Name: 3-Deazaneplanocin A (DZNep) Hydrochloride
Brand: Selleck Chemicals
SKU: S7120
Rating: 5 (96 reviews)

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품질 관리 (Quality Control)

배치: 순도: 99.92%

99.92

관련 타겟	HDAC JAK BET PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
기타 Histone Methyltransferase 억제제	Pinometostat (EPZ5676) BIX-01294 Trihydrochloride EPZ015666 (GSK3235025) EPZ004777 UNC1999 MM-102 (HMTase Inhibitor IX) Chaetocin SGC 0946 EPZ005687 UNC0638

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주	분석 유형	배양 시간	활성 설명	PMID
human PC3 cells	Cytotoxic assay	72 h	Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay, IC50=9.39 μM.	26010585
human A549 cells	Cytotoxic assay	72 h	Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay, IC50=1.4 μM.	26010585
human SNU638 cells	Cytotoxic assay	72 h	Cytotoxicity against human SNU638 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay, IC50=0.91 μM.	26010585
human SKHEP1 cells	Cytotoxic assay	72 h	Cytotoxicity against human SKHEP1 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay, IC50=0.72 μM.	26010585
human MDA-MB-231 cells	Cytotoxic assay	72 h	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay， IC50=0.3 μM.	26010585
human HCT116 cells	Cytotoxic assay	72 h	Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay, IC50=0.26 μM.	26010585
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량	298.73	화학식	C₁₂H₁₄N₄O₃.HCl	보관 (수령일로부터)	3년-20°C분말
CAS 번호	120964-45-6	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	NSC 617989 HCl			Smiles	C1=CN=C(C2=C1N(C=N2)C3C=C(C(C3O)O)CO)N.Cl

용해도 (Solubility)

In vitro
배치:

DMSO : 60 mg/mL (200.85 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 60 mg/mL

Ethanol : Insoluble

DMSO : 59 mg/mL (197.5 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 59 mg/mL

Ethanol : Insoluble

DMSO : 60 mg/mL (200.85 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 60 mg/mL

Ethanol : Insoluble

DMSO : 60 mg/mL (200.85 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 60 mg/mL

Ethanol : Insoluble

DMSO : 60 mg/mL (200.85 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 60 mg/mL

Ethanol : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	Saline Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	30.000mg/ml (100.43mM)	Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

특징	Carbocyclic analog of adenosine, and acts as anti-tumor and anti-virus inhibitor of EZH2.
Targets/IC₅₀/Ki	S-adenosylhomocysteine hydrolase 50 pM(Ki)
시험관 내(In vitro)	3-Deazaneplanocin A (1.0 μM) results in a significant increase in accumulation of cells in the G0/G1 phase (58.5%) with a concomitant decrease in the number of cells in S phase (35.2%) and G2/M phases (6.3%) of the cell cycle of human acute myeloid leukemia OCI-AML3 cells. 3-Deazaneplanocin A (1.0 μM) induces apoptosis in OCI-AML3 (~50%) and HL-60 cells (~50%), and a more than 90% reduction in colony growth at 48 hr. 3-Deazaneplanocin A depletes EZH2 levels, and inhibits trimethylation of lysine 27 on histone H3 in the HL-60 and OCI-AML3 cells and in primary AML cells. 3-Deazaneplanocin A treatment induces p16, p21, p27, and FBXO32 while depleting cyclin E and HOXA9 levels. 500 nM 3-Deazaneplanocin A induces differentiation of HL-60 to CD11b⁺ cell by nearly 3-folds time at 48 h. 3-Deazaneplanocin A has excellent activity against several viral types. 3-Deazaneplanocin A is activity against vesicular stomatitis in L929 cells, parainfluenza 3 in H.Ep-2, vaccinia and yellow fever viruses in vero cells with IC50 of 0.2, 3.6, 2.1 and 2.9 μg/mL, respectively. 3-Deazaneplanocin A displays a strongly and uniformly leishmanistatic effect on American Leishmania (L mexicana and L brasiliensis) strains in the study with average ID50 of 96 ng/mL, but shows no inhibition against the several T. cruzi and T. rangeli strains tested with concentrations up to 10 μg/mL. At a dose of 200 ng/mL, 3-Deazaneplanocin A inhibits S-adenosyl-L-3H-methylmethionine and 3-thymidine incorporation by promastigotes after four days. At a dose of 100 ng/mL, 3-Deazaneplanocin A eliminates approximately 56% of the L mexicana and L brasiliensis from infected human macrophages.
키나아제 분석	S-adenosylhomocysteine hydrolase activity assay
키나아제 분석	The reaction mixture used for assay of AdoHcyase contains, in a final volume of 0.5 mL, 50 mM potassium phosphate (pH 7.6), 5 mM dithiothreitol, 1 mM EDTA, 10% glycerol, and the enzyme. L-[8- ^14C]AdoHcy is used as substrate and 5 units of calf intestinal adenosine deaminase are included. The reaction is stopped by the addition of 100 μL of 5 M formic acid, and the reaction mixture is then poured onto a column (0.8×2.5 cm) of SP-Sephadex C-25, previously equilibrated in 0.1 M formic acid. Each test tube is rinsed with 0.5 mL of 0.1 M formic acid. [¹⁴C]Inosine formed is eluted from the column by 3.5 mL of 0.1 M formic acid into a scintillation vial. The radioactivity is determined after the addition of 10 mL of scintillation fluid. The amount of enzyme used is about 105 pU, or 75 ng of the purified enzyme. One unit is the amount of enzyme needed to form 1 pmol of product in 1 min at 37 ℃.
생체 내(In vivo)	3-Deazaneplanocin A shows antileukemia activity in vivo. 3-Deazaneplanocin A at the doses of 8 mg/kg shows in vivo antiviral activity against vaccinia virus in a mouse tailpox assay with median of 0.0 poxftail (84% protection). 3-Deazaneplanocin A at the doses ranging from 0.5 to 1.5 mg/kg/day, significantly reduced development of cutaneous leishmanial infection produced in inbred BALB/c mice by L. b. guyanensis inoculation. 3-Deazaneplanocin A induces massively increased interferon-α production in Ebola virus-infected mice. 3-Deazaneplanocin A (s.c. injection of 2 mg/kg postinfection) prevents death in mice infected with 1000 pfu (30 000 LD50) of mouse-adapted EBO-Z. Treatment with 3-Deazaneplanocin A on day 1 reduces mean serum viral titers on day 2 by 100-fold and on day 3 by 100 000-fold, compared with placebo controls, and results in a mean serum IFN-α level of 1420 pg/mL on day 2 and 1830 pg/mL on day 3.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/3790170/ [2] https://pubmed.ncbi.nlm.nih.gov/19638619/ [3] https://pubmed.ncbi.nlm.nih.gov/2544721/ [4] https://pubmed.ncbi.nlm.nih.gov/9347954/ [5] https://pubmed.ncbi.nlm.nih.gov/12076759/ [6] https://pubmed.ncbi.nlm.nih.gov/6639063/

적용 분야 (Applications)

방법	바이오마커	PMID
Western blot	EZH2 / H3K27me3 Suz12 / H3K4me3 / H3K36me2 TGFBR1 / TGFBR2 / Smad3 EED / p21 / p-RB / p27 / p-CDC2 HOXA6 / HOXB3 / HOXC4 / HOXD13 p-JNK / JNK / p-p38 / p38 / p-ERK / ERK / p-IκB-α / IκB-α	27223261
Immunofluorescence	α-tubulin F-actin / Paxillin EZH2 / Mst1	27226494
Growth inhibition assay	Cell viability	27223261

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

3-Deazaneplanocin A (DZNep) Hydrochloride EZH2 inhibitor

화학 구조

분자량: 298.73

품질 관리 (Quality Control)

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

용해도 (Solubility)

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘 (Mechanism of Action)

적용 분야 (Applications)

3-Deazaneplanocin A (DZNep) Hydrochloride EZH2 inhibitor

화학 구조

분자량: 298.73

품질 관리 (Quality Control)

세포 배양, 처리 및 작업 농도 (Cell Culture, Treatment & Working Concentration)

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

용해도 (Solubility)

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘 (Mechanism of Action)

적용 분야 (Applications)

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)