3-Deazaneplanocin A (DZNep) hydrochloride (Synonyms: 2,3DMMC) |
| Catalog No.GC17907 |
3-Deazaneplanocin A (DZNep) hydrochloride는 아데노신 유사물이자 경쟁적인 S-아데노실호모시스테인 횡분해효소 억제제로서 세포 없는 실험에서 Ki 값이 50pM이다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 120964-45-6
Sample solution is provided at 25 µL, 10mM.
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3-Deazaneplanocin A (DZNep) hydrochloride는 아데노신 유사물이자 경쟁적인 S-아데노실호모시스테인 횡분해효소 억제제로서 세포 없는 실험에서 Ki 값이 50pM이다. 이로 인해 세포 내 AdoHcy가 쌓이게 되어 S-아데노실-L-멩시온에 의존하는 KMTase 활성이 억제된다[1-2,5]. 3-Deazaneplanocin A(DZNep) hydrochloride는 또한 멜트릴트랜스퍼아제의 활동을 억제하여 mRNA의 과소 멜시티레이션을 유도하는 것으로 나타났다[3].
3-Deazaneplanocin A(DZNep) hydrochloride(100-750 nmol/L； 48시간) 치료는 AML 세포의 세포주기 정지와 조각사를 유도하고 덩크 형성 능력을 현저하게 낮추었다[4]. 3-Deazaneplanocin A(DZNep) hydrochloride는 유방암 세포에서 PRC2 복합체의 표현 수준을 고갈시키고 3Me H3K27 표시의 상실과 표현 유전적으로 침묵된 대상의 억제 해제와 함께 보고되었다[6]. 3-Deazaneplanocin A(DZNep) hydrochloride(10-6M-10-5M; 2일)는 세포 배양에서 벡터성 스톰티, 비인플루엔자 타입 3, 옐로 파이버, 백신아열 바이러스에 대한 탁월한 항바이럴활성을 나타냈다[1].
3-Deazaneplanocin A(DZNep) hydrochloride(1 mg/kg; 복강 주사; 2주)와 파노비노스타트는 AML 세포의 조각사를 유도하고 HL-60 백혈병을 가진 비비만 당뇨병/심각한 면역결핍 쥐의 생존률을 현저하게 향상시켰다[4]. 3-Deazaneplanocin A(DZNep)(복강 주사; 0.5-1.5 mg/kg /일; 2주)는 L. b. guyanensis 접종으로 인한 BALB/c 순수 계통 쥐의 피부에서의 리시마니아 감염 발생률을 현저하게 낮추었다[7].
References:
[1]. Glazer RI, Hartman KD, et,al.3-Deazaneplanocin: a new and potent inhibitor of S-adenosylhomocysteine hydrolase and its effects on human promyelocytic leukemia cell line HL-60. Biochem Biophys Res Commun. 1986 Mar 13;135(2):688-94. doi: 10.1016/0006-291x(86)90048-3. PMID: 3457563.
[2]. Bray M, Driscoll J, et,al.Treatment of lethal Ebola virus infection in mice with a single dose of an S-adenosyl-L-homocysteine hydrolase inhibitor. Antiviral Res. 2000 Feb;45(2):135-47. doi: 10.1016/s0166-3542(00)00066-8. PMID: 10809022.
[3]. Jiang X, Tan J, et,al. DACT3 is an epigenetic regulator of Wnt/beta-catenin signaling in colorectal cancer and is a therapeutic target of histone modifications. Cancer Cell. 2008 Jun;13(6):529-41. doi: 10.1016/j.ccr.2008.04.019. PMID: 18538736; PMCID: PMC2577847.
[4]. Fiskus W, Wang Y, et,al.Combined epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A and the histone deacetylase inhibitor panobinostat against human AML cells. Blood. 2009 Sep 24;114(13):2733-43. doi: 10.1182/blood-2009-03-213496. Epub 2009 Jul 28. PMID: 19638619; PMCID: PMC2756128.
[5]. Tseng CK, Marquez VE, Fuller RW, Goldstein BM, Haines DR, McPherson H, Parsons JL, Shannon WM, Arnett G, Hollingshead M, et al. Synthesis of 3-deazaneplanocin A, a powerful inhibitor of S-adenosylhomocysteine hydrolase with potent and selective in vitro and in vivo antiviral activities. J Med Chem. 1989 Jul;32(7):1442-6. doi: 10.1021/jm00127a007. PMID: 2544721.
[6]. Tan J, Yang X, et,al. Pharmacologic disruption of Polycomb-repressive complex 2-mediated gene repression selectively induces apoptosis in cancer cells. Genes Dev. 2007 May 1;21(9):1050-63. doi: 10.1101/gad.1524107. Epub 2007 Apr 16. PMID: 17437993; PMCID: PMC1855231.
[7]. Avila JL, Avila A, et,al.Specific inhibitory effect of 3-deazaneplanocin A against several Leishmania mexicana and L. braziliensis strains. Am J Trop Med Hyg. 1997 Oct;57(4):407-12. doi: 10.4269/ajtmh.1997.57.407. PMID: 9347954.
| 세포 실험 [1]: | |
세포 라인 | OCI-AML3 세포 |
제조 방법 | 세포는 지정된 농도의 DZNep으로 24시간 동안 처리되었습니다. |
반응 조건 | DZNep (0/1.0 µM); 24 시간 |
응용 분야 | DZNep(1.0 µM)으로 OCI-AML3 세포를 처리하면 G0/G1 단계의 세포 축적이 현저하게 증가하고 동시에 세포 주기의 S 단계와 G2/M 단계의 세포 수가 감소합니다. |
| 동물 실험 [2]: | |
동물 모형 | 암컷 비비만 당뇨병/심각한 결합 노결핍(NOD/SCID) 쥐 |
제조 방법 | HL-60 세포(500만)가 쥐의 꼬리 동맥에 주사되었습니다. 각각의 치료법은 7마리씩의 쥐 그룹에서 다음과 같이 행해졌습니다: 운송차량만, 1 mg/kg DZNep, 10 mg/kg PS, 그리고 DZNep와 PS. 치료는 7일째에 시작되었습니다. DZNep은 2주 동안 매주 두 번씩 복강 주사로 행해졌으며, 그 후 중단되었습니다. |
제형 | 1 mg/kg DZNep; i.p.; 매주 두번 , 2 주 동안 |
응용 분야 | NOD/SCID 쥐에 DZNep을 투여한 후, HL-60 세포로 인한AML의 생존률이 현저하게 향상되었습니다. |
참고문헌: [1]. Tseng CK, Marquez VE, Fuller RW, Goldstein BM, Haines DR, McPherson H, Parsons JL, Shannon WM, Arnett G, Hollingshead M, et al. Synthesis of 3-deazaneplanocin A, a powerful inhibitor of S-adenosylhomocysteine hydrolase with potent and selective in vitro and in vivo antiviral activities. J Med Chem. 1989 Jul;32(7):1442-6. doi: 10.1021/jm00127a007. PMID: 2544721. | |
| Cas No. | 120964-45-6 | SDF | |
| Synonyms | 2,3DMMC | ||
| Chemical Name | (1S,2R,5R)-5-(4-aminoimidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol;hydrochloride | ||
| Canonical SMILES | C1=CN=C(C2=C1N(C=N2)C3C=C(C(C3O)O)CO)N.Cl | ||
| Formula | C12H14N4O3.HCl | M.Wt | 298.73 |
| Solubility | ≥ 14.9mg/mL in DMSO, ≥ 18.32 mg/mL in Water with ultrasonic | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.3475 mL | 16.7375 mL | 33.475 mL |
| 5 mM | 0.6695 mL | 3.3475 mL | 6.695 mL |
| 10 mM | 0.3348 mL | 1.6738 mL | 3.3475 mL |
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- Purity: >99.50%
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