IGF Pathway Inhibitor Kit

Catalog No. K1050

A unique collection of 12 inhibitors for studying the IGF signaling pathway

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1ea USD 1130

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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.

    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.

  • 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.

    Mean IL-8 concentrations determined by ELISA of the supernatants of HeLa cells infected with wild-type Salmonella. Kinase inhibitors are indicated on the x axis, and the target families of the inhibitors are indicated above each column. CEC, chelerythrine; Pim Inh, Pim-1 inhibitor 2. Inhibitors that significantly affected IL-8 production relative to the control (P < 0.05, Bonferroni post hoc test from one-way ANOVA) are indicated with an asterisk. Relative cell viability is also shown, as determined by reduction of XTT by viable cells. A450, absorbance at 450 nm.

  • PANC1 cells were treated with GSK3 inhibitors SB216763 (SB 10μM or SB 20μM) or CHIR99021 (CHIR 5μM) for 72h. Cells were lysed and equal amounts of proteins were separated on SDS-PAGE and submitted to Western blot analysis using the indicated antibodies. GS, glycogen synthase.

    mTOR, P70S6K1, 4E-BP1 and PCNA activation in the basilar artery of SAH. Top, Western blotting bands of antibodies, bottom, density of the protein band from each group. A, mTOR activation in the basilar artery demonstrated an elevated expression of mTOR on day 7 following SAH in SAH and SAH+DMSO animals. The mTOR inhibitors, Rapamycin and AZD8055 reduced the enhanced expression of mTOR (pb0.05, ANOVA). B. P70S6K1 activation. C. 4E-BP1 activation. D. PCNA activation. Rapamycin and AZD8055 significantly decreased the expression of P70S6K1, 4E-BP1 and PCNA compared with the SAH and SAH+DMSO (pb0.05, respectively; ANOVA). There was no significant difference between the two inhibitors in mTOR, P70S6K1, 4E-BP1 and PCNA expression.


Cat.No. Product Name Targets and IC50s Suggested Solvent Amount Supplied
S1093 GSK1904529A A selective inhibitor of IGF-1R and IR with IC50s of 27 nM and 25 nM, respectively.   10 mg
S1124 BMS-754807 An IGF-1R inhibitor with an IC50 of 13 nM.   5 mg
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
S2247 BKM120 (NVP-BKM120) A selective Class I PI3K inhibitor of p110α, p110β, p110δ and p110γ with IC50s of 50-300 nM. DMSO 82 mg/mL 5 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
S2791 Sotrastaurin (AEB071) A potent selective pan-PKC inhibitor and highly inhibits PKCθ with a Ki of 0.22 nM. DMSO 87mg/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
S2924 CHIR-99021 (CT99021) HCl CHIR-99021 HCl (CT99021) is hydrochloride of CHIR-99021, which is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. DMSO 3 mg/mL 2 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
S1275 BX-912 A selective potent PDK-1 inhibitor with an IC50 of 12 nM. DMSO 94 mg/mL 2 mg
S1555 AZD8055 A novel ATP-competitive inhibitor of mTOR with an IC50 of 0.8 nM. DMSO 93mg/mL 10 mg

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Chemical Information

Formulation A unique collection of 12 inhibitors for studying the IGF signaling pathway supplied as lyophilized powder
Container Screw Cap Micro Tubes of WATSON
Powder -20℃ 2 years
In DMSO -80℃ 6 months
Shipping Blue ice
Packaging Inert gas

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