CI-1040 hydrochloride
Based on 23 publication(s) in Google Scholar
CI-1040 (PD 184352) hydrochloride is an orally active, highly specific inhibitor of MEK, with an IC50 of 17 nM for MEK1.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C17H15Cl2F2IN2O2
- Peso molecular:515.12
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) CI-1040 hydrochloride
More- Nat Methods. 2023 Dec;20(12):2021-2033. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Clin Cancer Res. 2020 Apr 15;26(8):2011-2021. [Abstract]
- Int J Biol Macromol. 2026 Mar 3:151196. [Abstract]
- Int J Biol Macromol. 2020 May 1;150:261-280. [Abstract]
- Int J Biol Macromol. 2018 Dec;120(Pt A):1039-1047. [Abstract]
- Cancer Cell Int. 2021 Jun 5;21(1):291. [Abstract]
- Biochem Pharmacol. 2023 May:211:115542. [Abstract]
- Life Sci. 2024 Dec 1:358:123163. [Abstract]
- Oncogenesis. 2019 Nov 4;8(11):65. [Abstract]
- Biol Direct. 2023 Oct 24;18(1):67. [Abstract]
- Glia. 2019 Jul;67(7):1320-1332. [Abstract]
- Brain Commun. 2024 Apr 29;6(3):fcae152. [Abstract]
- J Virol. 2023 Jun 29;97(6):e0037023. [Abstract]
- Neurotox Res. 2017 Nov;32(4):535-543. [Abstract]
- Curr Oncol. 2022 Sep 10;29(9):6508-6522. [Abstract]
- Biochim Biophys Acta Gen Subj. 2021 Mar;1865(3):129836. [Abstract]
- bioRxiv. 2025 Jun 24.
- McGill University. 2023 Dec.
- Research Square Preprint. 2023 Aug 25.
- Research Square Print. Nov 2nd, 2022
- Oncotarget. 2020 Nov 3;11(44):3921-3932. [Abstract]
- ACS Comb Sci. 2019 Dec 9;21(12):805-816. [Abstract]
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Actividad biológica
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MEK1 |
CI-1040 hydrochloride directly inhibits MEK1 with an IC50 of 17 nM. It has also been shown to have little activity against a panel of related kinases with IC50 values more than 2.5 orders of magnitude higher. Treatment of whole cells with CI-1040 hydrochloride completely inhibits the mitogen-stimulated phosphorylation of ERK. CI-1040 hydrochloride at a concentration of 1 μM is found to inhibit phosphorylation of ERK1 and ERK2 by 99% and 92%, respectively in MDA-MB-231 breast cancer cells[1].
CI-1040 hydrochloride induces apoptosis and inhibits proliferation in U-937 cells in a dose and time-dependent manner. CI-1040 hydrochloride induces a significant increase in PUMA mRNA and protein levels[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Peso molecular 515.12
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Fòrmula C17H15Cl2F2IN2O2
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SMILES
O=C(C1=CC=C(C(F)=C1NC2=CC=C(I)C=C2Cl)F)NOCC3CC3.Cl
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Synonyms
PD 184352 hydrochloride
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (23)
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Journal Impact Factor
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Most Recent
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Nat Methods
Reconstruction of dynamic mammary mini gland in vitro for normal physiology and oncogenesis. [Abstract]2023 Dec;20(12):2021-2033. PMID: 37919421 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Clin Cancer Res
Gene Expression Signatures Identify Novel Therapeutics for Metastatic Pancreatic Neuroendocrine Tumors. [Abstract]2020 Apr 15;26(8):2011-2021. PMID: 31937620 -
Int J Biol Macromol
Isolation, structural characterization and immunoregulatory activity of a novel acidic polysaccharide from Ganoderma sinense. [Abstract]2026 Mar 3:151196. PMID: 41786176 -
Int J Biol Macromol
Cordyceps militaris polysaccharide converts immunosuppressive macrophages into M1-like phenotype and activates T lymphocytes by inhibiting the PD-L1/PD-1 axis between TAMs and T lymphocytes. [Abstract]2020 May 1;150:261-280. PMID: 32044366 -
Int J Biol Macromol
Polysaccharide isolated from Sarcodon aspratus induces RAW264.7 activity via TLR4-mediated NF-κB and MAPK signaling pathways. [Abstract]2018 Dec;120(Pt A):1039-1047. PMID: 30171950 -
Cancer Cell Int
Construction of a prognostic model with histone modification-related genes and identification of potential drugs in pancreatic cancer. [Abstract]2021 Jun 5;21(1):291. PMID: 34090418 -
Biochem Pharmacol
PD184352 exerts anti-inflammatory and antioxidant effects by promoting activation of the Nrf2/HO-1 axis. [Abstract]2023 May:211:115542. PMID: 37028460
CI-1040 hydrochloride purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2023 May:211:115542. [Abstract]
CI-1040 (PD 184352; 10, 20, 40 nM; 48 h) significantly inhibits the expression of iNOS and COX2 in a dose-dependent manner in ATDC5 cells.
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Life Sci
A novel exosome-like nanovesicles from Cordyceps militaris potentiate immunomodulatory and anti-tumor effect by reprogramming macrophages. [Abstract]2024 Dec 1:358:123163. PMID: 39442867 -
Oncogenesis
A novel small-molecule inhibitor of trefoil factor 3 (TFF3) potentiates MEK1/2 inhibition in lung adenocarcinoma. [Abstract]2019 Nov 4;8(11):65. PMID: 31685806
CI-1040 hydrochloride purchased from MedChemExpress. Usage Cited in: Oncogenesis. 2019 Nov 4;8(11):65. [Abstract]
Western blot analysis of p-ERK and ERK protein levels in cell lysates of H1975 treated with AMPC, CI-1040 for 24 h. The levels of the total ERK was used as an input control.
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Biol Direct
Nuclear respiratory factor 1 drives hepatocellular carcinoma progression by activating LPCAT1-ERK1/2-CREB axis. [Abstract]2023 Oct 24;18(1):67. PMID: 37875967 -
Glia
Inhibition of MAPK/ERK pathway promotes oligodendrocytes generation and recovery of demyelinating diseases. [Abstract]2019 Jul;67(7):1320-1332. PMID: 30815939 -
Brain Commun
Spike-induced cytoarchitectonic changes in epileptic human cortex are reduced via MAP2K inhibition. [Abstract]2024 Apr 29;6(3):fcae152. PMID: 38741662 -
J Virol
2023 Jun 29;97(6):e0037023. PMID: 37219458 -
Neurotox Res
Lithium Chloride Facilitates Autophagy Following Spinal Cord Injury via ERK-dependent Pathway. [Abstract]2017 Nov;32(4):535-543. PMID: 28593525
CI-1040 hydrochloride purchased from MedChemExpress. Usage Cited in: Neurotox Res. 2017 Nov;32(4):535-543. [Abstract]
Lithium promotes autophagy flux by activating MEK/ERK pathway in cells. Original Western blot showing LC3-II and p62 abundance following treatment with lithium in the presence of PD184352 and SCH772984 in neurons. Arithmetic means±SEM (n=5) showing LC3-II abundance following treatment with lithium in the presence of PD184352 and SCH772984 in neurons.
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Curr Oncol
2022 Sep 10;29(9):6508-6522. PMID: 36135081 -
Biochim Biophys Acta Gen Subj
Human milk derived peptide AOPDM1 attenuates obesity by restricting adipogenic differentiation through MAPK signalling. [Abstract]2021 Mar;1865(3):129836. PMID: 33370564 -
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Oncotarget
2020 Nov 3;11(44):3921-3932. PMID: 33216841 -
ACS Comb Sci
Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]2019 Dec 9;21(12):805-816. PMID: 31689077
Pureza y Documentación
Referencias
[1]. Allen LF, et al. CI-1040 (PD184352), a targeted signal transduction inhibitor of MEK (MAPKK). Semin Oncol. 2003 Oct;30(5 Suppl 16):105-16. [Content Brief]
[2]. Wei CR, et al. MEK inhibitor CI-1040 induces apoptosis in acute myeloid leukemia cells in vitro. Eur Rev Med Pharmacol Sci. 2016 May;20(10):1961-8. [Content Brief] [Content Brief]
[3]. Kramer BW, et al. Use of mitogenic cascade blockers for treatment of C-Raf induced lung adenoma in vivo: CI-1040strongly reduces growth and improves lung structure. BMC Cancer. 2004 Jun 1;4:24. [Content Brief]
Calculators
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