| Description | BT173 is a novel inhibitor of homeodomain interacting protein kinase 2 (HIPK2 ), attenuating renal fibrosis through suppression of the TGF-ß1/Smad3 pathway. |
| In vitro | BT173显著抑制了HIPK2增强肾小管细胞中Smad3下游转录活性的能力。BT173与HIPK2的结合并未抑制HIPK2的激酶活性，而是通过变构干扰方式影响了HIPK2与Smad3的相互作用。体外实验中，BT173处理抑制了TGF-β1诱导的Smad3磷酸化以及人类肾小管上皮细胞中Smad3靶基因的表达。[1] |
| In vivo | 在体内，BT173的给药降低了Smad3的磷酸化作用，并在单侧输尿管阻塞以及Tg26小鼠肾脏纤维化模型中减轻了肾脏纤维化和细胞外基质的沉积[1]。 |
| molecular weight | 382.21 |
| Molecular formula | C18H12BrN3O2 |
| CAS | 2232180-74-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: Insoluble |
| References | 1. Ruijie Liu, et al. A Novel Inhibitor of Homeodomain Interacting Protein Kinase 2 Mitigates Kidney Fibrosis through Inhibition of the TGF-β1/Smad3 Pathway. J Am Soc Nephrol. 2017 Feb 20. pii: ASN.2016080841. |