 Ruxolitinib (INCB018424) A JAK family kinase inhibitor of JAK1, JAK2 and JAK3 with IC50s of 2.7 nM, 4.5 nM and 322 nM, respectively DMSO 61 mg/mL 5 mg
S1040 Sorafenib (Nexavar) A small molecular inhibitor of VEGFR, PDGFR, c-Raf and B-Raf with IC50s of 18 nM, 10 nM, 3 nM and 15 nM, respectively. DMSO 127 mg/mL 5 mg
S1152 PLX-4720 A potent and selective inhibitor of B-RafV600E and c-Raf-1Y340D/Y341D with IC50s of 13 nM and 6.7 nM, respectively. DMSO 83 mg/mL 10 mg
S1155 NSC 74859 (S3I-201) A chemical probe inhibitor of STAT3 with an IC50 of 86 µM. DMSO 73 mg/mL 5 mg
S2672 PF-00562271(PF-562271) A potent, ATP-competitive and reversible inhibitor of FAK and Pyk2 catalytic activity with IC50s of 1.5 nM and 14 nM, respectively. DMSO 5 mg/mL 5 mg
S2791 Sotrastaurin (AEB071) A potent selective pan-PKC inhibitor and highly inhibits PKCθ with a Ki of 0.22 nM. DMSO 87 mg/mL 5 mg
S2634 DCC-2036 (Rebastinib) A conformational control inhibitor of Abl1 and Abl1-T315I with IC50s of 0.8 nM and 4 nM, respectively. DMSO 111 mg/mL 10 mg

Research Area

Other Inhibitor Kits