M-30

MAO-IN-M30 dihydrochloride 是一种高效的非选择性 MAO-A 和 MAO-B抑制剂 （IC50 < 0.1 μM）。MAO-IN-M30 dihydrochloride 具有口服活性并且可以透过血脑屏障，是一种效的铁螯合剂、自由基清除剂。MAO-IN-M30 dihydrochloride在 帕金森病 （PD） 的体外和体内模型中具有神经保护活性，它会增加大脑多巴胺、血清素和去甲肾上腺素并且可作为开发具有多功能活性的药物以治疗各种神经退行性疾病的先导药物。

CBM-301940 (compound 5) 是一种高效和具有口服活性的MCD(Malonyl-CoA Decarboxylase)抑制剂，IC50=23 nM，改善了大鼠心脏缺血 再灌注模型的心脏效率和功能，具有心脏保护功能。

UM-3006作为一种高效的TLR7 8激动剂，其主要功能是通过激活TLR信号通路来增强免疫反应。该化合物在疫苗佐剂以及免疫疾病的研究和应用中展现出显著的潜力。

AFM-30a hydrochloride 是一种有效的、高度选择性的蛋白质精氨酸脱亚胺酶 2(PAD2) 抑制剂。AFM-30a hydrochloride 能够与 PAD2 结合 (EC50: 9.5 μM)，也能够抑制 H3 瓜氨酸化 (EC50: 0.4 μM)。AFM-30a hydrochloride 能够用于研究某些癌症和多种自身免疫性疾病如类风湿性关节炎 (RA)、多发性硬化症、狼疮和溃疡性结肠炎。

ZM-306416 hydrochloride (CB 676475), 作为一种针对VEGFR的有效抑制剂，其对KDR和Flt的IC50分别为0.1 μM和2 μM。此外，该化合物亦能抑制EGFR，其IC50值低于10 nM。

HM-30181 mesylate monohydrate 是一种口服 P-糖蛋白 (P-gp) 抑制剂，用于提高 P-gp 底物药物的口服生物利用度。

RO8191 (CDM-3008) 是干扰素 (IFN) 受体激动剂。它直接与 IFNα β 受体 2 结合，激活 IFN 刺激的基因表达和 JAK STAT 磷酸化。它通过具有干扰素样活性发挥 cccDNA 调节剂作用，并具有抗 HBV 活性。

ZM 306416 (CB 676475) 是一种 VEGFR 的有效抑制剂，能够抑制 KDR (IC50:0.1 μM) 和 Flt (IC50:2 μM)，也是一种 EGFR 的抑制剂(IC50<10 nM)。

HM30181AK is an inhibitor of the adenosine triphosphate (ATP) binding cassette (ABC) transporter P-glycoprotein (P-gp) with adjuvant activity.

Rastim 30 dkv is a plant growth regulator based on bensoline.

PSAM (pharmacologically selective actuator module) agonist. Activates PSAML141F-GlyR chimeric ion channels. Inhibits activity of neurons expressing PSAML141F-GlyR in vivo and activates locus coeruleus noradrenergic neurons expressing PSAML141F,Y115F-5-HT3 ion channels. Recommended concentration for use in mice is 5 mg kg or lower. Plasmid vectors for the transfection of cells with PSAML141F-GlyR and PSAML141F,Y115F-5-HT3 are available from Addgene. Lovett-Barron et al (2012) Regulation of neuronal input transformations by tunable dendritic inhibition. Nat.Neurosci. 15 423 PMID:22246433 |Satoh et al (2016) Context-dependent gait choice elicited by EphA4 mutation in Lbx1 spinal interneurons. Neuron 89 1046 PMID:26924434 |Atasoy et al (2012) Deconstruction of a neural circuit for hunger. Nature 488 172 PMID:22801496 |Hirschberg et al (2017) Functional dichotomy in spinal- vs prefrontal-projecting locus coeruleus modules splits descending noradrenergic analgesia from ascending aversion and anxiety in rats. Elife 6 e29808 PMID:29027903

ALM301 是一种高度特异性的、口服具有活力的 AKT 抑制剂，能够作用于 AKT1 (IC50: 0.13 μM)、AKT2 (IC50: 0.09 μM) 和 AKT3 (IC50: 2.75 μM)。ALM301 在体外能够抑制 AKT 磷酸化，并对下游信号具有调节作用。ALM301 对癌细胞增殖和肿瘤生长表现出抑制作用。

Encequidar, also known as HM-30181, is an oral P-glycoprotein (P-gp) inhibitor developed to enhance the oral bioavailability of P-gp substrate drugs. Encequidar showed the highest potency (IC(50)=0.63nM) among several MDR1 inhibitors, including cycloporin A, XR9576, and GF120918, and effectively blocked transepithelial transport of paclitaxel in MDCK monolayers (IC(50)=35.4nM). Encequidar is currently under clinical trials.

KNI 174 is a new type of anti‐AIDS drug used as an HIV‐1 protease inhibitor

AM-8508 is a potent and selective PI3Kδ inhibitor. AM-8508 showed good cellular potency (in vitro pAKT IC50 = 4.6 nM ). AM-8505 xhibited excellent HWB potency (HWB (pAKT) IC50 = 2.7 nM). AM-8508 inhibit KLH-specific antibodies in animal models, signifying its potential for the treatment of human inflammatory diseases. PI3Kα and PI3Kβ are ubiquitously expressed and play a role in cell growth, division, and survival.

CM304 is a highly selective sigma-1 receptor antagonist.

Mavrilimumab (CAM 3001) 是一种单克隆抗体，具有抗病毒活性，对粒细胞-巨噬细胞集落刺激因子 (GM-CSF) 受体的 α 亚基有亲和力，并阻止 GM-CSF 下游细胞内信号传导。GM-CSF 可能与呼吸衰竭和死亡相关的过度活跃炎症反应有关，可用于研究类风湿性关节炎。

Gancotamab (MM-302) 是一种靶向 HER2 的聚乙二醇化脂质体，它封装了阿霉素以促进其递送至 HER2 过表达的肿瘤细胞，同时限制了对非靶组织（包括心脏）的暴露。Gancotamab具有抗肿瘤活性，可用于研究晚期 HER2 阳性乳腺癌。

STM3006 是一种具有口服活性、选择性和和高效性的 METTL3 抑制剂，具有抗肿瘤活性，可用于研究急性髓系白血病(AML)。

BM30 是一种肽模拟物，属于选择性的NTMT1和NTMT2抑制剂，其对NTMT1的IC50为0.89 μM。

Fervenulin 具有杀灭线虫活性，抑制线虫M. incognita 卵孵化和 J2 的校正死亡率，MIC 分别为 30 μg mL 和 120 μg mL。

RIPK2 IN 10W 对RIPK2的IC50值为0.6 nM，是RIPK1的50000倍以上（IC50>30μM）。RIPK2 IN 10W 具有高激酶选择性，抑制RIPK2，防止NOD诱导的细胞因子在胞壁酰二肽（MDP）刺激后产生。RIPK2作为治疗靶点显示出治疗炎症性肠病的潜在能力。

7-oxo Staurosporine is an antibiotic originally isolated from S. platensis with diverse biological activites. It inhibits PKC, PKA, phosphorylase kinase, EGFR, and c-Src in vitro (IC50s = 9, 26, 5, 200, and 800 nM, respectively). 7-oxo Staurosporine induces cell cycle arrest in the G2/M phase in human leukemia K562 cells with a minimal effective dose (MED) of 30 ng/ml. It is cytotoxic to P388 mouse leukemia cells that are resistant and susceptible to doxorubicin . 7-oxo Staurosporine inhibits growth of the mycelial, but not yeast form of C. albicans, C. krusei, C. tropicalis, and C. lusitaniae (MICs = 3.1-25 μg/ml). It increases sphingomyelin synthesis in CHO-K1 cells when used at a concentration of 50 nM.

β-Defensin-2 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius.2β-Defensin-2 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes.3It also stimulates calcium mobilization, migration, and proliferation of keratinocytes when used at concentrations of 30, 10, and 40 μg/ml, respectively. β-Defensin-2 induces IL-31 production by human peripheral blood-derived mast cellsin vitrowhen used at a concentration of 10 μg/ml and by rat mast cellsin vivofollowing a 500 ng intradermal dose.4Expression of β-defensin-2 is increased in psoriatic skin and chronic wounds.5,6 1.Lehrer, R.I.Primate defensinsNat. Rev. Microbiol.2(9)727-738(2004) 2.Ouhara, K., Komatsuzawa, H., Yamada, S., et al.Susceptibilities of periodontopathogenic and cariogenic bacteria to antibacterial peptides, β-defensins and LL37, produced by human epithelial cellsJ. Antimicrob. Chemother.55(6)888-896(2005) 3.Niyonsaba, F., Ushio, H., Nakano, N., et al.Antimicrobial peptides human β-defensins stimulate epidermal keratinocyte migration, proliferation and production of proinflammatory cytokines and chemokinesJ. Invest. Dermatol.127(3)594-604(2007) 4.Niyonsaba, F., Ushio, H., Hara, M., et al.Antimicrobial peptides human β-defensins and cathelicidin LL-37 induce the secretion of a pruritogenic cytokine IL-31 by human mast cellsJ. Immunol.184(7)3526-3534(2010) 5.Huh, W.-K., Oono, T., Shirafuji, Y., et al.Dynamic alteration of human β-defensin 2 localization from cytoplasm to intercellular space in psoriatic skinJ. Mol. Med. (Berl.)80(10)678-684(2002) 6.Butmarc, J., Yufit, T., Carson, P., et al.Human β-defensin-2 expression is increased in chronic woundsWound Repair Regen.12(4)439-443(2004)