at 121

AT-121 是一种双重μ-阿片和神经肽受体部分激动剂（Kis 分别为 16.49 和 3.67 nM）。它能刺激[35S]GTPγS 与表达μ-阿片受体或神经肽受体的细胞膜结合（EC50s 分别为 19.6 和 34.7 nM）。AT-121（0.003-0.03 mg kg）能以剂量依赖的方式降低辣椒素诱导的热异感，但不会增加恒河猴的搔抓活动。在恒河猴药物自我给药试验中，AT-121 每次注射剂量为 0.3 至 10 μg kg，它缺乏强化作用（一种潜在的滥用标志），不能减少食物颗粒的强化作用。AT-121（0.01 或 0.03 毫克 千克）不会诱发恒河猴的超痛觉，超痛觉是产生耐受性的标志。AT-121 是一种安全、无成瘾性的缓解疼痛药，具有抗伤害和止痛作用。

AT-121 hydrochloride 是一种 nociception 和 mu 阿片受体 (mu opioid receptor)的双重激动剂，Ki 值分别为 3.67 和 16.49 nM。AT-121 hydrochloride 是一种安全、无成瘾性且科缓解疼痛的化合物，具有抗伤害和止痛活性。

PP121是一种多靶点激酶抑制剂，抑制 PDGFR、Hck、mTOR、VEGFR2、Src、Abl、DNK-PK 的 IC50值分别为2、8、10、12、14、18、60 nM。

CMS-121 是喹诺酮衍生物，对乙酰辅酶 A 羧化酶 1 具有抑制作用，具有口服活性。CMS-121具有保护 HT22 细胞免受缺血和氧化损伤的活性，EC50分别为7 nM 和200 nM。CMS-121具有强大的抗炎，抗氧化，神经保护和肾保护作用。

SKA-121 is a selective KCa3.1 activator (EC50s: 109 nM and 4.4 μM for KCa3.1 and KCa2.3, respectively).

Compound TM11（Antifungal agent 121）是一种苯并咪唑-丙烯腈衍生物的杀菌剂。

YS121 是微粒体前列腺素 E2 合酶-1 (mPGES-1;IC50=3.4 μM) 和 5-脂氧合酶 (5-LOX;IC50=6.5 μM) 的双重抑制剂。在 IL-1β 刺激的 A549 细胞中，YS121以剂量依赖性地方式减少 PGE2 的产生，EC50为 12 μM。

GSK121 Trifluoroacetate 是PAD4的选择性抑制剂。

A 121 is a non-polyene antifungal antibiotic. It is active against a number of filamentous fungi including some plant and human pathogens.

Sul-121 has anti-oxidative capacity. In experimental chronic obstructive pulmonary disease (COPD) models, Sul-121 HCl inhibits airway inflammation and hyperresponsiveness (AHR) prospectively through inhibition of oxidative stress.

TX2-121-1 targets HER3 for proteasome-mediated degradation to inhibit HER3-dependent signalling and growth.

RC 121 is a highly potent somatostatin (SRIF) analog.

KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50= 330 nM).1It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in anin vitromodel of cerebral ischemia.2It reduces infarction volume and increases the latency to fall in an accelerating rotarod test in a mouse model of focal cerebral ischemia induced by transient distal middle cerebral artery occlusion (MCAO) when administered at a dose of 100 mg/kg immediately following occlusion and again at 50 mg/kg following reperfusion. KUS121 (50 mg/kg) inhibits thinning of the retinal outer nuclear layer and preserves visual function in an rd10 mouse model of retinitis pigmentosa.1 1.Ikeda, H.O., Sasaoka, N., Koike, M., et al.Novel VCP modulators mitigate major pathologies of rd10, a mouse model of retinitis pigmentosaSci. Rep.45970(2014) 2.Kinoshita, H., Maki, T., Yasuda, K., et al.KUS121, a valosin-containing protein modulator, attenuates ischemic stroke via preventing ATP depletionSci. Rep.9(1)11519(2019)

NS2 (114-121), Influenza, is a fragment derived from the nonstructural protein 2 (NS2) of the influenza virus. This compound serves as an epitope for influenza research and can be utilized to study the CD8+ cytotoxic T lymphocyte (CTL) in antiviral immune responses.

CM121 is a reversible inhibitor of ALDH1A2 that acts specifically on the active site, exhibiting an IC50 of 0.54 μM and a Kd of 1.1 μM. It exerts its inhibitory effect through multiple hydrophobic interactions.

BCI-121是一种底物竞争性 SMYD3 抑制剂，可抑制癌细胞的增殖。

Antibacterial agent 121 (Compound 10) demonstrates antibacterial properties and exhibits efficacy against mycobacterial strains while also possessing anti-inflammatory activity. This compound finds potential applications in Tuberculosis (TB) research [1].

CYP121A1-IN-1 是一种有效的CYP121A1抑制剂，对抗结核分枝杆菌具有良好的活性 (H37RvMIC90～6.25 μM, ～2.2 μg mL)。CYP121A1-IN-1 通过抑制 CYP121A1 介导的环(l-酪氨酸-l-酪氨酸)转化为真菌环素，可显著减少真菌环素的产生。

Reversin 121为P-糖蛋白(P-glycoprotein) 抑制剂，能增加MDR1的ATP酶活性，可逆转P-糖蛋白介导的多药耐药性，适用于癌症研究。

Anticanceragent 121作为一种hLDHA (人类乳酸脱氢酶 A) 抑制剂，展现出卓越的抗癌活性，适用于抗肿瘤研究。

EGFR-IN-121(compound 15)作为EGFR与VEGFR-2的双重抑制剂,展现出对EGFR的IC50为84 nM,而对VEGFR-2的IC50则为3.5 nM.

TAS-121是一款第三代、高选择性、共价结合的口服EGFR-酪氨酸激酶抑制剂(EGFR-TKI).该化合物在多种EGFR突变体中表现出强效,包括L858R突变(IC50=1.7 nM)、Ex19del突变(IC50=2.7 nM)、L858R T790M双重突变(IC50=0.56 nM)以及Ex19del T790M双重突变(IC50=1.1 nM);同时对野生型EGFR的抑制作用也显著(IC50=8.2 nM).此外,TAS-121对HER2和HER4的抑制作用IC50值分别为110 nM和2.6 nM.该抑制剂能够阻断EGFR及其下游信号通路的磷酸化,从而抑制癌细胞增殖并诱导细胞凋亡.在包括SW48 (EGFR G719S)和NCI-H1975 (EGFR L858R T790M)在内的异种移植模型中,TAS-121展现了其抗肿瘤活性.

MAGL-IN-4 (His121 ARG57) 是选择性的、口服有效的、可透过血脑屏障的、可逆的单酰基甘油脂肪酶抑制剂，IC50=6.2 nM。它主要通过大脑中选择性抑制 MAGL 增加 2-花生四烯酰甘油水平来增强内源性大麻素信号。

Poloxamer 401 L121 是一种由聚氧乙烯和聚氧丙烯组成的嵌段共聚物。它在纳米颗粒工程中被应用于淋巴细胞营养颗粒、抑制多药耐药性和增加佐剂活性，也用于化妆品工业中作为表面活性剂和乳化剂。