10
2
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T17284 |
Zardaverine
BY 290,B 84290 |
PDE | Metabolism |
Zardaverine (BY 290) 是一种可口服且具有选择性和有效性的 PDE3/4 抑制剂 ,具有支气管扩张活性和抗肝癌活性。Zardaverine 在血小板中的作用是通过PDE III同工酶介导,可用于研究急性肾衰竭呵呵慢性气流阻塞。 | |||
TP1195 |
Cibinetide
ARA290 |
Others | Others |
Cibinetide (ARA290) 是特异性的 erythropoietin/CD131 heteroreceptor 的激动剂,是一种 EPO 衍生物,常用于神经系统疾病研究。 | |||
T5058 |
Pamiparib
BGB-290 |
PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Pamiparib (BGB-290) 是一种具有口服活性、强效、高选择性的 PARP 抑制剂,对PARP1和PARP2的IC50值分别为 0.9 nM 和 0.5 nM。它具有强大的 PARP 捕获能力,具有穿透大脑的能力,可用于研究癌症。 | |||
T5444 |
CLP290
CLP-290 |
Potassium Channel | Membrane transporter/Ion channel |
CLP-290 是一种神经特异性 K+-Cl−共转运体 KCC2的口服激活剂,在多种神经和精神疾病方面具有研究潜力。CLP290 能显著降低 STZ 大鼠的血液中 AVP 和血糖水平。 | |||
TP1271L |
Calmodulin-Dependent Protein Kinase II 290-309 acetate
Calmodulin-Dependent Protein Kinase II 290-309 acetate (115044-69-4 Free base) |
CaMK | Neuroscience |
Calmodulin-Dependent Protein Kinase II 290-309 acetate 是 Ca2+/calmodulin-dependent protein kinase II 的有效拮抗剂(IC50 = 52 nM)。 | |||
T69931 |
MFH290
|
||
MFH290 is a novel cysteine (Cys)-directed covalent inhibitor of CDK12/13. MFH290 forms a covalent bond with Cys-1039 of CDK12, exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes. Importantly, these effects were demonstrated to be CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290 and restored Pol II CTD phosphorylation ... | |||
T16101 | ML-290 | RXFP receptor | GPCR/G Protein |
ML-290 是一个松弛素/胰岛素样肽受体 (RXFP1) 偏向变构激动剂,为抗纤维化基因激活剂,EC50为 94 nM。 | |||
T75959 |
Calmodulin-Dependent Protein Kinase II(290-309) acetate
|
||
Calmodulin-Dependent Protein Kinase II (290-309) acetate 是有效的 CaMK 拮抗剂, 抑制抑制 Ca2+/钙调蛋白依赖性蛋白激酶II 的IC50值为52 nM。 | |||
T82514 |
EAC3I
|
||
EAC3I,一种生物活性肽,序列(KKALHRQEAVDAL)源自autocamtide-3的衍生抑制肽,模拟CaMKII调节域内的自抑制区域(残基278-290)。该肽通过与催化位点进行竞争性结合发挥作用。 | |||
T12407 |
Pepstatin Ammonium
Pepstatin A Ammonium |
Others | Others |
Pepstatin Ammonium is a specific inhibitor of aspartic proteaseproduced by actinomycetes(hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T75705 | Pepstatin Trifluoroacetate | ||
Pepstatin (Pepstatin A) Trifluoroacetate 是一种由放线菌产生的特异性天冬氨酸蛋白酶(aspartic proteases)抑制剂,口服活性强。该化合物能有效抑制hemoglobin-pepsin、hemoglobin-proctase、casein-pepsin、casein-proctase、casein-acid protease和hemoglobin-acid protease的活性,其IC50值分别为4.5 nM、6.2 nM、150 nM、290 nM、520 nM和260 nM。此外,对HIV protease也有抑制作用。 | |||
TN4140 |
Glochidiol
|
Others | Others |
Glochidiol exhibits strong inhibitory effects against all three human tumor cell lines (MCF-7, NCI-H-460 and SF-268), it exerts its antiproliferative activity through the involvement of apoptosis. It exhibits a strong inhibitory effect on mouse skin tumor |