製品番号: HY-110137A

Furamidine

(別名: DB75; NSC 305831)

4 Cited Publications

カスタマーレビュー

Based on 4 publication(s) in Google Scholar

Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC₅₀ of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC₅₀s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent.

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CAS 番号: 73819-26-8
分子式: C₁₈H₁₆N₄O
分子量:304.35

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

Furamidine 構造式

CAS 番号: 73819-26-8

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (4)
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

IC50: 9.4 μM (Protein arginine methyltransferase 1 (PRMT1)); 166 µM (PRMT5), 283 µM (PRMT6) and >400 µM (PRMT4)^[1]
Parasite^[1]
Tyrosyl-DNA phosphodiesterase 1 (TDP-1)^[2]

Histone Methyltransferase アイソフォーム固有の製品をすべて表示 :

Phosphodiesterase (PDE) アイソフォーム固有の製品をすべて表示 :

Parasite アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	15.5 μM Compound: 2	The compound was tested for cytotoxic potency against A2780R human tumor cell lines. The compound was tested for cytotoxic potency against A2780R human tumor cell lines.	10.1016/S0960-894X(97)00229-1
A2780	IC₅₀	46 μM Compound: 2	The compound was tested for cytotoxic potency against A2780 human tumor cell lines The compound was tested for cytotoxic potency against A2780 human tumor cell lines	10.1016/S0960-894X(97)00229-1
B16	IC₅₀	9.2 μM Compound: DB75	Drug concentration required to inhibit B16 cell growth by 50% after 72 hours of incubation Drug concentration required to inhibit B16 cell growth by 50% after 72 hours of incubation	[PMID: 11985467]
CH1	IC₅₀	46.5 μM Compound: 2	The compound was tested for cytotoxic potency against CH1 human tumor cell lines. The compound was tested for cytotoxic potency against CH1 human tumor cell lines.	10.1016/S0960-894X(97)00229-1
HEK293	IC₅₀	178.04 μM Compound: 7e; DB75	Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 24 hrs by Alamar blue assay Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 24 hrs by Alamar blue assay	[PMID: 28038325]
HEK-293T	IC₅₀	166 μM Compound: 1, DB75, furamidine	Inhibition of HA-tagged recombinant PRMT5 (unknown origin) expressed in HEK293T cells using [3H]SAM and histone H4 (1 to 20) as substrate after 8 mins by P81 filter binding assay Inhibition of HA-tagged recombinant PRMT5 (unknown origin) expressed in HEK293T cells using [3H]SAM and histone H4 (1 to 20) as substrate after 8 mins by P81 filter binding assay	[PMID: 24564570]
L6	IC₅₀	16.4 μM Compound: furamidine	Cytotoxicity against rat L6 cells Cytotoxicity against rat L6 cells	[PMID: 17439202]
L6	IC₅₀	23.3 μM Compound: FMD, DB75, Furamidine	Antiprotozoal activity against intracellular amastigote form of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ infected in rat L6 cells after 48 hrs Antiprotozoal activity against intracellular amastigote form of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ infected in rat L6 cells after 48 hrs	[PMID: 23795673]
L6	IC₅₀	6.4 mM Compound: FMD	Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay	[PMID: 23871911]
L6	IC₅₀	6.4 nM Compound: Furamidine	Cytotoxicity against rat L6 cells by alamar blue assay Cytotoxicity against rat L6 cells by alamar blue assay	[PMID: 17178177]
L6	IC₅₀	6.4 μM Compound: 2	Cytotoxicity against rat L6 cells Cytotoxicity against rat L6 cells	[PMID: 16913722]
L6	IC₅₀	6.4 μM Compound: FMD	Cytotoxicity against rat L6 cells Cytotoxicity against rat L6 cells	[PMID: 19409677]
L6	IC₅₀	6.4 μM Compound: FMD	Cytotoxicity against rat L6 cells by Alamar blue assay Cytotoxicity against rat L6 cells by Alamar blue assay	[PMID: 34146914]
L6	IC₅₀	6.4 μM Compound: FMD, DB75, Furamidine	Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay	[PMID: 23795673]
L6	IC₅₀	6.4 μM Compound: FMD, Furamidine	Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay	[PMID: 24268543]
L6	IC₅₀	6.4 μM Compound: Furamidine	Cytotoxicity against rat L6 cells by alamar blue assay Cytotoxicity against rat L6 cells by alamar blue assay	[PMID: 21194955]
L6	IC₅₀	6.4 μM Compound: IIa	Cytotoxicity against rat L6 cells Cytotoxicity against rat L6 cells	[PMID: 21421317]
L6	IC₅₀	6.5 μM Compound: IIa	Cytotoxicity against rat L6 cells Cytotoxicity against rat L6 cells	[PMID: 20403703]
L6	IC₅₀	6.7 μM Compound: Furamidine	Cytotoxicity against rat L6 cells Cytotoxicity against rat L6 cells	[PMID: 20031421]
L6	IC₅₀	6.7 μM Compound: Table 1, R1C1	Cytotoxicity against rat L6 cells assessed as reduction in cell viability incubated for 70 hrs by Alamar blue based microplate fluorescence assay Cytotoxicity against rat L6 cells assessed as reduction in cell viability incubated for 70 hrs by Alamar blue based microplate fluorescence assay	[PMID: 36958267]
L6	IC₅₀	6400 nM Compound: 2a	Cytotoxicity against rat L6 cells Cytotoxicity against rat L6 cells	[PMID: 19699098]
L6	IC₅₀	6400 nM Compound: 2a	Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay	[PMID: 24012380]
L6	IC₅₀	6400 μM Compound: IIa, furamidine	Cytotoxicity against rat L6 cells Cytotoxicity against rat L6 cells	[PMID: 17976993]
SK-OV-3	IC₅₀	42.5 μM Compound: 2	The compound was tested for cytotoxic potency against SKOV-3 human tumor cell lines. The compound was tested for cytotoxic potency against SKOV-3 human tumor cell lines.	10.1016/S0960-894X(97)00229-1

体外実験

Furamidine (compound 1; 20 μM; 72 hours; leukemia cell lines) inhibits cell growth for most of the leukemia cell lines except HEL cells which have JAK2V617F mutations^[1].
Furamidine (compound 1; 20 μM; 15 hours; 293T cells) treatment significantly reduces the expression level of the methylated GFP-ALY protein in 293T cells^[1].
Furamidine binds duplex DNA in the DNA minor groove selectively at AT rich sites [(A/T)4]. Furamidine can also intercalate between GC base pairs of duplex DNA. Furamidine could therefore interfere with DNA processing enzymes such as TDP-1^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

Meg-01, K562, HL-60, NB4, MOLM13, HEL, CMK, CMY, CMS and CHRF cells
Concentration:

20 μM
Incubation Time:

72 hours
Result:

Inhibited cell growth for most of the leukemia cell lines except HEL cells which have JAK2V617F mutations.

Western Blot Analysis^[1]

Cell Line:

293T cells
Concentration:

20 μM
Incubation Time:

15 hours
Result:

The expression level of the methylated GFP-ALY protein is significantly reduced.

体内実験

Furamidine (1 mg/kg; intraperitoneal injection; 3 times a week and repeated every 4 weeks; for 34 weeks; female NZB/NZW mice) and Irinotecan combined treatment suppresses proteinuria and prolongs survival of lupus-prone NZB/NZW mice. The combination treatment does not change the levels of anti-dsDNA antibodies^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female NZB/NZW mice (6-week-old) with Irinotecan (1 mg/kg)^[3]
Dosage:

1 mg/kg
Administration:

Intraperitoneal injection; 3 times a week and repeated every 4 weeks; for 34 weeks
Result:

Suppressed proteinuria and prolongs survival of lupus-prone NZB/NZW mice combined with Irinotecan.

化学情報

CAS 番号 73819-26-8
分子量 304.35
分子式 C₁₈H₁₆N₄O
SMILES

N=C(C1=CC=C(C2=CC=C(C3=CC=C(C(N)=N)C=C3)O2)C=C1)N
別名

DB75; NSC 305831
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (4)

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Antioxidants (Basel)

A Novel SIRT1 Activator Hydroxygenkwanin Alleviates Osteoporosis by Inhibiting Ferroptosis and Lactylation in Skeletal Stem/Progenitor Cells. [Abstract]

2026 May 12;15(5):612. PMID: 42193234
Cell Rep

CRISPR screening identifies PRMT1 as a key pro-ferroptotic gene via a two-layer regulatory mechanism. [Abstract]

2024 Aug 22;43(9):114662. PMID: 39178116
Int Immunopharmacol

DB75 targets PRMT1 to suppress liver metastasis and synergizes with PD-L1 blockade for enhanced therapeutic efficacy. [Abstract]

2025 Oct 30:164:115327. PMID: 40782428
Research Square Print

September 20th, 2022.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (273 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Yan L, et al. Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. J Med Chem. 2014 Mar 27;57(6):2611-22. [Content Brief]

[2]. Antony S, et al. Novel high-throughput electrochemiluminescent assay for identification of human tyrosyl-DNA phosphodiesterase (Tdp1) inhibitors and characterization of furamidine (NSC 305831) as an inhibitor of Tdp1. Nucleic Acids Res. 2007;35(13):4474-8 [Content Brief]

[3]. Keil A, et al. The Topoisomerase I Inhibitor Irinotecan and the Tyrosyl-DNA Phosphodiesterase 1 Inhibitor Furamidine Synergistically Suppress Murine Lupus Nephritis. Arthritis Rheumatol. 2015 Jul;67(7):1858-67. [Content Brief]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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希釈計算機

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濃度 _(開始) 濃度 _(開始)

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濃度 _(終了) 濃度 _(終了)

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Furamidine

4 Cited Publications

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Furamidine

MedChemExpress（MCE）の使用を引用している文献 Furamidine

Histone Methyltransferase アイソフォーム固有の製品をすべて表示

Phosphodiesterase (PDE) アイソフォーム固有の製品をすべて表示

Parasite アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (4)

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

Furamidine 関連分類

HY-110137A 関連分類