T16922
|
|
|
Others
|
SPOP-IN-6b 是一种有效的斑点型 POZ 蛋白 (SPOP) 抑制剂,IC50 为 3.58 μM,可用于肾癌治疗的研究。 |
T4348
|
|
|
5-HT Receptor
Syk
|
Syk Inhibitor II 是一种可渗透细胞、具有 ATP 竞争性的嘧啶-甲酰胺化合物,可选择性且可逆地抑制 Syk,IC50为 41 nM。 |
T75075
|
|
|
|
4-Amino-1-(β-D-ribofuranosyl)-7H-pyrrolo[2.3-d]pyrimidine-5-carboxamide 是一种具有广泛抗肿瘤活性的嘌呤核苷类似物,主要针对惰性淋巴系统恶性肿瘤。其作用机制包括抑制DNA合成和诱导细胞凋亡(apoptosis)。 |
TNU0272
|
|
|
|
Nucleoside Derivatives - 7-Deaza-purine nucleosides; Natural product; inhibitor of protein kinase C 蛋白激酶抑制剂 |
TNU0278
|
|
|
|
4-Amino-1-(3-deoxy-3-fluoro-b-D-ribofuranosyl)-7H-pyrrolo[2.3-d]pyrimidine-5-carboxamide 是一种有用的有机化合物,可用于生命科学领域的相关研究,其产品编号为 TNU0278。 |
TNU0274
|
|
|
|
Nucleoside Derivatives - 7-Deaza-purine nucleosides; 2’-Modified nucleosides |
T65994
|
|
|
|
Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Cyclic AMP response element-binding protein (CREB) is a transcription factor that is a member of the leucine zipper family of DNA binding proteins. This protein binds as a homodimer to the cAMP-responsive element, an octameric palindrome. The protein is phosphorylated by several protein kinases, and induces transcription of genes in response to hormonal stimulation of the cAMP pathway. Via generating a transcriptionally active complex with β-catenin, CREB acts as a mediator of Wnt signaling.ICG-001 is an inhibitor of β-catenin/CREB mediated transcription. The direct cellular target of ICG-001 is CREB. the inhibitory IC50of ICG-001 against β-catenin/CREB mediated transcription was 3 μM. ICG-001 treatment at the concentration of 25 μM for 24h significantly increased caspase activity in both colon cancer cell lines SW480 and HCT116 cell lines but not in normal colonic epithelial cells CCD-841Co. In a cell growth inhibition assay, the IC50s of ICG-001 against SW480 and HCT116 cells were 4.43 μM and 5.95 μM, respectively.In a SW620 nude mouse xenograft model, an water-soluble analog of ICG-001 given at the dose of 150 mg/kg i.v. once in every 2 days dramatically suppressed tumor growth. In a bleomycin-induced pulmonary fibrosis mice model, ICG-001 given at the dose of 5 mg/kg per day reversed pulmonary fibrosis. In a rat myocardial infarction model, ICG-001 was administrated subcutaneously at the dose of 50 mg/kg/day for 10 days which significantly improved cardiac contractile function after myocardial infarction in the rats. |
T4391
|
|
|
Others
Tyrosine Kinases
Syk
PKC
BTK
|
Syk Inhibitor II (hydrochloride) 是一种非受体酪氨酸激酶,磷酸化后,它与 FcRγ 链的基于免疫受体酪氨酸的激活基序结合,并介导与血小板功能和炎症相关的下游信号传导。 Syk inhibitor II 是一种可渗透细胞的嘧啶-甲酰胺化合物,以 ATP 竞争性方式选择性和可逆地阻断 Syk (IC50 = 41 nM)。它对 PKCε、PKCβII、ZAP-70、Btk 和 Itk 的效力要低得多(IC50s 分别为5.1、11、11.2、15.5 和 22.6 μM)。 |
T72203
|
|
|
|
Reverse transcriptase-IN-3, 作为一种嘧啶-5-羧酰胺衍生物,主要用于抑制HIV-1。它对HIV-1野生型及其突变型病毒株均展示出高效的抑制活性。 |
T78762
|
|
|
|
SIKs-IN-1(compound 8h)为一种嘧啶-5-羧酰胺衍生物,并充当盐诱导激酶(SIKs)的抑制剂。该化合物通过抑制SIK活性,上调IL-10抗炎细胞因子,下调IL-12促炎细胞因子,调控M1/M2巨噬细胞的极化,并在DSS诱导的结肠炎模型中展现出明显的抗炎效果。 |