GSK-J4
Based on 65 publication(s) in Google Scholar
GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1. GSK-J4 induces endoplasmic reticulum stress-related apoptosis.
For research use only. We do not sell to patients.
- Purity: 99.67%
- CAS No.: 1373423-53-0
- Formula: C24H27N5O2
- Molecular Weight:417.50
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Epigenetics Compound Library
HY-L005
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Histone Modification Research Compound Library
HY-L024
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Anti-Cancer Compound Library
HY-L025
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Anti-diabetic Compound Library
HY-L040
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Endoplasmic Reticulum Stress Compound Library
HY-L054
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Chemical Probe Library
HY-L063
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Anti-Cancer Metabolism Compound Library
HY-L083
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Human Metabolite Library
HY-L123
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Cancer Stem Cells Compound Library
HY-L135
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Heterocyclic Compound Library
HY-L138
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Pain-Related Compound Library
HY-L139
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Cell Death Library
HY-L162
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Macrophage Related Compound Library
HY-L174
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Bioactive Compound Library Max
HY-L181
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Epigenetics Compound Library Mini
HY-L005M
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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Methylation Compound Library
HY-L203
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High-Throughput Bioactive Compound Library
HY-L205
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Mass Spectrometry Human Metabolite Library
HY-L215
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Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) GSK-J4
More- Immunity. 2024 May 14;57(5):1087-1104.e7. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2023 Jan 20;14(1):336. [Abstract]
- Bone Res. 2026 Jun 11;14(1):65. [Abstract]
- Adv Sci (Weinh). 2023 Aug;10(22):e2206798. [Abstract]
- J Clin Invest. 2018 Jan 2;128(1):483-499. [Abstract]
- Sci Adv. 2021 Mar 5;7(10):eabe7853. [Abstract]
- J Biomed Sci. 2025 Jan 13;32(1):8. [Abstract]
- Cell Death Dis. 2025 Nov 3;16(1):782. [Abstract]
- Cell Death Dis. 2023 Aug 15;14(8):520. [Abstract]
- Cell Commun Signal. 2022 Oct 27;20(1):168. [Abstract]
- Free Radic Biol Med. 2024 Jan:210:462-477. [Abstract]
- Neoplasia. 2025 Oct:68:101223. [Abstract]
- Br J Pharmacol. 2023 Sep;180(17):2250-2265. [Abstract]
- Stem Cell Res Ther. 2024 Nov 15;15(1):431. [Abstract]
- Cell Death Discov. 2026 May 25. [Abstract]
- Cell Death Discov. 2023 Nov 14;9(1):413. [Abstract]
- Mol Metab. 2025 Apr:94:102113. [Abstract]
- EMBO Rep. 2024 Dec;25(12):5429-5455. [Abstract]
- Ecotoxicol Environ Saf. 2025 Feb 6:291:117847. [Abstract]
- Cancer Cell Int. 2020 Jun 3;20:209. [Abstract]
- Cells. 2026 Jan;15(13):1154.
- Commun Biol. 2022 Sep 2;5(1):904. [Abstract]
- Invest Ophthalmol Vis Sci. 2024 Feb 1;65(2):34. [Abstract]
- Clin Epigenetics. 2024 Jan 20;16(1):14. [Abstract]
- Biochem J. 2019 Jun 26;476(12):1741-1751. [Abstract]
- Transl Oncol. 2025 Jan 14:52:102271. [Abstract]
- iScience. 2024 May 16;27(6):110011. [Abstract]
- J Biomed Mater Res A. 2025 Jan;113(1):e37861. [Abstract]
- Oncol Rep. 2019 May;41(5):2667-2678. [Abstract]
- Mol Divers. 2024 Dec;28(6):4403-4424. [Abstract]
- Cell Signal. 2023 May:105:110626. [Abstract]
- J Proteome Res. 2024 Apr 5;23(4):1495-1505. [Abstract]
- Exp Cell Res. 2026 Jul 1;460(1):115042. [Abstract]
- Clin Exp Med. 2025 Nov 25;26(1):33. [Abstract]
- Exp Cell Res. 2020 Oct 15;395(2):112173. [Abstract]
- Toxicol Appl Pharmacol. 2026 Jun:511:117810. [Abstract]
- Biochim Biophys Acta Mol Cell Biol Lipids. 2021 Jun;1866(6):158901. [Abstract]
- IUBMB Life. 2019 Nov;71(11):1711-1719. [Abstract]
- Adv Cancer Biol Metastasis. 2026 Jan 12;16:100171.
- Front Cardiovasc Med. 2022 Jun 2;9:907747. [Abstract]
- Genes (Basel). 2020 Apr 30;11(5):495. [Abstract]
- Gene. 2022 May 15:822:146317. [Abstract]
- Biomed Res Int. 2020 Mar 18;2020:2953068. [Abstract]
- bioRxiv. 2026 Jun 10:2026.06.09.731212. [Abstract]
- bioRxiv. 2026 May 28.
- bioRxiv. 2026 May 26:2026.05.22.726988. [Abstract]
- bioRxiv. 2026 Apr 21:2026.04.17.718779. [Abstract]
- bioRxiv. 2026 Apr 1.
- bioRxiv. 2025 Oct 14.
- bioRxiv. 2025 Jul 12:2025.07.08.663754. [Abstract]
- University of New York
- bioRxiv. 2025 Jul 21.
- bioRxiv. 2024 August 09.
- bioRxiv. 2024 July 27.
- biorxiv. 2024 Jun 03.
- bioRxiv. 2023 Apr 3.
- Research Square Preprint. 2022 Jul.
- Research Square Preprint. 2022 Feb.
- University of Kentucky. 2021 May.
- Patent. US20200376146A1.
- Patent. US20200376102A1.
- Research Square Preprint. 2020 Nov.
- Research Square Preprint. 2020 Jul.
- Patent. US20180263995A1.
Customer Validation & Images
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IHC
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IF
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WB
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RT-PCR
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WB
Biological Activity
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KDM6 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
14.7 μM
Compound: GSK-J4
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Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 37660833] |
| HCT-116 | IC50 |
1.77 μM
Compound: GSK-J4
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Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 37660833] |
| HeLa | IC50 |
21.65 μM
Compound: GSK-J4
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Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 37660833] |
| HT-29 | IC50 |
14.93 μM
Compound: GSK-J4
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Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 37660833] |
| Macrophage | IC50 |
9 μM
Compound: Chemical probe: GSK-J4
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Antiinflammatory activity in human primary macrophages assessed as inhibition of LPS-induced TNFalpha production measured after 6 hrs by ELISA
Antiinflammatory activity in human primary macrophages assessed as inhibition of LPS-induced TNFalpha production measured after 6 hrs by ELISA
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[PMID: 22842901] |
| Macrophage | IC50 |
9 μM
Compound: GSK-J4
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Antiinflammatory activity against human primary macrophages assessed as inhibition of LPS-activated TNF-alpha production incubated for 6 hrs by ELISA
Antiinflammatory activity against human primary macrophages assessed as inhibition of LPS-activated TNF-alpha production incubated for 6 hrs by ELISA
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[PMID: 25279926] |
| MCF7 | IC50 |
16.44 μM
Compound: GSK-J4
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Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 37660833] |
| SW480 | IC50 |
1.08 μM
Compound: GSK-J4
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Antiproliferative activity against human SW480 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human SW480 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 37660833] |
| T47D | IC50 |
13.21 μM
Compound: GSK-J4
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Antiproliferative activity against human T47D cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human T47D cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 37660833] |
| U-937 | IC50 |
13.5 μM
Compound: GSK-J4
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Antiproliferative activity against human U-937 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human U-937 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 37660833] |
GSK-J4 has cellular activity in Flag-JMJD3-transfected HeLa cells, in which GSK-J4 prevents the JMJD3-induced loss of nuclear H3K27me3 immunostaining. Administration of GSK-J4 increases total nuclear H3K27me3 levels in untransfected cells. GSK-J4 significantly reduces the expression of 16 of 34 LPS-driven cytokines, including tumour-necrosis factor-α (TNF-α)[1].
GSK-J4 (5 μM; 48 hours) causes a more than 3-fold increase in mouse podocyte H3K27me3 content. H3K27me3 levels in cultured podocytes, GSK-J4 reduces Jagged-1 mRNA and Jagged-1 protein levels. Correspondingly, when exposed podocytes to the inducer of dedifferentiation TGF-β1, pretreatment with GSK-J4 preventes both the increase in intracellular N1-ICD levels and the increase in α-SMA and the decrease in podocin mRNA levels[2].
GSK-J4 (10, 25 nM) acts upon DCs promoting the differentiation of Treg cells, improving Treg stability and suppressive capacities, without affecting the differentiation of Th1 and Th17 cells[3].
GSK-J4 inhibits JMJD3 expression that is induced by TGF-β1[4].
GSK-J4 inhibits H3K4 demethylation at Xist, Nodal, and HoxC13 in female embryonic stem cells[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GSK-J4 (0.5 mg/kg, i.p.) significantly reduces the severity and delays the onset of the disease of the mouse model of experimental autoimmune encephalomyelitis[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Eight-week-old male db/m and db/db mice[2]
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Dosage:10 mg/kg
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Administration:i.p.; thrice-weekly for 10 weeks
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Result:Attenuated the development of kidney disease in diabetic mice.
Chemical Information
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CAS No. 1373423-53-0
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Appearance Solid
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Molecular Weight 417.50
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Formula C24H27N5O2
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Color White to yellow
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SMILES
O=C(OCC)CCNC1=NC(C2=CC=CC=N2)=NC(N3CCC(C=CC=C4)=C4CC3)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (65)
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Journal Impact Factor
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Most Recent
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Immunity
25-Hydroxycholesterol regulates lysosome AMP kinase activation and metabolic reprogramming to educate immunosuppressive macrophages. [Abstract]2024 May 14;57(5):1087-1104.e7. PMID: 38640930 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Nat Commun
Polycomb deficiency drives a FOXP2-high aggressive state targetable by epigenetic inhibitors. [Abstract]2023 Jan 20;14(1):336. PMID: 36670102 -
Bone Res
JMJD3-driven epigenetic reprogramming of p16INK4a-positive cells promotes tendon regeneration. [Abstract]2026 Jun 11;14(1):65. PMID: 42276987 -
Adv Sci (Weinh)
Donafenib and GSK-J4 Synergistically Induce Ferroptosis in Liver Cancer by Upregulating HMOX1 Expression. [Abstract]2023 Aug;10(22):e2206798. PMID: 37330650 -
J Clin Invest
2018 Jan 2;128(1):483-499. PMID: 29227285
GSK-J4 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2018 Jan 2;128(1):483-499. [Abstract]
Immunoblotting for H3K27me3 in cultured mouse podocytes treated with the Jmjd3 and UTX inhibitor GSK-J4 (5 μM for 48 hours) (n=3).
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Sci Adv
2021 Mar 5;7(10):eabe7853. PMID: 33674313 -
J Biomed Sci
N6-methyladenosine RNA modification regulates the transcription of SLC7A11 through KDM6B and GATA3 to modulate ferroptosis. [Abstract]2025 Jan 13;32(1):8. PMID: 39800682 -
Cell Death Dis
JMJD3 upregulates ALOX5 to drive malignancy and concomitant ferroptosis sensitivity in gastric cancer. [Abstract]2025 Nov 3;16(1):782. PMID: 41184226 -
Cell Death Dis
m5C-methylated lncRNA NR_033928 promotes gastric cancer proliferation by stabilizing GLS mRNA to promote glutamine metabolism reprogramming. [Abstract]2023 Aug 15;14(8):520. PMID: 37582794 -
Cell Commun Signal
DNMT3A R882H mutation drives daunorubicin resistance in acute myeloid leukemia via regulating NRF2/NQO1 pathway. [Abstract]2022 Oct 27;20(1):168. PMID: 36303144 -
Free Radic Biol Med
27-Hydroxycholesterol induces liver fibrosis via down-regulation of trimethylation of histone H3 at lysine 27 by activating oxidative stress; effect of nutrient interventions. [Abstract]2024 Jan:210:462-477. PMID: 38056577 -
Neoplasia
A methyl-to-acetyl switch in H3K27 drives metabolic reprogramming and resistance to BRAFV600E inhibition in melanoma. [Abstract]2025 Oct:68:101223. PMID: 40850308 -
Br J Pharmacol
JMJD3 Promotes Myeloid Fibroblast Activation and Macrophage Polarization in Kidney Fibrosis. [Abstract]2023 Sep;180(17):2250-2265. PMID: 37076137
GSK-J4 purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2023 Sep;180(17):2250-2265. [Abstract]
GSK-J4 (50 mg/kg, intraperitoneal injection for 10 days) significantly reduced total collagen deposition in the kidneys of mice with UUO compared with vehicle-treated UUO mice.
GSK-J4 purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2023 Sep;180(17):2250-2265. [Abstract]
Immunofluorescence staining revealed that GSK-J4 (50 mg/kg, intraperitoneal injection for 10 days) attenuated the upregulation of collagen I and fibronectin in the kidneys of UUO mice.
GSK-J4 purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2023 Sep;180(17):2250-2265. [Abstract]
Western blot analysis demonstrated that administration of GSK-J4 (50 mg/kg, intraperitoneal injection for 10 days) suppressed collagen I and fibronectin expression in obstructed kidneys.
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Stem Cell Res Ther
AGEs impair osteogenesis in orthodontic force-induced periodontal ligament stem cells through the KDM6B/Wnt self-reinforcing loop. [Abstract]2024 Nov 15;15(1):431. PMID: 39548506 -
Cell Death Discov
ATP2B4 driven chromatin compaction exacerbates pancreatic cancer radiotherapy resistance. [Abstract]2026 May 25. PMID: 42185253 -
Cell Death Discov
The EZH2-H3K27me3 axis modulates aberrant transcription and apoptosis in cyclophosphamide-induced ovarian granulosa cell injury. [Abstract]2023 Nov 14;9(1):413. PMID: 37963880 -
Mol Metab
BIX01294 suppresses PDAC growth through inhibition of glutaminase-mediated glutathione dynamics. [Abstract]2025 Apr:94:102113. PMID: 39961401 -
EMBO Rep
Histone modifications and Sp1 promote GPR160 expression in bone cancer pain within rodent models. [Abstract]2024 Dec;25(12):5429-5455. PMID: 39448865 -
Ecotoxicol Environ Saf
Bisphenol B restrains rat leydig cell function via H3K27me3/H3K9me3 histone modifications. [Abstract]2025 Feb 6:291:117847. PMID: 39919587 -
Cancer Cell Int
GSK-J4 induces cell cycle arrest and apoptosis via ER stress and the synergism between GSK-J4 and decitabine in acute myeloid leukemia KG-1a cells. [Abstract]2020 Jun 3;20:209. PMID: 32514253
GSK-J4 purchased from MedChemExpress. Usage Cited in: Cancer Cell Int. 2020 Jun 3;20:209. [Abstract]
The mRNA expression level of PKC-α is detected using qRT-PCR. GAPDH is used as an internal control.
GSK-J4 purchased from MedChemExpress. Usage Cited in: Cancer Cell Int. 2020 Jun 3;20:209. [Abstract]
After treatment with GSK-J4, the expression levels of PKC-α and p-Bcl2 in KG-1a cells are detected by Western blotting.
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Commun Biol
Pigment epithelium-derived factor promotes peritoneal dissemination of ovarian cancer through induction of immunosuppressive macrophages. [Abstract]2022 Sep 2;5(1):904. PMID: 36056141 -
Invest Ophthalmol Vis Sci
2024 Feb 1;65(2):34. PMID: 38393716 -
Clin Epigenetics
2024 Jan 20;16(1):14. PMID: 38245781 -
Biochem J
2019 Jun 26;476(12):1741-1751. PMID: 31138771 -
Transl Oncol
Combined anti-leukemic effect of gilteritinib and GSK-J4 in FLT3-ITD+ acute myeloid leukemia. [Abstract]2025 Jan 14:52:102271. PMID: 39813767 -
iScience
Transcriptional synergy in human aortic endothelial cells is vulnerable to combination p300/CBP and BET bromodomain inhibition. [Abstract]2024 May 16;27(6):110011. PMID: 38868181 -
J Biomed Mater Res A
Sliding Hydrogels Reveal the Modulation of Mechanosensing Attenuates the Inflammatory Phenotype of Osteoarthritic Chondrocytes in 3D. [Abstract]2025 Jan;113(1):e37861. PMID: 39718447 -
Oncol Rep
Targeting P16INK4A in uterine serous carcinoma through inhibition of histone demethylation. [Abstract]2019 May;41(5):2667-2678. PMID: 30896884 -
Mol Divers
Exploring host epigenetic enzymes as targeted therapies for visceral leishmaniasis: in silico design and in vitro efficacy of KDM6B and ASH1L inhibitors. [Abstract]2024 Dec;28(6):4403-4424. PMID: 38522046 -
Cell Signal
DNMT3A R882H mutation promotes acute leukemic cell survival by regulating glycolysis through the NRF2/NQO1 axis. [Abstract]2023 May:105:110626. PMID: 36758683 -
J Proteome Res
Quantitative Pattern of hPTMs by Mass Spectrometry-Based Proteomics with Implications for Triple-Negative Breast Cancer. [Abstract]2024 Apr 5;23(4):1495-1505. PMID: 38576392 -
Exp Cell Res
The combinations of histone lysine demethylase inhibitors with panobinostat exert enhanced effects against head and neck cancer cells. [Abstract]2026 Jul 1;460(1):115042. PMID: 42019757 -
Clin Exp Med
Corin: a dual inhibitor for KDM1A/HDAC1, suppresses hepatocellular carcinoma by triggering cuproptosis. [Abstract]2025 Nov 25;26(1):33. PMID: 41286164 -
Exp Cell Res
Endothelial progenitor cells-secreted extracellular vesicles containing microRNA-93-5p confer protection against sepsis-induced acute kidney injury via the KDM6B/H3K27me3/TNF-α axis. [Abstract]2020 Oct 15;395(2):112173. PMID: 32679234 -
Toxicol Appl Pharmacol
Nickel exposure disrupts epigenetic repression of developmental genes in mouse embryonic stem cells. [Abstract]2026 Jun:511:117810. PMID: 41932553 -
Biochim Biophys Acta Mol Cell Biol Lipids
Histone H3 methyltransferase Ezh2 promotes white adipocytes but inhibits brown and beige adipocyte differentiation in mice. [Abstract]2021 Jun;1866(6):158901. PMID: 33571671 -
IUBMB Life
2019 Nov;71(11):1711-1719. PMID: 31241814 -
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Front Cardiovasc Med
GSK-J4, a Specific Histone Lysine Demethylase 6A Inhibitor, Ameliorates Lipotoxicity to Cardiomyocytes via Preserving H3K27 Methylation and Reducing Ferroptosis. [Abstract]2022 Jun 2;9:907747. PMID: 35722096 -
Genes (Basel)
Activation of Steroidogenesis, Anti-Apoptotic Activity, and Proliferation in Porcine Granulosa Cells by RUNX1 Is Negatively Regulated by H3K27me3 Transcriptional Repression. [Abstract]2020 Apr 30;11(5):495. PMID: 32365901 -
Gene
EZH2 suppresses insulinoma development by epigenetically reducing KIF4A expression via H3K27me3 modification. [Abstract]2022 May 15:822:146317. PMID: 35182680 -
Biomed Res Int
IL-4 Alleviates Ischaemia-Reperfusion Injury by Inducing Kupffer Cells M2 Polarization via STAT6-JMJD3 Pathway after Rat Liver Transplantation. [Abstract]2020 Mar 18;2020:2953068. PMID: 32258110 -
bioRxiv
Epigenetic de-repression of basal cell metaplasia in aging AT2 cells is a risk factor for idiopathic pulmonary fibrosis (IPF). [Abstract]2026 Jun 10:2026.06.09.731212. PMID: 42327275 -
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bioRxiv
Spatially-Resolved Multiomic Atlas of Leiomyosarcoma Identifies Two Clinically Relevant Epigenetically-Driven Cell States. [Abstract]2026 May 26:2026.05.22.726988. PMID: 42244620 -
bioRxiv
2026 Apr 21:2026.04.17.718779. PMID: 42079196 -
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bioRxiv
2025 Jul 12:2025.07.08.663754. PMID: 40672312 -
University of New York
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Solvent & Solubility
DMSO : 100 mg/mL (239.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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 (4.98 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 (4.98 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
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.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Kruidenier L, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8. [Content Brief]
[2]. Majumder S, et al. Shifts in podocyte histone H3K27me3 regulate mouse and human glomerular disease. J Clin Invest. 2018 Jan 2;128(1):483-499. [Content Brief]
[3]. Donas C, et al. The histone demethylase inhibitor GSK-J4 limits inflammation through the induction of a tolerogenic phenotype on DCs. J Autoimmun. 2016 Dec;75:105-117. [Content Brief]
[5]. Yapp C, et al. H3K27me3 demethylases regulate in vitro chondrogenesis and chondrocyte activity in osteoarthritis. Arthritis Res Ther. 2016 Jul 7;18(1):158 [Content Brief]
[6]. Kamikawa YF, et al. Histone demethylation maintains Prdm14 and Tsix expression and represses xIst in embryonic stem cells. PLoS One. 2015 May 20;10(5):e0125626 [Content Brief]
[7]. Heinemann B, et al. Inhibition of demethylases by GSK-J1/J4. Nature. 2014 Oct 2;514(7520):E1-2 [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3952 mL | 11.9760 mL | 23.9521 mL | 59.8802 mL |
| 5 mM | 0.4790 mL | 2.3952 mL | 4.7904 mL | 11.9760 mL | |
| 10 mM | 0.2395 mL | 1.1976 mL | 2.3952 mL | 5.9880 mL | |
| 15 mM | 0.1597 mL | 0.7984 mL | 1.5968 mL | 3.9920 mL | |
| 20 mM | 0.1198 mL | 0.5988 mL | 1.1976 mL | 2.9940 mL | |
| 25 mM | 0.0958 mL | 0.4790 mL | 0.9581 mL | 2.3952 mL | |
| 30 mM | 0.0798 mL | 0.3992 mL | 0.7984 mL | 1.9960 mL | |
| 40 mM | 0.0599 mL | 0.2994 mL | 0.5988 mL | 1.4970 mL | |
| 50 mM | 0.0479 mL | 0.2395 mL | 0.4790 mL | 1.1976 mL | |
| 60 mM | 0.0399 mL | 0.1996 mL | 0.3992 mL | 0.9980 mL | |
| 80 mM | 0.0299 mL | 0.1497 mL | 0.2994 mL | 0.7485 mL | |
| 100 mM | 0.0240 mL | 0.1198 mL | 0.2395 mL | 0.5988 mL |
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