a-186

Z 6031 is a biochemical.

GCA-186 is an effective non-nucleoside HIV-1 reverse transcriptase inhibitor.

Cortistatin-14 is a neuropeptide have structural similarity to somatostatin-14. It is produced in the cortex and hippocampus of central nervous system.

Edaravone (MCI-186) 是一种新型自由基清除剂，能够抑制大鼠与 MMP-9有关的脑出血。

diABZI STING agonist-1 (Tautomerism) (diABZI STING agonist (Compound 3)) 是一个选择性的干扰素基因刺激受体 (STING) 的激动剂，其在人和小鼠中的 EC50 值分别为 130 nM 和 186 nM。。

diABZI STING agonist-1 trihydrochloride 是选择性的干扰素基因刺激受体(STING)激动剂，在人和小鼠中都能发挥作用，其 EC50值分别为 130 和 186 nM。

OUP-186 is a high affinity and human rat species-selective antagonist of histamine H3 receptor. OUP-186 suppressed the proliferation of breast cancer cells. The IC50 values at 48 hours for OUP-186 was approximately 50 μM. OUP-186 potently induced cell dea

PI3K mTOR Inhibitor-1 is a potent, orally bioavailable dual inhibitor of PI3K mTOR (PI3Kα PI3Kβ PI3Kδ PI3Kγ mTOR with IC50s of 20 376 204 46 186 nM)

PKR-IN-C16 是一种特异性蛋白激酶抑制剂。它能够抑制 PKR 的自磷酸化，解除 PKR 在原代神经元细胞培养中诱导的翻译阻断。

AC-186 是一种非甾体雌激素受体 β (ERβ) 激动剂，对 ERβ 和 ERα 的亲和力不同，对 ERβ的 EC50 为 6 nM ，对 ERα 的 EC50 为 5000 nM。AC-186 具有神经保护活性，可用于研究帕金森病。

TL12-186 是一种依赖于 Cereblon 的激酶降解剂，可降解 CDK，BTK，FLT3，Aurora 等激酶。TL12-186 对 CDK2 cyclin A 和 CDK9 cyclin T1 有抑制作用，IC50 分别为 73 和 55 nM。

TL13-27 is a negative control for TL12-186.

Ipivivint, a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer[1]. Ipivivint (SW480 cells; 0.01~10 μM; 1 hour) potently inhibits SRSF5 6 phosphorylation[1].Ipivivint (SW480 cells; 0.03 μM~3 μM; 48 hour) induced apoptosis[1]..Ipivivint (HEK-293T cells; 0.03 μM~3 μM; 1 hour) inhibits Wnt β-catenin signaling induced by Wnt3a[1].Ipivivint (SW480 cells; 0.3~10 μM; 6 hour) increases nuclear speckle enlargement[1].Ipivivint (SW480 cells; 0.3~3μM; 24hours) significantly decreases expression of Wnt target genes (AXIN2, LEF1, MYC, and TCF7) and TCF7L2. SM08502 (SW480 cells; 0.03~3μM; 24hours) inhibits cytoplasmic or nuclear fractions protein expression. Ipivivint (NCI-N87 cells) inhibits proliferation[1].Ipivivint strongly inhibits Wnt pathway signaling activity (EC50 = 0.046 μM) in SW480 colon cancer cells[1]. Ipivivint (25 mg kg; p.o.) potently inhibits tumor SRSF6 phosphorylation[1]. [1]. Tam BY, et al. The CLK inhibitor SM08502 induces anti-tumor activity and reduces Wnt pathway gene expression in gastrointestinal cancer models. Cancer Lett. 2020;473:186-197.

Betamethasone 21-phosphate is a synthetic glucocorticoid.1It prevents increases in macrophage and eosinophil numbers in bronchoalveolar lavage fluid (BALF) and decreases in blood leukocyte numbers in a guinea pig model of parainfluenza-3 viral infection when administered at a dose of 8 mg/kg but does not prevent airway hyperresponsiveness after infection.2Betamethasone 21-phosphate inhibits cell infiltration into the aqueous humor in a rat model of endotoxin-induced uveitis when administered topically or subcutaneously at doses of 0.01-1% or 1 mg/kg, respectively.3It increases maximal lung pressure volume curves in fetal sheep when administered to pregnant ewes at 0.75 gestation at doses of 80 and 170 μg/kg.1Betamethasone 21-phosphate increases body weight, impairs learning and memory, increases anxiolytic behavior, and reduces hippocampal neurogenesis in CD-1 mice but reduces body weight and increases neurogenesis with no effect on anxiety in high-anxiety DBA/2 mice when administered at a dose of approximately 25 mg/kg per day in the drinking water for seven weeks.4Formulations containing betamethasone 12-phosphate and betamethasone acetate have been used in the treatment of severe allergic conditions and a variety of immune-related conditions. 1.Loehle, M., Schwab, M., Kadner, S., et al.Dose-response effects of betamethasone on maturation of the fetal sheep lungAm. J. Obstet. Gynecol.202(2)186.e181-186.e187(2010) 2.Leusink-Muis, A., Ten Broeke, R., Folkerts, G., et al.Betamethasone prevents virus-induced airway inflammation but not airway hyperresponsiveness in guinea pigsClin. Exp. Allergy29(Suppl. 2)82-85(1999) 3.Tsuji, F., Sawa, K., Kato, M., et al.The effects of betamethasone derivatives on endotoxin-induced uveitis in ratExp. Eye Res.64(1)31-36(1997) 4.Aiello, R., Crupi, R., Leo, A., et al.Long-term betamethasone 21-phosphate disodium treatment has distinct effects in CD1 and DBA/2 mice on animal behavior accompanied by opposite effects on neurogenesisBehav. Brain Res.278155-166(2015)

Ro 04-5595 is a selective antagonist of NMDA receptors NR2B subunits. Ro 04-5595 had an EC 50 of 186 ± 32 nmol L. Ro 04-5595 was predicted to bind the EVT-101 binding site, not the ifenprodil-binding site. Specific binding, defined with a new NR2B-specific antagonist Ro 04-5595 at 10 microM was fully inhibited by several compounds with the following rank order of affinities--Ro 25-6981 > CP-101,606 > Ro 04-5595 = ifenprodil >> eliprodil > haloperidol > spermine > spermidine > MgCl2 > CaCl2--and partially inhibited by competitive glutamate recognition site antagonists. Complementary high-resolution autoradiographic images using [3H]Ro04-5595 demonstrated strong binding in NR2B receptor-rich regions and low binding in cerebellum where NR2B concentration is low.

ARC 186 是一种核酸适配体，是高效的补体抑制剂，通过阻断转化酶催化的C5 激活发挥作用。

Dalazatide (ShK-186)是一种针对Kv1.3钾通道的特异性肽抑制剂，用于研究多种自身免疫性疾病，包括多发性硬化症(MS)、红斑狼疮、银屑病、类风湿性关节炎、1型糖尿病及炎症性肠病。

Dalazatide (ShK-186) TFA 是特异性 Kv1.3 钾通道肽抑制剂，适用于研究多发性硬化症 (MS)、红斑狼疮、银屑病、类风湿性关节炎、1型糖尿病及炎症性肠病等自身免疫性疾病。

HBVSeq2 aa:179-186 作为 H-2b 系统中 CTL 反应的有效基序，能在体外再刺激致敏 T 细胞后发挥作用，同时被认为是鉴定乙型肝炎病毒表面抗原的新表位。

PAP-IN-2 (Compound 35)，作为紫色酸性磷酸酶（PAP）的抑制剂，其抑制常数（Ki）为186 nM，适用于开发治疗骨质疏松的化合物。

DHX9-IN-17 (186) 是一种RNA解旋酶DHX9抑制剂，其在细胞实验中的靶向EC50值为0.161 μM。适用于癌症研究。

Moronic acid shows oral therapeutic efficacy in HSV-infected mice and possessed novel anti-HSV activity. It also shows significant anti-HIV activity (EC(50) 186) and was modified to develop more potent anti-AIDS agents. Moronic acid is a new structural lead for anti-EBV drug development, can substantially reduce the numbers of EBV particles produced by the cells after lytic induction. Morolic and moronic acids have shown sustained antidiabetic and antihyperglycemic action possibly mediated by an insulin sensitization with consequent changes of glucose, cholesterol and triglycerides, in part mediated by inhibition of 11β-HSD 1 as indicated by in vitro.