Mirdametinib
Based on 157 publication(s) in Google Scholar
Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. Mirdametinib exhibits a Kiapp of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts.
For research use only. We do not sell to patients.
- Purity: 99.95%
- CAS No.: 391210-10-9
- Formula: C16H14F3IN2O4
- Molecular Weight:482.19
-
Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) Mirdametinib
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- Nat Protoc. 2026 Jan 26. [Abstract]
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- Nat Struct Mol Biol. 2025 Sep 1. [Abstract]
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- Cell Death Dis. 2022 Mar 30;13(3):284. [Abstract]
- Cell Death Dis. 2021 Oct 30;12(11):1034. [Abstract]
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- Stem Cell Res Ther. 2025 Oct 8;16(1):547. [Abstract]
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- Aging Cell. 2026 Jan 20;25(2):e70352.
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- Cell Death Discov. 2021 Oct 2;7(1):271. [Abstract]
- Cell Rep. 2025 Mar 5;44(3):115362. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- Cell Rep. 2022 Mar 29;38(13):110570. [Abstract]
- Sci Signal. 2026 Jun 23;19(943):eaef1474. [Abstract]
- Lwt-Food Sci Technol. 11 Oct 2021.
- Sci Signal. 2021 Jun 22;14(688):eabe6156. [Abstract]
- Comput Biol Med. 2025 Jul 5;196(Pt A):110721. [Abstract]
- EMBO Rep. 2022 Feb 3;23(3):e53191. [Abstract]
- JCI Insight. 2025 Sep 23;10(18):e190716. [Abstract]
- Cancer Cell Int. 2021 Jun 5;21(1):291. [Abstract]
- J Invest Dermatol. 2026 Jan 23:S0022-202X(26)00030-8. [Abstract]
- J Invest Dermatol. 2022 Mar;142(3 Pt A):613-623.e7. [Abstract]
- Cell Prolif. 2023 Dec;56(12):e13498. [Abstract]
- Cell Prolif. 2022 Apr;55(4):e13209. [Abstract]
- Mol Cancer Ther. 2024 Dec 3;23(12):1789-1800. [Abstract]
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- Glia. 2019 Jul;67(7):1320-1332. [Abstract]
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- Eur J Pharm Sci. 2021 Dec 1:167:106003. [Abstract]
- Int Immunopharmacol. 2021 Apr:93:107395. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Lung Cancer. 2025 Nov 19:211:108848. [Abstract]
- Cancers (Basel). 2022 Oct 31;14(21):5368. [Abstract]
- Front Cell Dev Biol. 2018 Sep 25:6:111. [Abstract]
- iScience. 2023 Jul 26;26(8):107469. [Abstract]
- Transl Oncol. 2023 Mar:29:101628. [Abstract]
- Sci Rep. 2025 Nov 17;15(1):40227. [Abstract]
- J Biol Chem. 2020 Oct 16;295(42):14325-14342. [Abstract]
- J Biol Chem. 2012 Mar 23;287(13):9742-52. [Abstract]
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- J Cell Sci. 2024 May 1;137(9):jcs261241. [Abstract]
- Stem Cells. 2022 Oct 21;40(10):892-905. [Abstract]
- Exp Cell Res. 2026 Mar 10;458(1):114982. [Abstract]
- Front Med. 2025 Dec 27. [Abstract]
- Exp Cell Res. 2023 Jun 15;427(2):113603. [Abstract]
- Viruses. 2018 Apr 13;10(4). pii: E191. [Abstract]
- Andrology. 2025 Jun 16. [Abstract]
- Stem Cells Int. 2020 Feb 3;2020:8483035. [Abstract]
- Stem Cells Int. 2018 Dec 25:2018:5965727. [Abstract]
- Front Neurosci. 2022 Jun 7;16:901688. [Abstract]
- Biol Reprod. 2024 May 9;110(5):950-970. [Abstract]
- Bioorg Med Chem. 2023 Jul 15:90:117366. [Abstract]
- J Anim Sci. 2024 Jan 3:102:skae251. [Abstract]
- Genes (Basel). 2024 Oct 30;15(11):1400. [Abstract]
- Neuroscience. 2024 May 9:S0306-4522(24)00196-9. [Abstract]
- Animals (Basel). 2024 May 4;14(9):1382. [Abstract]
- Animals (Basel). 2021 Feb 6;11(2):425. [Abstract]
- Platelets. 2022 Jul 4;33(5):755-763. [Abstract]
- Fundam Clin Pharmacol. 2020 Oct;34(5):571-580. [Abstract]
- Toxicon. 2026 Jan:269:108660. [Abstract]
- Gene. 2025 Jan 15:933:148985. [Abstract]
- PeerJ. 2020 Oct 2;8:e9981. [Abstract]
- Virology. 2020 Jan 2;539:121-128. [Abstract]
- FEBS Open Bio. 2025 Sep 10. [Abstract]
- FEBS Open Bio. 2021 Oct;11(10):2740-2755. [Abstract]
- Biochem Biophys Res Commun. 2023 Jan 29:642:145-153. [Abstract]
- Biochem Biophys Res Commun. 2022 Jan 29:590:125-131. [Abstract]
- Biochem Biophys Res Commun. 2020 Apr 2;524(2):280-287. [Abstract]
- Epilepsy Res. 2022 Mar:181:106890. [Abstract]
- STAR Protoc. 2023 Mar 16;4(2):102151. [Abstract]
- STAR Protoc. 2023 Feb 3;4(1):102092. [Abstract]
- STAR Protoc. 2021 Nov 5;2(4):100881. [Abstract]
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- medRxiv. 2026 Mar 7.
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- bioRxiv. 2025 Oct 17:2025.10.17.683020. [Abstract]
- bioRxiv. 2025 Oct 14:2025.10.12.681919. [Abstract]
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- bioRxiv. 2024 Dec 10:2024.12.09.627542. [Abstract]
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- bioRxiv. 2023 Jun 15:2023.06.15.545148. [Abstract]
- Preprints. 2023 May 5.
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- Research Square Preprint. 2022 Feb.
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IF
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2D/3D Cell Culture and Differentiation
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IF
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Cell Proliferation/Viability Assay
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WB
All MEK Isoforms
More
Biological Activity
|
MEK1 1 nM (Ki) |
MEK2 1 nM (Ki) |
MEK 0.33 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
13 nM
Compound: PD325901
|
Antiproliferative activity against human A375 cells expressing BRAF V600E mutant after 72 hrs by Cell titer-glo assay
Antiproliferative activity against human A375 cells expressing BRAF V600E mutant after 72 hrs by Cell titer-glo assay
|
[PMID: 23474388] |
| A-375 | GI50 |
1.28 nM
Compound: 5; PD-325901
|
Antiproliferative activity against human A-375 cells harboring BRAF V600E mutant assessed as cell growth inhibition incubated for 72 hrs in the absence of UV irradiation by CellTiter-Glo luminescent assay
Antiproliferative activity against human A-375 cells harboring BRAF V600E mutant assessed as cell growth inhibition incubated for 72 hrs in the absence of UV irradiation by CellTiter-Glo luminescent assay
|
[PMID: 36924668] |
| A-375 | GI50 |
1.37 nM
Compound: 5; PD-325901
|
Antiproliferative activity against human A-375 cells harboring BRAF V600E mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 1 min and measured 72 hrs post compound treatment by CellTiter-Glo lumi
Antiproliferative activity against human A-375 cells harboring BRAF V600E mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 1 min and measured 72 hrs post compound treatment by CellTiter-Glo lumi
|
[PMID: 36924668] |
| A-375 | GI50 |
1.49 nM
Compound: 5; PD-325901
|
Antiproliferative activity against human A-375 cells harboring BRAF V600E mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 5 mins and measured 72 hrs post compound treatment by CellTiter-Glo lum
Antiproliferative activity against human A-375 cells harboring BRAF V600E mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 5 mins and measured 72 hrs post compound treatment by CellTiter-Glo lum
|
[PMID: 36924668] |
| A-375 | GI50 |
1.59 nM
Compound: 5; PD-325901
|
Antiproliferative activity against human A-375 cells harboring BRAF V600E mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 3 mins and measured 72 hrs post compound treatment by CellTiter-Glo lum
Antiproliferative activity against human A-375 cells harboring BRAF V600E mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 3 mins and measured 72 hrs post compound treatment by CellTiter-Glo lum
|
[PMID: 36924668] |
| A-431 | IC50 |
<0.014 μM
Compound: PD-0325901
|
Inhibition of MEK/ERK signaling pathway in TNFalpha-stimulated human A431 cells transfected with COT siRNA assessed as reduction in ERK1/2 phosphorylation incubated for 60 mins followed by stimulation with TNFalpha for 10 mins by Western blot analysis
Inhibition of MEK/ERK signaling pathway in TNFalpha-stimulated human A431 cells transfected with COT siRNA assessed as reduction in ERK1/2 phosphorylation incubated for 60 mins followed by stimulation with TNFalpha for 10 mins by Western blot analysis
|
[PMID: 27502541] |
| A-431 | IC50 |
0.038 μM
Compound: PD-0325901
|
Inhibition of MEK/ERK signaling pathway in EGF-stimulated human A431 cells transfected with COT siRNA assessed as reduction in ERK1/2 phosphorylation incubated for 60 mins followed by stimulation with EGF for 10 mins by Western blot analysis
Inhibition of MEK/ERK signaling pathway in EGF-stimulated human A431 cells transfected with COT siRNA assessed as reduction in ERK1/2 phosphorylation incubated for 60 mins followed by stimulation with EGF for 10 mins by Western blot analysis
|
[PMID: 27502541] |
| A549 | IC50 |
166 nM
Compound: PD325901
|
Antiproliferative activity against human A549 cells
Antiproliferative activity against human A549 cells
|
[PMID: 23474388] |
| A549 | IC50 |
166 nM
Compound: PD325901
|
Antiproliferative activity against human A549 cells harboring K-Ras mutation
Antiproliferative activity against human A549 cells harboring K-Ras mutation
|
[PMID: 26611920] |
| A549 | IC50 |
0.06 μM
Compound: PD0325901
|
Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
|
[PMID: 32305784] |
| A549 | CC50 |
>100 μM
Compound: PD-0325901
|
Cytotoxicity against human A549 cells
Cytotoxicity against human A549 cells
|
[PMID: 33539089] |
| A549 | GI50 |
10.6 nM
Compound: 5; PD-325901
|
Antiproliferative activity against human A549 cells harboring KRas G13S mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 5 mins and measured 72 hrs post compound treatment by CellTiter-Glo lumin
Antiproliferative activity against human A549 cells harboring KRas G13S mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 5 mins and measured 72 hrs post compound treatment by CellTiter-Glo lumin
|
[PMID: 36924668] |
| A549 | GI50 |
4.94 nM
Compound: 5; PD-325901
|
Antiproliferative activity against human A549 cells harboring KRAS G13S mutant assessed as cell growth inhibition incubated for 72 hrs in the absence of UV irradiation by CellTiter-Glo luminescent assay
Antiproliferative activity against human A549 cells harboring KRAS G13S mutant assessed as cell growth inhibition incubated for 72 hrs in the absence of UV irradiation by CellTiter-Glo luminescent assay
|
[PMID: 36924668] |
| COLO 205 | IC50 |
5 nM
Compound: PD325901
|
Antiproliferative activity against human COLO205 cells harboring BRAF mutation
Antiproliferative activity against human COLO205 cells harboring BRAF mutation
|
[PMID: 26611920] |
| COLO 205 | GI50 |
0.2 nM
Compound: 4; PD0325901
|
Antiproliferative activity against human COLO205 cells assessed as reduction in cell growth after 3 days by WST8 assay
Antiproliferative activity against human COLO205 cells assessed as reduction in cell growth after 3 days by WST8 assay
|
[PMID: 31730343] |
| HCT-116 | IC50 |
194 nM
Compound: PD325901
|
Antiproliferative activity against human HCT116 cells expressing KRAS G13D mutant
Antiproliferative activity against human HCT116 cells expressing KRAS G13D mutant
|
[PMID: 23474388] |
| HCT-116 | IC50 |
185 nM
Compound: PD325901
|
Antiproliferative activity against human HCT116 cells harboring K-Ras G13D mutation
Antiproliferative activity against human HCT116 cells harboring K-Ras G13D mutation
|
[PMID: 26611920] |
| HCT-116 | IC50 |
0.09 μM
Compound: PD0325901
|
Antiproliferative activity against human HCT116 cells harboring KRAS G13D mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
Antiproliferative activity against human HCT116 cells harboring KRAS G13D mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
|
[PMID: 32305784] |
| HCT-116 | GI50 |
44.7 nM
Compound: 5; PD-325901
|
Antiproliferative activity against human HCT-116 cells harboring KRAS G13D mutant assessed as cell growth inhibition incubated for 72 hrs in the absence of UV irradiation by CellTiter-Glo luminescent assay
Antiproliferative activity against human HCT-116 cells harboring KRAS G13D mutant assessed as cell growth inhibition incubated for 72 hrs in the absence of UV irradiation by CellTiter-Glo luminescent assay
|
[PMID: 36924668] |
| HCT-116 | GI50 |
52.5 nM
Compound: 5; PD-325901
|
Antiproliferative activity against human HCT-116 cells harboring KRAS G13D mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 5 mins and measured 72 hrs post compound treatment by CellTiter-Glo lu
Antiproliferative activity against human HCT-116 cells harboring KRAS G13D mutant assessed as cell growth inhibition preincubated with compound for 1 hrs followed by UV irradiation for 5 mins and measured 72 hrs post compound treatment by CellTiter-Glo lu
|
[PMID: 36924668] |
| HEK-293T | GI50 |
>10000 nM
Compound: 5; PD-325901
|
Cytotoxicity against HEK293T cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against HEK293T cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 36924668] |
| HepG2 | IC50 |
5 nM
Compound: PD325901
|
Antiproliferative activity against human HepG2 cells harboring N-Ras mutation
Antiproliferative activity against human HepG2 cells harboring N-Ras mutation
|
[PMID: 26611920] |
| HL-60 | IC50 |
0.0013 μM
Compound: PD0325901
|
Antiproliferative activity against human HL60 cells harboring NRAS K61L mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
Antiproliferative activity against human HL60 cells harboring NRAS K61L mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
|
[PMID: 32305784] |
| HT-29 | GI50 |
3.1 nM
Compound: 4; PD0325901
|
Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth after 3 days by MTT assay
Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth after 3 days by MTT assay
|
[PMID: 31730343] |
| LoVo | IC50 |
128 nM
Compound: PD325901
|
Antiproliferative activity against human LoVo cells
Antiproliferative activity against human LoVo cells
|
[PMID: 23474388] |
| MCF7 | IC50 |
9550 nM
Compound: PD325901
|
Antiproliferative activity against human MCF7 cells
Antiproliferative activity against human MCF7 cells
|
[PMID: 26611920] |
| MDA-MB-231 | GI50 |
1 μM
Compound: PD-0325901
|
Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
|
[PMID: 30802730] |
| MDA-MB-231 | IC50 |
0.082 μM
Compound: PD0325901
|
Antiproliferative activity against human MDA-MB-231 cells harboring KRAS G13D/BRAF G464V mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
Antiproliferative activity against human MDA-MB-231 cells harboring KRAS G13D/BRAF G464V mutant assessed as inhibition of cell viability after 96 hrs by Celltiter-Glo assay
|
[PMID: 32305784] |
| MIA PaCa-2 | IC50 |
17 nM
Compound: PD325901
|
Antiproliferative activity against human MIAPaCa2 cells
Antiproliferative activity against human MIAPaCa2 cells
|
[PMID: 23474388] |
| Sf21 | IC50 |
>25 μM
Compound: PD-0325901
|
Inhibition of human COT (66 to 395 residues) expressed in Sf21 cells using 5-Fluo-Ahx-AGAGSGQLIDSNleANSFVGTR-NH2 as substrate after 60 mins by caliper microfluidic mobility shift assay
Inhibition of human COT (66 to 395 residues) expressed in Sf21 cells using 5-Fluo-Ahx-AGAGSGQLIDSNleANSFVGTR-NH2 as substrate after 60 mins by caliper microfluidic mobility shift assay
|
[PMID: 27502541] |
| SK-MEL-28 | GI50 |
2.9 nM
Compound: 4; PD0325901
|
Antiproliferative activity against human SK-MEL-28 cells assessed as reduction in cell growth after 3 days by MTT assay
Antiproliferative activity against human SK-MEL-28 cells assessed as reduction in cell growth after 3 days by MTT assay
|
[PMID: 31730343] |
| SU-DHL-1 | GI50 |
350 nM
Compound: 1; PD0325901
|
Antiproliferative activity against human SU-DHL-1 cells incubated for 3 days by WST8 assay
Antiproliferative activity against human SU-DHL-1 cells incubated for 3 days by WST8 assay
|
[PMID: 33284613] |
| UACC-257 | GI50 |
0.2 nM
Compound: 4; PD0325901
|
Antiproliferative activity against human UACC257 cells assessed as reduction in cell growth after 3 days by MTT assay
Antiproliferative activity against human UACC257 cells assessed as reduction in cell growth after 3 days by MTT assay
|
[PMID: 31730343] |
Mirdametinib (PD325901; 0.0064, 0.032, 0.16, 0.8, 4, 20, 100 nM; for 2 days) inhibits the growth of Papillary thyroid carcinomas (PTC) cell lines (TPC-1 cells and K2 cells) with GC50 of 11 nM and 6.3 nM, respectively[3].
Mirdametinib (100 nmol/L; for 4 days) induces apoptosis in K2 cells (top) or TPC-1 cells[3].
Mirdametinib (0.1, 1, 10, 100, 1000 nM; for 1 hour) suppresses the expression of p-ERK1/2 in K2 cells (top) or TPC-1 cells[3].
Mirdametinib prevents the growth of melanoma cell lines. Mirdametinib significantly prevents the the growth of PTC cells harboring a BRAF mutation at very low concentration (10 nM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mirdametinib (20-25 mg/kg/day; oral gavage; for 3 weeks (5 consecutive days/week)) suppresses tumor growth completely in mice inoculated with PTC cells carrying a BRAF mutation (K2) and significantly decreased tumor growth in mice inoculated with PTC cells carrying the RET/PTC1 rearrangement (TPC-1) in athymic Ncr-nu/nu mice at ages 6 to 8 weeks[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 391210-10-9
-
Appearance Solid
-
Molecular Weight 482.19
-
Formula C16H14F3IN2O4
-
Color White to off-white
-
SMILES
O=C(C1=CC=C(C(F)=C1NC2=CC=C(I)C=C2F)F)NOC[C@H](O)CO
-
Synonyms
PD0325901; PD325901
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (157)
-
Journal Impact Factor
-
Most Recent
-
Signal Transduct Target Ther
Tet methylcytosine dioxygenase 2 (TET2) deficiency elicits EGFR-TKI (tyrosine kinase inhibitors) resistance in non-small cell lung cancer. [Abstract]2024 Mar 9;9(1):65. PMID: 38461173 -
Nature
2025 Jan;637(8046):726-735. PMID: 39537929 -
Nature
2022 Jan;601(7894):600-605. PMID: 34856602
Mirdametinib purchased from MedChemExpress. Usage Cited in: Nature. 2022 Jan;601(7894):600-605. [Abstract]
Upon exposure to lysophosphatidic acid (LPA) (a Hippo pathway inhibitor), A83-01 (an inhibitor of TGFβ family receptors) and PD0325901 (an ERK inhibitor) in a chemically defined medium containing the STAT activator leukaemia inhibitory factor (LIF) and Y-27632 (a ROCK inhibitor) (10 µM, 7 days),blastocyst-like structures formed efficiently from naive PSCs.
Mirdametinib purchased from MedChemExpress. Usage Cited in: Nature. 2022 Jan;601(7894):600-605. [Abstract]
Upon exposure to lysophosphatidic acid (LPA) (a Hippo pathway inhibitor), A83-01 (an inhibitor of TGFβ family receptors) and PD0325901 (an ERK inhibitor) in a chemically defined medium containing the STAT activator leukaemia inhibitory factor (LIF) and Y-27632 (a ROCK inhibitor) (10 µM, 7 days), blastocyst-like structures formed efficiently from naive PSCs. trophectoderm (TE) cell analogues (identified as GATA2+GATA3+CDX2+TROP2+) formed, proliferated, and established adherens junctions (marked by CDH1), apical-basal polarity (indicated by aPKC) and tight junctions (marked by ZO-1).
-
Cell
2025 Oct 30;188(22):6301-6316.e29. PMID: 40818455 -
Cell
2024 Nov 14;187(23):6566-6583.e22. PMID: 39332412 -
Nat Methods
Challenging the Astral mass analyzer to quantify up to 5,300 proteins per single cell at unseen accuracy to uncover cellular heterogeneity. [Abstract]2025 Mar;22(3):510-519. PMID: 39820751 -
Nat Immunol
Type A cholesterol-dependent cytolysins translocate to the trans-Golgi network for NLRP3 inflammasome activation. [Abstract]2025 Oct;26(10):1673-1685. PMID: 40913097
Mirdametinib purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2025 Oct;26(10):1673-1685. [Abstract]
Representative immunofluorescence images in HeLa cells stably expressing NLRP3-GFP pre-treated with DMSO (solvent control), 20 μM U0126 or 20 μM Mirdametinib for 30 min before addition of rPFO or not (Mock) for 80 min. The results showed that significantly enhanced rPFO-induced TGN remodeling and NLRP3 recruitment in HeLa NLRP3-GFP. Scale bar, 10 μm.
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Nat Biomed Eng
TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]2018 Aug;2(8):578-588. PMID: 31015631 -
Cell Stem Cell
An inducible model of human post-implantation development derived from primed and naive stem cells. [Abstract]2025 Oct 2;32(10):1509-1527.e9. PMID: 40885193 -
Cell Stem Cell
Modeling early gastrulation in human blastoids with DNA methylation patterns of natural blastocysts. [Abstract]2025 Mar 6;32(3):409-425.e8. PMID: 39814012 -
Cell Stem Cell
Epiblast inducers capture mouse trophectoderm stem cells in vitro and pattern blastoids for implantation in utero. [Abstract]2022 Jul 7;29(7):1102-1118.e8. PMID: 35803228 -
Nat Protoc
2026 Jan 26. PMID: 41588252 -
Nat Protoc
2023 May;18(5):1584-1620. PMID: 36792779 -
Nat Commun
Klf5-adjacent super-enhancer functions as a 3D genome structure-dependent transcriptional driver to safeguard ESC identity. [Abstract]2025 Jul 1;16(1):5540. PMID: 40592854 -
Nat Commun
Semi-automated IT-scATAC-seq profiles cell-specific chromatin accessibility in differentiation and peripheral blood populations. [Abstract]2025 Mar 17;16(1):2635. PMID: 40097444 -
Nat Commun
An actin bracket-induced elastoplastic transition determines epithelial folding irreversibility. [Abstract]2024 Dec 12;15(1):10476. PMID: 39668169 -
Nat Commun
2024 Sep 5;15(1):7758. PMID: 39237615 -
Nat Commun
2022 Nov 29;13(1):7345. PMID: 36446858
Mirdametinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Nov 29;13(1):7345. [Abstract]
Cell numbers of hepatocytes cultured in IL6-HCM and a number of pathway modulators, including Crytotanshinone and BP-1-102 (JAK/STAT3 inhibitor), MK2206 and GSK2141795 (PI3K/AKT inhibitor), PD0325901 (MARK/ERK1/2 inhibitor), and TGFβ1 for 14 days.The results showed that PD0325901 (PD) could inhibit IL6-induced hepatocyte proliferation.
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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 -
Adv Sci (Weinh)
Dynamics of the Mammalian Placental Metabolome in Placentogenesis and Embryonic Development. [Abstract]2026 Jan 28:e07928. PMID: 41603190 -
Neuro Oncol
Preclinical assessment of MEK1/2 inhibitors for neurofibromatosis type 2-associated schwannomas reveals differences in efficacy and drug resistance development. [Abstract]2019 Mar 18;21(4):486-497. PMID: 30615146 -
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Nucleic Acids Res
Enhancer architecture-dependent multilayered transcriptional regulation orchestrates RA signaling-induced early lineage differentiation of ESCs. [Abstract]2021 Nov 18;49(20):11575-11595. PMID: 34723340 -
Biomaterials
A fluorescent chemical probe CDy9 selectively stains and enables the isolation of live naïve mouse embryonic stem cells. [Abstract]2018 Oct;180:12-23. PMID: 30014963 -
J Exp Clin Cancer Res
Dual CDK and MEK Inhibition potentiates CD8+ T cell-mediated antitumor immunity by inducing pyroptotic cell death in high-mutational head and neck cancer. [Abstract]2025 Nov 6;44(1):300. PMID: 41194215 -
J Exp Clin Cancer Res
Supervillin promotes epithelial-mesenchymal transition and metastasis of hepatocellular carcinoma in hypoxia via activation of the RhoA/ROCK-ERK/p38 pathway. [Abstract]2018 Jun 28;37(1):128. PMID: 29954442
Mirdametinib purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 28;37(1):128. [Abstract]
MHCC-97H cells are transfected with control or supervillin-specific siRNA for 48 h, exposed to hypoxia for 16 h, and lysates are assayed for the relative amounts of GTP-loaded (activated) Rac1, Cdc42, and RhoA. Cells that have been transfected with control RNAi are treated with a PD0325901 or SB239063 before assaying for GTP-Rac1, Cdc42, and RhoA levels.
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J Exp Clin Cancer Res
FAK-ERK activation in cell/matrix adhesion induced by the loss of apolipoprotein E stimulates the malignant progression of ovarian cancer. [Abstract]2018 Feb 20;37(1):32. PMID: 29458390 -
Redox Biol
The protective role of GPX4 in naïve ESCs is highlighted by induced ferroptosis resistance through GPX4 expression. [Abstract]2025 Apr:81:103539. PMID: 40010136 -
J Hazard Mater
Triazole fungicides exert neural differentiation alteration through H3K27me3 modifications: In vitro and in silico study. [Abstract]2023 Oct 5:459:132225. PMID: 37557044 -
Clin Cancer Res
Gene Expression Signatures Identify Novel Therapeutics for Metastatic Pancreatic Neuroendocrine Tumors. [Abstract]2020 Apr 15;26(8):2011-2021. PMID: 31937620 -
Clin Cancer Res
Upregulation of IGF1R by mutant RAS in leukemia and potentiation of RAS signaling inhibitors by small-molecule inhibition of IGF1R. [Abstract]2014 Nov 1;20(21):5483-95. PMID: 25186968 -
Nat Struct Mol Biol
2025 Sep 1. PMID: 40890525 -
Cancer Lett
Zoledronic acid enhances the efficacy of the MEK inhibitor trametinib in KRAS mutant cancers. [Abstract]2019 Feb 1:442:202-212. PMID: 30429107 -
Environ Int
2025 Sep 28:204:109820. PMID: 41033068 -
Cell Death Dis
Genome-wide screening in the haploid system reveals Slc25a43 as a target gene of oxidative toxicity. [Abstract]2022 Mar 30;13(3):284. PMID: 35354792 -
Cell Death Dis
Activation of G protein coupled estrogen receptor prevents chemotherapy-induced intestinal mucositis by inhibiting the DNA damage in crypt cell in an extracellular signal-regulated kinase 1- and 2- dependent manner. [Abstract]2021 Oct 30;12(11):1034. PMID: 34718327 -
Sci China Life Sci
Maternal transcription factor OTX2 directly induces SETD1A and promotes embryonic genome activation in human pre-implantation embryos. [Abstract]2025 Apr 22. PMID: 40285911 -
Genome Biol
IT-scC&T-seq streamlines scalable, parallel profiling of protein-DNA interactions in single cells. [Abstract]2025 Jul 7;26(1):196. PMID: 40624534 -
Proc Natl Acad Sci U S A
2019 Jun 18;116(25):12147-12152. PMID: 31127047 -
Dev Cell
Identifying cross-lineage dependencies of cell-type-specific regulators in mouse gastruloids. [Abstract]2025 Jul 21;60(14):2007-2022.e7. PMID: 40101716 -
Cell Syst
Receptor-Driven ERK Pulses Reconfigure MAPK Signaling and Enable Persistence of Drug-Adapted BRAF-Mutant Melanoma Cells. [Abstract]2020 Nov 18;11(5):478-494.e9. PMID: 33113355 -
Cell Syst
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]2018 Apr 25;6(4):424-443.e7. PMID: 29655704 -
Stem Cell Res Ther
Generation of equine induced pluripotent stem cells from cells of embryonic, perinatal and adult tissues. [Abstract]2025 Oct 8;16(1):547. PMID: 41063189 -
Stem Cell Res Ther
Human platelet lysate enhances small lipid droplet accumulation of human MSCs through MAPK phosphorylation. [Abstract]2024 Dec 18;15(1):473. PMID: 39696689 -
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Blood Adv
Melanocortin/MC5R axis regulates the proliferation of hematopoietic stem cells in mice after ionizing radiation injury. [Abstract]2023 Jul 11;7(13):3199-3212. PMID: 36920787 -
Cell Death Discov
Gadd45g initiates embryonic stem cell differentiation and inhibits breast cell carcinogenesis. [Abstract]2021 Oct 2;7(1):271. PMID: 34601500 -
Cell Rep
2025 Mar 5;44(3):115362. PMID: 40053453 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
Cell Rep
2022 Mar 29;38(13):110570. PMID: 35354046 -
Sci Signal
The APC/C adaptor Cdh1 stabilizes STING to potentiate innate immune activation in renal cell carcinoma. [Abstract]2026 Jun 23;19(943):eaef1474. PMID: 42335217 -
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Sci Signal
TSHZ2 is an EGF-regulated tumor suppressor that binds to the cytokinesis regulator PRC1 and inhibits metastasis. [Abstract]2021 Jun 22;14(688):eabe6156. PMID: 34158398 -
Comput Biol Med
Identification of inflammation-related biomarkers and therapeutic targets for neurogenic bladder fibrosis via multi-omics analysis. [Abstract]2025 Jul 5;196(Pt A):110721. PMID: 40618693 -
EMBO Rep
ZFP207 sustains pluripotency by coordinating OCT4 stability, alternative splicing and RNA export. [Abstract]2022 Feb 3;23(3):e53191. PMID: 35037361 -
JCI Insight
FXR shapes an immunosuppressive microenvironment in PD-L1lo/- non-small cell lung cancer by upregulating HVEM. [Abstract]2025 Sep 23;10(18):e190716. PMID: 40985894 -
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 -
J Invest Dermatol
Botulinum neurotoxin type A1 alleviates bleomycin-induced skin fibrosis by inhibiting phosphatidylinositol 3-kinase-protein kinase B (PI3K-Akt) pathway and associated cell cycle and proliferation. [Abstract]2026 Jan 23:S0022-202X(26)00030-8. PMID: 41581589 -
J Invest Dermatol
Combined Cyclin-Dependent Kinase Inhibition Overcomes MAPK/Extracellular Signal-Regulated Kinase Kinase Inhibitor Resistance in Plexiform Neurofibroma of Neurofibromatosis Type I. [Abstract]2022 Mar;142(3 Pt A):613-623.e7. PMID: 34534577 -
Cell Prolif
2023 Dec;56(12):e13498. PMID: 37144356 -
Cell Prolif
Genome-scale screening in a rat haploid system identifies Thop1 as a modulator of pluripotency exit. [Abstract]2022 Apr;55(4):e13209. PMID: 35274380 -
Mol Cancer Ther
2024 Dec 3;23(12):1789-1800. PMID: 39295275 -
Stem Cell Reports
An acidic residue within the OCT4 dimerization interface of SOX17 is necessary and sufficient to overcome its pluripotency-inducing activity. [Abstract]2025 Jan 23:102398. PMID: 39919754 -
Glia
Inhibition of MAPK/ERK pathway promotes oligodendrocytes generation and recovery of demyelinating diseases. [Abstract]2019 Jul;67(7):1320-1332. PMID: 30815939 -
Int J Mol Sci
The Rab18/Ras/ERK/FosB/MMP3 Signaling Pathway Mediates Cell Migration Regulation by 2'3'-cGAMP. [Abstract]2025 Jun 16;26(12):5758. PMID: 40565221 -
Int J Mol Sci
2024 Sep 21;25(18):10138. PMID: 39337621 -
Stem Cells Transl Med
High-throughput screening in postimplantation haploid epiblast stem cells reveals Hs3st3b1 as a modulator for reprogramming. [Abstract]2021 May;10(5):743-755. PMID: 33511777 -
Cell Regen
A single-cell hematopoietic microenvironmental atlas reveals progressive maturation of bone marrow vascular niche. [Abstract]2025 Dec 4;14(1):50. PMID: 41339619 -
Bioorg Chem
PD0325901, an ERK inhibitor, attenuates RANKL-induced osteoclast formation and mitigates cartilage inflammation by inhibiting the NF-κB and MAPK pathways. [Abstract]2023 Mar:132:106321. PMID: 36642020 -
Eur J Pharm Sci
Velvet antler polypeptide-loaded polyvinyl alcohol-sodium alginate hydrogels promote the differentiation of neural progenitor cells in 3D towards oligodendrocytes in vitro. [Abstract]2021 Dec 1:167:106003. PMID: 34517106 -
Int Immunopharmacol
Z-guggulsterone induces PD-L1 upregulation partly mediated by FXR, Akt and Erk1/2 signaling pathways in non-small cell lung cancer. [Abstract]2021 Apr:93:107395. PMID: 33529916 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Lung Cancer
KRASG12D/G13D-USP15 axis promotes TGF-β/SMAD signaling and glycolytic flux to accelerate NSCLC pathogenesis. [Abstract]2025 Nov 19:211:108848. PMID: 41317688 -
Cancers (Basel)
Nuclear Membrane Protein SUN5 Is Highly Expressed and Promotes Proliferation and Migration in Colorectal Cancer by Regulating the ERK Pathway. [Abstract]2022 Oct 31;14(21):5368. PMID: 36358787 -
Front Cell Dev Biol
Fast Dynamic in vivo Monitoring of Erk Activity at Single Cell Resolution in DREKA Zebrafish. [Abstract]2018 Sep 25:6:111. PMID: 30320107 -
iScience
Network characterization linc1393 in the maintenance of pluripotency provides the principles for lncRNA targets prediction. [Abstract]2023 Jul 26;26(8):107469. PMID: 37588167 -
Transl Oncol
CKAP4-mediated activation of FOXM1 via phosphorylation pathways regulates malignant behavior of glioblastoma cells. [Abstract]2023 Mar:29:101628. PMID: 36701930 -
Sci Rep
Enhancement of melanoma aggressiveness via p38-MAPK, HIF-1α pathways, and metabolic reprogramming induced by Candida albicans. [Abstract]2025 Nov 17;15(1):40227. PMID: 41249785 -
J Biol Chem
2020 Oct 16;295(42):14325-14342. PMID: 32796029 -
J Biol Chem
Kinome-wide selectivity profiling of ATP-competitive mammalian target of rapamycin (mTOR) inhibitors and characterization of their binding kinetics. [Abstract]2012 Mar 23;287(13):9742-52. PMID: 22223645 -
Brain Res Bull
FGF9 alters the Wallerian degeneration process by inhibiting Schwann cell transformation and accelerating macrophage infiltration. [Abstract]2019 Oct:152:285-296. PMID: 31220553 -
J Cell Sci
Tbl1 promotes Wnt/β-catenin signaling-induced degradation of the Tcf7l1 protein in mouse ESCs. [Abstract]2024 May 1;137(9):jcs261241. PMID: 38639717 -
Stem Cells
P21-activated kinase 4 Pak4 maintains embryonic stem cell pluripotency via Akt activation. [Abstract]2022 Oct 21;40(10):892-905. PMID: 35896382 -
Exp Cell Res
2026 Mar 10;458(1):114982. PMID: 41819468 -
Front Med
ASPH interacts with RUVBL2 to promote tumor metastasis in lung adenocarcinoma via MAPK and Notch signaling pathways. [Abstract]2025 Dec 27. PMID: 41454078 -
Exp Cell Res
Oxymatrine boosts hematopoietic regeneration by modulating MAPK/ERK phosphorylation after irradiation-induced hematopoietic injury. [Abstract]2023 Jun 15;427(2):113603. PMID: 37075826 -
Viruses
2018 Apr 13;10(4). pii: E191. PMID: 29652799
Mirdametinib purchased from MedChemExpress. Usage Cited in: Viruses. 2018 Apr 13;10(4). pii: E191. [Abstract]
H2.35 cells are serum starved for 72 h and then are pre-treated with either DMSO or 10 µM PD0325901 (ERK IN). Cells are infected with MP12 (MOI 5) for one hour, followed by removal of viral inoculum, and addition of growth medium containing DMSO or 10 µM ERK IN. At 18 hpi, cell lysates are collected for western blot analysis.
Mirdametinib purchased from MedChemExpress. Usage Cited in: Viruses. 2018 Apr 13;10(4). pii: E191. [Abstract]
H2.35 cells are serum starved for 72 h and then were pre-treated with either DMSO or BI-D1870 (p90 IN, 10 µM). Cells are infected with MP12 (MOI 5) for one hour, followed by removal of viral inoculum, and addition of growth medium containing DMSO or p90 IN (10 µM). At 18 hpi, cell lysates are collected for western blot analysis.
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Andrology
Expression of IL-33 in rodent testes and its role in Leydig cell steroidogenesis and aging. [Abstract]2025 Jun 16. PMID: 40521800 -
Stem Cells Int
Screening Genes Promoting Exit from Naive Pluripotency Based on Genome-Scale CRISPR-Cas9 Knockout. [Abstract]2020 Feb 3;2020:8483035. PMID: 32089710 -
Stem Cells Int
Establishment and Identification of a CiPSC Lineage Reprogrammed from FSP-tdTomato Mouse Embryonic Fibroblasts (MEFs). [Abstract]2018 Dec 25:2018:5965727. PMID: 30675169 -
Front Neurosci
Extracellular Adenosine Triphosphate Binding to P2Y1 Receptors Prevents Glutamate-Induced Excitotoxicity: Involvement of Erk1/2 Signaling Pathway to Suppress Autophagy. [Abstract]2022 Jun 7;16:901688. PMID: 35747207 -
Biol Reprod
2024 May 9;110(5):950-970. PMID: 38330185 -
Bioorg Med Chem
Daphnanes diterpenes from the latex of Hura crepitans L. and their PKCζ-dependent anti-proliferative activity on colorectal cancer cells. [Abstract]2023 Jul 15:90:117366. PMID: 37329676 -
J Anim Sci
Ubiquitination plays an important role during the formation of chicken primordial germ cells. [Abstract]2024 Jan 3:102:skae251. PMID: 39187982 -
Genes (Basel)
Influence and Optimization of Diverse Culture Systems on Chicken Embryonic Stem Cell Culture. [Abstract]2024 Oct 30;15(11):1400. PMID: 39596599 -
Neuroscience
DCPIB Attenuates Ischemia-Reperfusion Injury by Regulating Microglial M1/M2 Polarization and Oxidative Stress. [Abstract]2024 May 9:S0306-4522(24)00196-9. PMID: 38734301 -
Animals (Basel)
The Effect of Inhibiting the Wingless/Integrated (WNT) Signaling Pathway on the Early Embryonic Disc Cell Culture in Chickens. [Abstract]2024 May 4;14(9):1382. PMID: 38731386 -
Animals (Basel)
Glycolysis Combined with Core Pluripotency Factors to Promote the Formation of Chicken Induced Pluripotent Stem Cells. [Abstract]2021 Feb 6;11(2):425. PMID: 33562170 -
Platelets
EloA promotes HEL polyploidization upon PMA stimulation through enhanced ERK1/2 activity. [Abstract]2022 Jul 4;33(5):755-763. PMID: 34697988 -
Fundam Clin Pharmacol
Urolithin C increases glucose-induced ERK activation which contributes to insulin secretion. [Abstract]2020 Oct;34(5):571-580. PMID: 32083757 -
Toxicon
Deoxynivalenol-induced anorexia is mediated by brain-gut peptides through CaSR-TRPM5 signaling axis. [Abstract]2026 Jan:269:108660. PMID: 41241198 -
Gene
Immune-related glycosylation genes based classification predicts prognosis and therapy options of osteosarcoma. [Abstract]2025 Jan 15:933:148985. PMID: 39369757 -
PeerJ
A novel dual MEK/PDK1 inhibitor 9za retards the cell cycle at G0/G1 phase and induces mitochondrial apoptosis in non-small cell lung cancer cells. [Abstract]2020 Oct 2;8:e9981. PMID: 33072436 -
Virology
EGR1 upregulation following Venezuelan equine encephalitis virus infection is regulated by ERK and PERK pathways contributing to cell death. [Abstract]2020 Jan 2;539:121-128. PMID: 31733451 -
FEBS Open Bio
Establishment and optimization of the two-step induction system for generating primordial germ cell-like cells from chicken embryonic stem cells. [Abstract]2025 Sep 10. PMID: 40926636 -
FEBS Open Bio
Activation of ERK-Drp1 signaling promotes hypoxia-induced Aβ accumulation by upregulating mitochondrial fission and BACE1 activity. [Abstract]2021 Oct;11(10):2740-2755. PMID: 34403210 -
Biochem Biophys Res Commun
COL8A1 enhances the invasion/metastasis in MDA-MB-231 cells via the induction of IL1B and MMP1 expression. [Abstract]2023 Jan 29:642:145-153. PMID: 36577251 -
Biochem Biophys Res Commun
SEPHS1 is dispensable for pluripotency maintenance but indispensable for cardiac differentiation in mouse embryonic stem cells. [Abstract]2022 Jan 29:590:125-131. PMID: 34974300 -
Biochem Biophys Res Commun
β-catenin stimulates Tcf7l1 degradation through recruitment of casein kinase 2 in mouse embryonic stem cells. [Abstract]2020 Apr 2;524(2):280-287. PMID: 31987502
Mirdametinib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2020 Apr 2;524(2):280-287. [Abstract]
Western blot analysis of Tcf7l1 protein levels in mESCs pre-treated with D4476 or DMAT and then treated with CHIR or PD03 for 24 h.
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Epilepsy Res
Inhibition of MEK-ERK signaling reduces seizures in two mouse models of tuberous sclerosis complex. [Abstract]2022 Mar:181:106890. PMID: 35219048 -
STAR Protoc
2023 Mar 16;4(2):102151. PMID: 36930647 -
STAR Protoc
2023 Feb 3;4(1):102092. PMID: 36853659 -
STAR Protoc
2021 Nov 5;2(4):100881. PMID: 34806042 -
bioRxiv
Large RNA polymerase II condensates are promoter-centric assemblies associated with early stages of transcription at all expressed genes. [Abstract]2026 May 25:2026.05.25.727590. PMID: 42244752 -
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2026 Jan 20:rs.3.rs-8607320. PMID: 41646411 -
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bioRxiv
Hidden-driver inference reveals synergistic brain-penetrant therapies for medulloblastoma. [Abstract]2025 Nov 20:2025.11.20.689490. PMID: 41332625 -
bioRxiv
Noncanonical amino acid incorporation enables minimally disruptive labeling of stress granule and TDP-43 proteinopathy. [Abstract]2025 Oct 17:2025.10.17.683020. PMID: 41279779 -
bioRxiv
Restoration of Spermatogenesis is Dependent on Activation of a SPRY4-ERK Checkpoint Following Germline Stem Cell Damage. [Abstract]2025 Oct 14:2025.10.12.681919. PMID: 41279276 -
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bioRxiv
2025 Feb 2:2025.02.01.636075. PMID: 39975412 -
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bioRxiv
A direct interaction between the Chd1 CHCT domain and Rtf1 controls Chd1 distribution and nucleosome positioning on active genes. [Abstract]2024 Dec 6:2024.12.06.627179. PMID: 39677735 -
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bioRxiv
2024 Dec 10:2024.12.09.627542. PMID: 39713309 -
bioRxiv
Amputation Triggers Long-Range Epidermal Permeability Changes in Evolutionarily Distant Regenerative Organisms. [Abstract]2024 Aug 31:2024.08.29.610385. PMID: 39257748 -
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bioRxiv
ASCL1-ERK1/2 Axis: ASCL1 restrains ERK1/2 via the dual specificity phosphatase DUSP6 to promote survival of a subset of neuroendocrine lung cancers. [Abstract]2023 Jun 15:2023.06.15.545148. PMID: 37398419 -
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Solvent & Solubility
DMSO : ≥ 56 mg/mL (116.14 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.31 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.31 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Incorporation of 32P into myelin basic protein (MBP) is assayed in the presence of a glutathione S-transferase fusion protein containing p44MAP kinase (GST-MAPK) and a glutathione S-transferase protein containing p45MEK (GST-MEK). The assay solution contained 20 mM HEPES, pH 7.4, 10 mM MgCl2, 1 mM MnCl2, 1 mM EGTA, 50 mM [gamma-32P]ATP, 10 mg GST-MEK, 0.5 mg GST-MAPK and 40 mg MBP in a final volume of 100 mL. Reactions are stopped after 20 minutes by addition of trichloroacetic acid and filtered through a GF/C filter mat. 32P retained on the filter mat is determined using a 1205 Betaplate. PD0325901 is assessed at various dose ranges in order to determine dose response curves.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PTC cells (1×104) are seeded in 24-well plates with 1 mL of medium for 4 days in a 37°C incubator. MEK inhibitor PD0325901 at varying concentrations is added to the cells in triplicate on day 0. MTT dissolved in 0.8% NaCl solution at 5 mg/mL is added to each well (0.2 mL) on day 2 to test GC50 or every day for cell growth curves. The cells are incubated at 37°C for 3 hours with MTT. The liquid is then aspirated from the wells and discarded. Stained cells are dissolved in 0.5 mL of DMSO and their absorption at 570 nm is measured using a Synergy HT multidetection microplate reader. For GC50, cell growth is calculated as 100×(T−T0)/(C−T0), where T is the optical density of the wells treated with inhibitors after a 48-hour period, T0 is the optical density at time zero, and C is the control optical density with DMSO only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice (10-14 per group) are anesthetized s.c. with a cocktail. K2 and TPC-1 cells stably infected with a retrovirus expressing luciferase (5×105 cells in 5 μL RPMI1640 medium) are inoculated into the thyroid gland, and the mice are monitored weekly for tumor growth by Xenogen using Living Image 3.0 software. One week after inoculation, PD0325901 is dissolved in 80 mM citric buffer (pH 7) by sonication and given to mice daily by oral gavage (20-25 mg/kg) for 3 weeks (5 consecutive days/week). Mice are sacrificed only due to tumor burden or loss of 20% of body weight. Tumor sizes are measured with calipers and tumor volume (V) is calculated by the formula (V=length×width×depth). Control mice are given 80 mM citric buffer (pH 7) alone. All in vivo experiments are done at least twice.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (788 KB)
- English - EN (788 KB)
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Handling Instructions (2659 KB)
References
[1]. Barrett SD, et al. The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6501-4. [Content Brief]
[3]. Henderson YC, et al. MEK inhibitor PD0325901 significantly reduces the growth of papillary thyroid carcinoma cells in vitro and in vivo. Mol Cancer Ther. 2010 Jul;9(7):1968-76. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0739 mL | 10.3694 mL | 20.7387 mL | 51.8468 mL |
| 5 mM | 0.4148 mL | 2.0739 mL | 4.1477 mL | 10.3694 mL | |
| 10 mM | 0.2074 mL | 1.0369 mL | 2.0739 mL | 5.1847 mL | |
| 15 mM | 0.1383 mL | 0.6913 mL | 1.3826 mL | 3.4565 mL | |
| 20 mM | 0.1037 mL | 0.5185 mL | 1.0369 mL | 2.5923 mL | |
| 25 mM | 0.0830 mL | 0.4148 mL | 0.8295 mL | 2.0739 mL | |
| 30 mM | 0.0691 mL | 0.3456 mL | 0.6913 mL | 1.7282 mL | |
| 40 mM | 0.0518 mL | 0.2592 mL | 0.5185 mL | 1.2962 mL | |
| 50 mM | 0.0415 mL | 0.2074 mL | 0.4148 mL | 1.0369 mL | |
| 60 mM | 0.0346 mL | 0.1728 mL | 0.3456 mL | 0.8641 mL | |
| 80 mM | 0.0259 mL | 0.1296 mL | 0.2592 mL | 0.6481 mL | |
| 100 mM | 0.0207 mL | 0.1037 mL | 0.2074 mL | 0.5185 mL |