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| 5mg |
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| 10mg |
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Purity: ≥98%
3-deazaneplanocin A HCl (known also as DZNep; C-c3Ado; NSC-617989), the hydrochloride salt of 3-deazaneplanocin A which is an adenosine analog, is a novel and competitive inhibitor of S-adenosylhomocysteine hydrolase and also an EZH2 (histone methyltransferase) inhibitor with anticancer activity. It inhibits S-adenosylhomocysteine hydrolase with a Ki of 50 pM in a cell-free assay. 3-deazaneplanocin A demostrates excellent antiproliferative activity and high in vivo antitumor efficacy. It disrupts polycomb-repressive complex 2 (PRC2), and induces apoptosis, while inhibiting proliferation and metastasis, in cancer cells, including acute myeloid leukemia, breast cancer and glioblastoma. DZNep is a promising therapeutic agent for ovarian cancer cells, with potential to inhibit proliferation, induce apoptosis and decrease migration.
| ln Vitro |
3-Deazaneplanocin A hydrochloride (DZNep) hydrochloride is a potent inhibitor of histone methyltransferase EZH2. Treatment of OCI-AML3 cells with 3-Deazaneplanocin A hydrochloride (1.0 μM) resulted in a significant increase in the accumulation of cells in the G0/G1 phase (58.5%) and concomitant cell numbers in the S phase (35.2%) and G2/M phase (6.3%) of the cell cycle. decreased (P<0.05). Treatment with 3-Deazaneplanocin A hydrochloride (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 hydrochloride (DZNep) hydrochloride can reduce the expression of EZH2, especially after 72 hours (for example, EZH2 in PANC-1, MIA-PaCa-2, and LPc006 cells decreased by 48%, 32%, and 36%, respectively )[2]. 3-Deazaneplanocin A hydrochloride (DZNep) hydrochloride exhibits minimal growth inhibition in PANC-1 cells. When exposed to the greatest dose (20 μM), almost 50% of these cells kept growing. The IC0 values of MIA-PaCa-2 and LPc006 cells are 1.0±0.3 and 0.10±0.03 μM, respectively, indicating their higher sensitivity [2]. 3-Deazaneplanocin A hydrochloride (DZNep) hydrochloride, with IC0 values ranging from 0.08 to 0.24 μM, inhibits NSCLC cell line growth in a dose-dependent manner [3].
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| ln Vivo |
3-Deazaneplanocin A hydrochloride Rats have significantly higher survival rates [1]. Patients with acute myeloid leukemia (AML) caused by HL-60 cells had lower NOD/SCID if treated with 3-Deazaneplanocin A hydrochloride (DZNep) and LBH589 (PS) compared to those treated with PS. In rats given saline, body weight increased gradually over time at an average growth rate of 3.19% per day. When rats were given 20 mg/kg of 3-Deazaneplanocin A hydrochloride (DZNep), their relative body weight decreased significantly in the first three days of treatment (-2.0%, -4.9%, and -1.2%). It also significantly decreased starting on the fourth day of administration. At that point, the daily weight growth rate was suppressed to 2.6% [4].
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| Animal Protocol |
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| 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 |
| Molecular Formula |
C12H14N4O3.HCL
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| Molecular Weight |
298.73
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| Exact Mass |
298.083
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| CAS # |
120964-45-6
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| Related CAS # |
3-Deazaneplanocin A;102052-95-9;3-Deazaneplanocin A hydrochloride;120964-45-6
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| PubChem CID |
14563109
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| Appearance |
White to light brown solid powder
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| Melting Point |
168-169℃
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| LogP |
0.591
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
378
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C1=CN=C(C2=C1N(C=N2)[C@@H]3C=C([C@H]([C@H]3O)O)CO)N.Cl
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| InChi Key |
UNSKMHKAFPRFTI-FDKLLANESA-N
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| InChi Code |
InChI=1S/C12H14N4O3.ClH/c13-12-9-7(1-2-14-12)16(5-15-9)8-3-6(4-17)10(18)11(8)19;/h1-3,5,8,10-11,17-19H,4H2,(H2,13,14);1H/t8-,10-,11+;/m1./s1
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| Chemical Name |
(1S,2R,5R)-5-(4-amino-1H-imidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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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) |
Solubility in Formulation 1: 50 mg/mL (167.38 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*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.
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