HDAC1-IN-12
HDAC1-IN-12 is a Plasmodium falciparum HDAC1 (PfHDAC1) inhibitor with an IC50 of 4.1 nM against Pf3D7. HDAC1-IN-12 inhibits PfHDAC1, upregulates histone H3 acetylation in P. falciparum parasites, downregulates malaria invasion-related gene expression, and exhibits favorable safety profiles, improved physicochemical properties, and potent in vivo antimalarial activity. HDAC1-IN-12 can be used for the research of malaria.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C23H26FN7O3
- 分子量:467.50
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
Parasite アイソフォーム固有の製品をすべて表示
More
生物活性
HDAC1-IN-12 (compound 5ac) (72 h) potently inhibits P. falciparum 3D7 growth with high selectivity over human HepG2 and HEK293T cells (IC50 = 4.1 nM for P. falciparum 3D7, 1.5 μM for HepG2, 15 μM for HEK293T)[1].
HDAC1-IN-12 (72 h; 6 h) retains potency against multidrug-resistant P. falciparum strains and inhibits artemisinin-resistant ring-stage parasites (IC50 = 3.9 nM for GB4, 6 nM for CP286, 5.3 nM for 6267)[1].
HDAC1-IN-12 (5 nM, 50 nM; 3 h) increases the acetylation level of P. falciparum histone H3[1].
HDAC1-IN-12 (5-50 nM; 3 h) downregulates invasion-related genes and blocks P. falciparum egress and erythrocyte invasion[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c mice (female, 6–8 weeks old) were inoculated with 105 P. berghei ANKA\r\nparasite-infected erythrocytes via intraperitoneal injection (i.p.) on\r\nday 0.[1]
-
Dosage:30 mg/kg
-
Administration:i.p.; daily; 4 days
-
Result:Showed no detectable parasitemia until day 11, with parasitemia levels remaining markedly lower than the DMSO control group.
化学情報
-
分子量 467.50
-
分子式 C23H26FN7O3
-
SMILES
O=C(C1=CN=C(N2CCN(C(CN3CC(C4=CC(F)=CC=C4N5C)=C5CC3)=O)CC2)N=C1)NO
-
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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
HDAC1-IN-12 関連分類
HY-181010 関連分類
Powered by Bioz
- HDAC1-IN-12
- HDAC
- Parasite
- Plasmodium falciparum histone deacetylase 1
- histone H3 acetylation
- human HepG2 cells
- Plasmodium falciparum
- GB4
- PfHDAC1
- artemisinin-resistant ring-stage parasites
- P. falciparum egress
- Plasmodium berghei ANKA-infected model
- 6267
- malaria invasion-related gene
- P. falciparum 3D7
- BALB/c mice
- HEK293T cells
- erythrocyte invasion
- multidrug-resistant P. falciparum strains
- Quisinostat
- P. falciparum histone H3
- P. falciparum parasites
- CP286
- Inhibitor
- inhibitor
- inhibit