Cat. No.: HY-50295A

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CI-1040 hydrochloride

Name: CI-1040 hydrochloride
Brand: MedChemExpress
SKU: HY-50295A
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(Synonyms: PD 184352 hydrochloride)

23 Cited Publications

Customer Review

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.

For research use only. We do not sell to patients.

Formula: C₁₇H₁₅Cl₂F₂IN₂O₂
Molecular Weight:515.12

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (276 KB)

CI-1040 hydrochloride Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (23)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

CI-1040 (PD 184352) hydrochloride is an orally active, highly specific inhibitor of MEK, with an IC₅₀ of 17 nM for MEK1^[1]^[2]^[3].

IC₅₀ & Target

MEK1

All MEK Isoforms :

In Vitro

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.

In Vivo

The systemic administration of the MEK inhibitor CI-1040 hydrochloride reduces adenoma formation to a third and significantly restores lung structure. The proliferation rate of lung cells of mice treated with CL-1040 hydrochloride is decreased without any obvious effects on differentiation of pneumocytes^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

Molecular Weight 515.12
Formula C₁₇H₁₅Cl₂F₂IN₂O₂
SMILES

O=C(C1=CC=C(C(F)=C1NC2=CC=C(I)C=C2Cl)F)NOCC3CC3.Cl
Synonyms

PD 184352 hydrochloride
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (23)

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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.
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.
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

Targeting Cell Cycle Facilitates E1A-Independent Adenoviral Replication. [Abstract]

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.
Curr Oncol

Direct Targeting of the Raf-MEK-ERK Signaling Cascade Inhibits Neuroblastoma Growth. [Abstract]

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
bioRxiv

2025 Jun 24.
McGill University

2023 Dec.
Research Square Preprint

2023 Aug 25.
Research Square Print

Nov 2nd, 2022
Oncotarget

MEK is a promising target in the basal subtype of bladder cancer. [Abstract]

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Keywords

CI-1040 hydrochloride

23 Cited Publications

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CI-1040 hydrochloride

Publications Citing Use of MedChemExpress (MCE) CI-1040 hydrochloride

All MEK Isoforms

Biological Activity

Chemical Information

Publications (23)

Purity & Documentation

References

Calculators

Help & FAQs

CI-1040 hydrochloride Related Classifications

HY-50295A Related Classifications

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