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[CAS NO. 120964-45-6] 3-DeazaneplanocinAhydrochloride
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-12186 |
| Brand: | MCE |
| CAS: | 120964-45-6 |
Overview
| MDL | MFCD18782644 |
|---|---|
| Molecular Weight | 298.73 |
| Molecular Formula | C12H15ClN4O3 |
| SMILES | O[C@@H]1[C@H](O)C(CO)=C[C@H]1N2C=NC3=C2C=CN=C3N.[H]Cl |
19 Publications Citing Use of MCE
- [1]Nat Commun. 2022 Jan 10;13(1):12.
- [2]Nat Commun. 2021 Feb 23;12(1):1237.
- [3]J Immunother Cancer. 2019 Nov 14;7(1):300.
- [4]J Am Soc Nephrol. 2016 Jul;27(7):2021-34.
- [5]Cell Death Dis. 2020 Oct 23;11(10):906.
- [6]Cancers (Basel). 2022 Jul 23;14(15):3600.
- [7]Apoptosis. 2020 Oct;25(9-10):697-714.
- [8]Lab Invest. 2021 Mar 10.
- [9]J Mol Cell Cardiol. 2019 Oct;135:119-133.
- [10]Int Immunopharmacol. 2022 Feb 19;106:108612.
- [11]J Pharmacol Exp Ther. 2019 Sep;370(3):490-503.
- [12]Biochem Biophys Res Commun. 2018 Sep 10;503(3):2061-2067.
- [13]Exp Mol Pathol. 2020 Feb;112:104344.
- [14]Cells Tissues Organs. 2021 Jan 18;1-9.
- [15]Cell Reprogram. 2017 Dec;19(6):363-371.
- [16]Research Square Print. September 13th, 2022.
- [17]Università degli Studi di CAGLIARI. Dipartimento di Scienze Biomediche. 2021 May.
- [18]Research Square Preprint. 2020 May.
- [19]Patent. US20180263995A1.
Summary
3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor [1] [2] . 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor [6] . 3-Deazaneplanocin A hydrochloride also has anti- orthopoxvirus and anti-variola activities [7] .
In Vitro
3-Deazaneplanocin A (DZNep) hydrochloride is a potent histone methyltransferase EZH2 inhibitor. Treatment of OCI-AML3 cells with 3-Deazaneplanocin A (1.0 μM) results in a significant increase in accumulation of cells in the G 0 /G 1 phase (58.5%) with a concomitant decrease in the number of cells in S phase (35.2%) and G 2 /M phases (6.3%) of the cell cycle (P<0.05). Treatment with 3-Deazaneplanocin A (200 nM to 2.0 μM) for 48 hours, dose dependently, inhibits colony growth of OCI-AML3 and HL-60 cells [1] . 3-Deazaneplanocin A (DZNep) hydrochloride reduces the expression of EZH2, especially after 72 hours (e.g. 48%, 32% and 36% reduction of EZH2 in PANC-1, MIA-PaCa-2 and LPc006 cells, respectively) [2] . 3-Deazaneplanocin A (DZNep) hydrochloride shows minimal growth inhibition in PANC-1 cells. More than 50% of these cells are still growing after exposure at the highest concentration (20 μM). MIA-PaCa-2 and LPc006 cells are much more sensitive, with IC 0 values of 1.0±0.3 and 0.10±0.03 μM, respectively [2] . 3-Deazaneplanocin A (DZNep) hydrochloride causes dose-dependent inhibition of cell proliferation of NSCLC cell lines, and the IC 0 values range from 0.08 to 0.24 μM [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
The survival of NOD/SCID mice with acute myeloid leukemia (AML) due to HL-60 cells is significantly higher, if treated with 3-Deazaneplanocin A (DZNep) and LBH589 (PS) compare to treatment with PS, 3-Deazaneplanocin A, or vehicle alone (P<0.05). Median survival is as follows: control, 36 days; PS, 42 days; 3-Deazaneplanocin A, 43 days; and 3-Deazaneplanocin A plus PS, 52 days [1] . There is a progressive increase in weight of rats treated with physiological saline in a time-dependent manner (the mean growth rate=3.19% per day). Administration of 20 mg/kg 3-Deazaneplanocin A (DZNep) not only markedly reduces the relative weight of the rats compare to the initial weight (−2.0%, −4.9% and −1.2%) in the first three days post-treatment, but also suppresses the weight growth rate to 2.6% per day from the fourth day onwards post-dose [4] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 50 mg/mL ( 167.38 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.3475 mL | 16.7375 mL | 33.4750 mL |
| 5 mM | 0.6695 mL | 3.3475 mL | 6.6950 mL |
| 10 mM | 0.3348 mL | 1.6738 mL | 3.3475 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (167.38 mM); Clear solution; Need ultrasonic
References
- [1] Fiskus W, et al. Combined epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A and the histone deacetylase inhibitor LBH589 against human AML cells. Blood, 2009, 114(13), 2733-2743.
- [2] Avan A, et al. Molecular mechanisms involved in the synergistic interaction of the EZH2 inhibitor 3-deazaneplanocin A with LY 188011 in pancreatic cancer cells. Mol Cancer Ther. 2012 Aug;11(8):1735-46.
- [3] Kikuchi J, et al. Epigenetic therapy with 3-deazaneplanocin A, an inhibitor of the histone methyltransferase EZH2, inhibits growth of non-small cell lung cancer cells. Lung Cancer. 2012 Nov;78(2):138-43.
- [4] Sun F, et al. Preclinical pharmacokinetic studies of 3-deazaneplanocin A, a potent epigenetic anticancer agent, and its human pharmacokinetic prediction using GastroPlus?. Eur J Pharm Sci. 2015 Sep 18;77:290-302.
- [5] Noriko Uchiyama, et al. Aristeromycin and DZNeP cause growth inhibition of prostate cancer via induction of mir-26a. Eur J Pharmacol. 2017 Oct 5;812:138-146.
- [6] Robert O Baker, et al. Potential antiviral therapeutics for smallpox, monkeypox and other orthopoxvirus infections. Antiviral Res. 2003 Jan;57(1-2):13-23.
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