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Purity: ≥98%
UNC0321 (UNC-0321) is a novel, potent and selective G9a histone methyltransferase inhibitor with anticancer activity. It inhibits G9a with Ki of 63 pM, UNC0321 was discovered by optimizing the 7-dimethylaminopropoxy side chain on the basis of the structural insights revealed by UNC0224-G9a cocrystal structure. UNC0321 is the first G9a inhibitor with picomolar potency.
| ln Vitro |
Compound 29 (UNC0321) has IC50 values of 9 nM, 6 nM, 15 nM, and 23 nM, respectively, which inhibit the activities of G9a ECSD, G9a CLOT, GLP ECSD, and GLP CLOT. In HUVECs in MDA-MB-231 cells, UNC0321 (Compound 3) decreases Rab4 expression. Rab4 expression is markedly suppressed in HUVEC by UNC0321 (200 pM; 48 h) [3].
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| Cell Assay |
Western Blot Analysis[3]
Cell Types: HUVEC. Level of H3K9me2, IC50 value is 11 µM[2]. Tested Concentrations: 50 pM, 100 pM, 200 pM. Incubation Duration: 48 hrs (hours). Experimental Results: Glucose-induced reduction in Cleared Caspase3 and Bax expression. Release glucose from inhibiting the expression of Bcl-2, Caspase3, p-AKT, p-mTOR and p70. Promote proliferation and inhibit apoptosis by inhibiting Rab4. Apoptosis analysis[3] Cell Types: HUVEC. Tested Concentrations: 50 pM, 100 pM, 200 pM. Incubation Duration: 48 hrs (hours). Experimental Results: Inhibition of glucose-induced apoptosis. Cell proliferation assay [3] Cell Types: HUVEC. Tested Concentrations: 50 pM, 100 pM, 200 pM. Incubation Duration: 48 hrs (hours). Experimental Results: The inhibitory effect of glucose on HUVEC proliferation was relieved. |
| References |
[1]. Liu F, et al. Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem. 2010 Aug 12;53(15):5844-57.
[2]. Liu F, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50. [3]. Nie J. UNC0321 inhibits high glucose induced apoptosis in HUVEC by targeting Rab4. Biomed Pharmacother. 2020 Nov;131:110662. |
| Molecular Formula |
C27H45N7O3
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|---|---|
| Molecular Weight |
515.6913
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| CAS # |
1238673-32-9
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| SMILES |
CN1CCC(NC2=C3C=C(OC)C(OCCOCCN(C)C)=CC3=NC(N4CCN(C)CCC4)=N2)CC1
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| InChi Key |
AULLUGALUBVBDD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H45N7O3/c1-31(2)15-16-36-17-18-37-25-20-23-22(19-24(25)35-5)26(28-21-7-11-33(4)12-8-21)30-27(29-23)34-10-6-9-32(3)13-14-34/h19-21H,6-18H2,1-5H3,(H,28,29,30)
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| Chemical Name |
7-(2-(2-(dimethylamino)ethoxy)ethoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine
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| Synonyms |
UNC0321, CHEBI:785916, NCGC0018778901, UNC-0321, CHEMBL1214066, UNC 0321, KB81388
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO : ≥ 31 mg/mL (~60.11 mM)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9391 mL | 9.6957 mL | 19.3915 mL | |
| 5 mM | 0.3878 mL | 1.9391 mL | 3.8783 mL | |
| 10 mM | 0.1939 mL | 0.9696 mL | 1.9391 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.
 The 7-dimethylamino propoxy side chain (gray, blue, and red) of10does not fully occupy the lysine binding channel in the X-ray crystal structure of the G9a-10complex (PDB code: 3K5K).J Med Chem.2010 Aug 12;53(15):5844-57. |
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 MorrisonKis of compounds29,10, and3ain the G9a MCE assay.J Med Chem.2010 Aug 12;53(15):5844-57. |
 The lipophilic benzyl group (top) is exposed to solvent and does not makes any interactions with the protein in the X-ray crystal structure of the GLP-3acomplex (PDB code: 3FPD).J Med Chem.2010 Aug 12;53(15):5844-57. |
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