Affinity purified from pooled serum. Learn more.

MerTK Tyr749/753/754 Antibody

Catalog #: p186-749 Category: Datasheet:

$109.00$365.00

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Rabbit Polyclonal Antibody

Pooled Serum
Formulation:
Affinity Purified from Pooled Serum
Species Reactivity:
Avian, Bovine, Canine, Guinea Pig, Human, Mouse, Rat, Non-human primate
Applications:
WB 1:1000
Species:
Rabbit Polyclonal
Gene Name:
MERTK
Molecular Weight:
160 kD
Cite This Antibody:
PhosphoSolutions Cat# p186-749: RRID:AB_2744537
Antigen/Purification: ExpandCollapse

Phosphopeptide corresponding to amino acid residues surrounding the phospho-Tyr749/753/754 of human MerTK.

Prepared from pooled rabbit serum by affinity purification via sequential chromatography on phospho and non-phosphopeptide affinity columns.

 

Biological Significance: ExpandCollapse

Along with Tyro-3 and Axl, Mer is a member of the TAM family of receptor tyrosine kinases (RTKs). The TAM family of RTKs regulates cell proliferation/survival, cell adhesion and migration, and blood clot stabilization processes, along with the regulation of inflammatory cytokine release (Linger et al, 2008). Additionally, the TAM family has been linked to coagulopathy and cancer when altered experimentally or genetically (Linger et al, 2008). Tri-phosphorylation of MerTK at tyr749, tyr753 and tyr754 has been identified as a key target in platelet aggregation for developing a new anti-platelet drug that decreases bleeding complications, which are current side effects of similar drugs on the market today (Zhang et al, 2013). MerTK is also seen as a therapeutic target for treating lymphoblastic leukemias, melanoma, breast, lung, colon, liver, gastric, kidney, ovarian, uterine and brain cancers (Graham et al, 1994). There has recently been increased interest in synthesizing novel ATP-competitive small molecule tyrosine kinase inhibitors to decrease tri-phosphorylation of MerTK at tyr749, tyr753, and tyr754 as a therapeutic target to treat AML (Lee-Sherick et al, 2013).

Synonyms: ExpandCollapse

• c MER antibody
• c mer proto oncogene tyrosine kinase antibody
• c-mer antibody
• cMER antibody
• cmer protooncogene tyrosine kinase antibody
• Eyk antibody
• MER antibody
• MER receptor tyrosine kinase antibody
• MERK antibody
• MERPEN antibody
• Mertk antibody
• MERTK c-mer proto-oncogene tyrosine kinase antibody
• MERTK_HUMAN antibody
• MGC133349 antibody
• nmf12 antibody
• Nyk antibody
• Proto oncogene tyrosine protein kinase MER antibody
• Proto oncogene tyrosine protein kinase MER precursor antibody
• Proto-oncogene c-Mer antibody
• Receptor tyrosine kinase MerTK antibody
• RP38 antibody
• STK kinase antibody
• Tyrosine-protein kinase Mer antibody

Storage

100 µl in 10 mM HEPES (pH 7.5), 150 mM NaCl, 100 µg per ml BSA and 50% glycerol. Adequate amount of material to conduct 10-mini Western blots.

Storage at -20°C is recommended, as aliquots may be taken without freeze/thawing due to presence of 50% glycerol. Stable for at least 1 year at -20°C.

Product Specific References

Branchford, B.R., Stalker, T.J., Law, L., Acevedo, G., Sather, S., Brzezinski, C., Wilson, K.M., Minson, K., Lee?Sherick, A.B., Davizon?Castillo, P. and Ng, C. The small molecule MERTK inhibitor UNC2025 decreases platelet activation and prevents thrombosis. Journal of Thrombosis and Haemostasis. Oct 17, 2017.

DeRyckere D, Lee-Sherick AB, Huey MG, Hill AA, Tyner JW, Jacobsen KM, Page LS, Kirkpatrick GG, Eryildiz F, Montgomery SA, Zhang W, Wang X, Frye SV, Earp HS, Graham DK. UNC2025, a MERTK Small-Molecule Inhibitor, Is Therapeutically Effective Alone and in Combination with Methotrexate in Leukemia Models. Clin Cancer Res. 2017 Mar 15;23(6):1481-1492.

Sufit A, Lee-Sherick AB, DeRyckere D, Rupji M, Dwivedi B, Varella-Garcia M, Pierce AM, Kowalski J, Wang X, Frye SV, Earp HS, Keating AK, Graham DK. MERTK Inhibition Induces Polyploidy and Promotes Cell Death and Cellular Senescence in Glioblastoma Multiforme. PLoS One. 2016 Oct 26;11(10):e0165107.

Minson KA, Smith CC, DeRyckere D, Libbrecht C, Lee-Sherick AB, Huey MG, Lasater EA, Kirkpatrick GD, Stashko MA, Zhang W, Jordan CT, Kireev D, Wang X, Frye SV, Earp HS, Shah NP, Graham DK. The MERTK/FLT3 inhibitor MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia. JCI Insight. 2016 Mar;1(3):e85630.

Cummings CT, Zhang W, Davies K, Kirkpatrick GD, Zhang D, DeRyckere D, Wang X, Frye SV, Shelton Earp H, Graham DK. Small molecule inhibition of MERTK is efficacious in non-smal cell lung cancer models independent of driver oncogene status. Mol Cancer Ther. 2015 Sept;14(9):2014-2022.

Lee-Sherick AB, Zhang W, Menachof KK, Hill AA, Rinella S, Kirkpatrick G, Page LS, Stashko MA, Jordan CT, Wei Q, Liu J, Zhang D, DeRyckere D, Wang X, Frye S, Earp HS, Graham DK. Efficacy of a Mer and lt3 tyrosine kinase small molecule inhibitor, UNC1666, in acute myeloid leukemia. Oncotarget. 2015 Mar 30;6(9):6722-36.

Cummings CT, Linger RM, Cohen RA, Sather S, Kirkpatrick GD, Davies KD, DeRyckere D, Earp HS, Graham DK. Mer590, a novel monoclonal antibody targeting MER receptor tyrosine kinase, decreases colony formation and increases chemosensitivity in non-small cell lung cancer. Oncotarget. 2014 Nov 15;5(21):10434-45.

Zhang W, DeRyckere D, Hunter D, Liu J, Stashko MA, Minson KA, Cummings CT, Lee M, Glaros TG, Newton DL, Sather S, Zhang D, Kireev D, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X. UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor. J Med Chem. 2014 Aug 28;57(16):7031-41. doi: 10.1021/jm500749d. Epub 2014 Aug 6.

Zhang W, McIver AL, Stashko MA, DeRyckere D, Branchford BR, Hunter D, Kireev D, Miley MJ, Norris-Drouin J, Stewart WM, Lee M, Sather S, Zhou Y, Di Paola JA, Machius M, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X. Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis. J Med Chem. 2013 Dec 12;56(23):9693-700.

Zhang W, Zhang D, Stashko MA, DeRyckere D, Hunter D, Kireev D, Miley MJ, Cummings C, Lee M, Norris-Drouin J, Stewart WM, Sather S, Zhou Y, Kirkpatrick G, Machius M, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X. Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new Mer kinase inhibitors. J Med Chem. 2013 Dec 12;56(23):9683-92.

Lee-Sherick AB, Eisenman KM, Sather S, McGrananhan A, Armistead PM, McGary CS, Hunsucker SA, Schlegel J, Martinson H, Cannon C, Keating AK, Earp HS, Liang X, DeRyckere D, Graham DK(2013). Aberrant Mer receptor tyrosine kinase expression contributes to leukemogenesis in acute myeloid leukemia. Oncogene. 2013 Nov 14;32(46):5359-68.

Christoph S, Deryckere D, Schlegel J, Frazer JK, Batchelor LA, Trakhimets AY, Sather S, Hunter DM, Cummings CT, Liu J, Yang C, Kireev D, Simpson C, Norris-Drouin J, Hull-Ryde EA, Janzen WP, Johnson GL, Wang X, Frye SV, Earp HS 3rd, Graham DK. UNC569, a novel small-molecule mer inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo. Mol Cancer Ther. 2013 Nov;12(11):2367-77.

Linger R, Cohen RA, Cummings CT, Sather S, Migdall-Wilson J, Middleton DH, Lu X, Baron AE, Franklin WA, Merrik DT, Jedlicka P, DeRyckere D, Heasley LE, Graham DK. Mer or Axl Receptor Tyrosine Kinase Inhibition Promotes Apoptosis, Blocks Growth, and Enhances Chemosensitivity of Human Non-Small Cell Lung Cancer. Oncogene. 2013 July 18; 32(29):3420-3431.

Liu J, Zhang W, Stashko MA, Deryckere D, Cummings CT, Hunter D, Yang C, Jayakody CN, Cheng N, Simpson C, Norris-Drouin J, Sather S, Kireev D, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X. UNC1062, a new and potent Mer inhibitor. Eur J Med Chem. 2013 Jul;65:83-93.

Schlegel J, Sambade MJ, Sather S, Moschos SJ, Tan AC, Winges A, DeRyckere D, Carson CC, Trembath DG, Tentler JJ, Eckhardt SG, Kuan PF, Hamilton RL, Duncan LM, Miller CR, Nikolaishvili-Feinberg N, Midkiff BR, Liu J, Zhang W, Yang C, Wang X, Frye SV, Earp HS, Shields JM, Graham DK. MERTK receptor tyrosine kinase is a therapeutic target in melanoma. J Clin Invest. 2013 May;123(5):2257-67.

Brandao LN, Winges A, Christoph S, Sather S, Migdall-Wilson J, Schlegel J, McGranahan A, Gao D, Liang X, Deryckere D, Graham DK. Inhibition of MerTK increases chemosensitivity and decreases oncogenic potential in T-cell acute lymphoblastic leukemia. Blood Cancer J. 2013 Jan 25;3:e101.

 

  • 5 – Excellent (publishable, performed ideally)
  • 4 – Good (publishable, would use again)
  • 3 – Average (publishable, might use again)
  • 2 – Poor (unpublishable, signal inconclusive)
  • 1 – No signal (unpublishable)
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Western blot of HEK293 lysate showing specific immunolabeling of the ~160 kDa MerTK phosphorylated at Tyr749/753/754 in the first lane (-). Phosphospecificity is shown in the second lane (+) where the immunolabeling is completely eliminated by blot treatment with lambda phosphatase (λ-Ptase, 1200 units for 60 minutes).

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