| Bioactivity | HDAC-IN-76 (compound 6i) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-76 IC50 values of 30 nM and 98 nM for Pf3D7 (chloroquine (HY-17589A) drug-susceptible strain) and PfDd2 (chloroquine (HY-17589A) drug-resistant strain), has a highly potent antimalarial activity against asexual blood-stage Plasmodium, respectively, and exhibits selective inhibition against parasites, with IC50 values of 7 nM and 9 nM for human HDAC1 and HDAC6, respectively, while inhibiting PfHDAC1[1]. |
| Invitro | HDAC-IN-76 对 HEK293 细胞毒性低[1]。HDAC-IN-76 (1 μM) 有效抑制 PfHDAC1，抑制率为 70.2%[1]。HDAC-IN-76 对肝期寄生虫活性较低 (IC50 PbEEF (伯氏疟原虫红细胞外肝期寄生虫)=0.25 μM)，具有良好的微粒体稳定性 (t1/2 > 60 min)，并在 HEK293 细胞中的毒性较低 (IC50=136 μM，选择指数 SI=544)[1]。HDAC-IN-76 能够有效进入 HepG2 细胞，抑制 HDAC 活性[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> HDAC-IN-76 相关抗体: Cell Cytotoxicity Assay[1] Cell Line: |
| Formula | C27H26N4O4 |
| Molar Mass | 470.52 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Daniel Stopper , et al. Development of peptoid-based heteroaryl-decorated histone deacetylase (HDAC) inhibitors with dual-stage antiplasmodial activity. Eur J Med Chem. 2024 Nov 5:277:116782. |