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| 5mg |
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Purity: ≥98%
Description: UNC0379 is a substrate competitive lysine methyltransferase SETD8 (KMT5A) inhibitor with antineoplastic activity. It inhibits KMT5A with an IC50 of 7.9 μM, and shows higher selectivity for KMT5A over 15 other methyltransferases.
| ln Vitro |
UNC0379 (1–10 μM, 9 days) prevents the growth of HGSOC cells[2]. UNC0379 (10 μM, 96 h) causes an increase in the percentage of HGSOC cells in the sub-G1 phase[2]. Myofibroblast de-differentiation is induced and further fibroblast to myofibroblast differentiation is inhibited by UNC0379 (10 μM, 96 h) 48 h][3].
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| ln Vivo |
In mice with lung fibrosis induced by bleomycin (BLM), UNC0379 (intratracheal administration, 1 mg/kg/day, on days 7, 8, and 9) ameliorates the lung fibrosis[3].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: JHOS2, JHOS3, JHOS4, OVCAR3, OVCAHO, OVKATE, KURAMOCHI, TYKnu Tested Concentrations: 1-10 μM Incubation Duration: 9 days Experimental Results: Inhibited HGSOC cells proliferation with IC50s ranging from 0.39 to 3.20 µM. Cell Cycle Analysis[1] Cell Types: JHOS3, OVCAR3 Tested Concentrations: 10 µM Incubation Duration: 96 h Experimental Results: Arrested cells in sub-G1 phase. |
| Animal Protocol |
Animal/Disease Models: Bleomycin (BLM)-induced lung fibrosis mouse model[3]
Doses: 1 mg/kg/day Route of Administration: Intracheal administration, on day7, 8, and 9. Experimental Results: Ameliorated BLM-induced lung fibrosis (supported by the evaluation of the Ashcroft score and changes in the collagen content in the lung samples) without affecting pulmonary inflammation. |
| References |
[1]. Ma A, et al. Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33.
[2]. Miku Wada, et al. Epigenetic Modifier SETD8 as a Therapeutic Target for High-Grade Serous Ovarian Cancer. Biomolecules. 2020 Dec 16;10(12):1686. [3]. Keita Ugai, et al. Inhibition of the SET8 Pathway Ameliorates Lung Fibrosis Even Through Fibroblast Dedifferentiation. Front Mol Biosci. 2020 Aug 5;7:192. |
| Molecular Formula |
C23H35N5O2
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| Molecular Weight |
413.56
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| CAS # |
1620401-82-2
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| Related CAS # |
UNC0379 TFA;1620401-83-3
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| SMILES |
O(C([H])([H])[H])C1=C(C([H])=C2C(=C1[H])C(=NC(=N2)N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H])N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H])OC([H])([H])[H]
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4180 mL | 12.0901 mL | 24.1803 mL | |
| 5 mM | 0.4836 mL | 2.4180 mL | 4.8361 mL | |
| 10 mM | 0.2418 mL | 1.2090 mL | 2.4180 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Compound 1 binds SETD8 with a KD of 18.3 ± 3.2 μM (n = 3) in ITC studies.J Med Chem.2014 Aug 14;57(15):6822-33. |
Compound1was identified as an inhibitor of SETD8 by cross-screening a quinazoline-based inhibitor set. |
Compound1exhibits rapid on and off rates in SPR studies. |
MOA studies of compound1.J Med Chem.2014 Aug 14;57(15):6822-33. |
Peptide displacement assay.J Med Chem.2014 Aug 14;57(15):6822-33. |
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