i-100

CI-1002 is a novel anticholinesterase and muscarinic antagonist that can be used to treat cognitive dysfunction in AD with fewer peripheral side effects.

(S)-BI-1001 is an active S-enantiomer of BI-1001. (S)-BI-1001 has antiviral potency against HIV-1 integrase (IC50: 28 nM, and EC50: 450 nM and a Kd: 4.7 μM).

AJI-100是一种针对Aurora Kinase A和JAK2的双靶点抑制剂，其IC50值分别为12.7 nM和18.5 nM。该化合物通过抑制Aurora Kinase A实现对T细胞有丝分裂进程和细胞极性的调控，并通过阻断JAK2活性减少STAT3的磷酸化，从而抑制TH1和TH17细胞的分化。AJI-100主要用于研究调节免疫反应及防治移植物抗宿主病(GVHD)的应用潜力。

BI1002494 is an effective and selective Syk inhibitor.

JAMI1001A is a positive allosteric modulator of the AMPA receptor, effectively modulating the deactivation and desensitization of both flip and flop receptor isoforms.

KNI 10033 is a potent inhibitor of HIV protease

JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19. JH-XI-10-02 is a potent and selective degrader of CDK8, with an IC50 of 159 nM, based on PROTAC.

ZD-6888 is an angiotensin type 1 receptor antagonist potentially for the treatment of hypertension.

TREM2 agonist-1 (I-246) 是一种髓系细胞触发受体 2 (triggering receptor expressed on myeloid cells-2,TREM2) 激动剂 (EC50: 3.0 μM-100 μM)。该化合物的粉末形式不稳定，建议选择其他盐形式产品。

Finasteride (MK-906) 是 5α-还原酶的竞争性抑制剂，对 II 型 5α-还原酶的IC50为 4.2 nM，对 II 型 5α-还原酶的亲和力是 I 型酶的 100 倍。它可用于研究前列腺增生和雄激素性脱发。

Chlorin E6 (CE6) 是一种第二代光敏剂，在与辐照结合使用时具有抗肿瘤活性。在植入性纤维肉瘤的小鼠模型中，Chlorin E6（2.5-10 毫克 千克，静脉注射，50-200 焦耳 平方厘米的辐照）在不同程度的辐照后会导致肿瘤完全消失。在一项针对支气管源性早期浅表鳞状细胞癌患者的 I 期临床研究中，对包括 Chlorin E6 在内的制剂进行了测试，结果良好（40 毫克 平方米，静脉注射，100 焦耳 平方厘米的激光辐照）。在一项针对早期肺癌患者的二期临床试验中，同样的给药模式使 82.9% 的患者获得了完全应答。Chlorin E6 已被研究为一种纳米技术给药工具。

PF-543 hydrochloride (PF-543) 是一种选择性可逆和鞘氨醇竞争性SPHK1抑制剂，对SPHK1的选择性是 SPHK2 的 100 倍以上。它还是全血中 1-磷酸鞘氨醇形成的有效抑制剂，诱导细胞凋亡、坏死和自噬。

FTI-277 hydrochloride (FTI 277 HCl) 是一种法尼基转移酶FTase 抑制剂，高效 Ras CAAX 肽模拟物，可抑制H-Ras 和K-Ras 信号转导，还可抑制hepatitis delta virus 感染。

ACY-738 对重组 HDAC6 具有抑制活性IC50值为 1.7 nM。它也可抑制 HDAC1、HDAC2 和 HDAC3 的活性，IC50值分别为 94、128 和 218 nM。

RS 25344 hydrochloride 是 cAMP-磷酸二酯酶 4 的选择性抑制剂，在人淋巴细胞中的 IC50为 0.28 nM，对 PDE I、II、III 仅具有微弱的抑制作用，IC50分别为 >100 μM、160 μM、330 μM。它具有抗炎、增强记忆力和认知能力以及抗肿瘤活性。

Harzianopyridone is an atpenin-like compound that functions as an inhibitor of mammalian and nematode mitochondrial complex II, also known as succinate:ubiquinone oxidoreductase (SQR), demonstrating IC50 values of 0.017, 0.2, and 2 μM against bovine, rat, and nematode complex II, respectively. Additionally, it inhibits nematode quinol-fumarate reductase (QFR) with an IC50 value of 0.36 μM. Significantly selective for complex II over complexes I and III in rats and cattle, as well as complex I in nematodes, with IC50 values exceeding 100 μM, it exhibits notable antibacterial and antifungal properties, with EC50 values of 35.9, 42.2, 60.4, and 50.2 μg ml against R. solani, S. rolfsii, M. phaseolina, and F. oxysporum, respectively.

SMARCA2 degrader-2 (compound I-322) 作为一种针对SMARCA2的PROTAC降解剂，在 A549 细胞中表现出极高的效率，其DC50值低于100 nM，并在24小时处理后，SMARCA2 蛋白的最大降解率 (Dmax%) 超过90。

SMARCA2 degrader-3 (compound I-323) 作为一种针对SMARCA2的PROTAC降解剂，在A549细胞中表现出卓越的降解活性，其DC50值低于100 nM，并在24小时处理后，其最大降解率 (Dmax%) 超过90%。

PROTAC SMARCA2 degrader-9 (compound I-285) 作为靶向SMARCA2的PROTAC降解剂, 在 A549 细胞中表现出卓越的效果, 其DC50 值低于100 nM，并且在处理24小时后达到超过90%的最大降解率 (Dmax%)。

PROTAC SMARCA2 4-degrader-32 (compound I-446) 作为一种针对SMARCA2和SMARCA4的PROTAC降解剂，展示了极高的效力。在A549细胞系中，其对SMARCA2 4蛋白的DC50s均低于100 nM，24小时处理后的最大降解率 (Dmax%) 均超过90%。

PROTAC SMARCA2 degrader-16 (compound I-278)，作为针对SMARCA2的降解剂，在A549细胞中展示出显著的降解活性，其DC50值小于100 nM，并在24小时处理后达到超过90%的最大降解率（Dmax%）。

PROTAC SMARCA2 4-degrader-29 (Compound I-279) 作为一种针对 SWI SNF 复合体的催化亚基 SMARCA2 和 SMARCA4 的降解剂，表现出了优异的活性。在 A549 细胞中对 SMARCA2 的降解 DC50 值小于 100 nM，在 MV411 细胞中对 SMARCA4 的降解 DC50 同样小于 100 nM。

Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF1 over CRF2 receptors (Kis = 0.66 and >100 nM, respectively) and induces cAMP production in CHO cells expressing CRF2 (EC50 = 0.14 nM). In vivo, urocortin II suppresses nighttime food intake by 35% in rats when administered intracerebroventricularly at a dose of 1 μg. Urocortin II (0.1 and 0.5 μg, i.c.v) stimulates fecal pellet output, increases distal colonic transit, and inhibits gastric emptying in mice.2References1. Reyes, T.M., Lewis, K., Perrin, M.H., et al. Urocortin II: A member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc. Natl. Acad. Sci. U.S.A. 98(5), 2843-2848 (2001).2. Martinez, V., Wang, L., Million, M., et al. Urocortins and the regulation of gastrointestinal motor function and visceral pain. Peptides 25(10), 1733-1744 (2004). Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF1 over CRF2 receptors (Kis = 0.66 and >100 nM, respectively) and induces cAMP production in CHO cells expressing CRF2 (EC50 = 0.14 nM). In vivo, urocortin II suppresses nighttime food intake by 35% in rats when administered intracerebroventricularly at a dose of 1 μg. Urocortin II (0.1 and 0.5 μg, i.c.v) stimulates fecal pellet output, increases distal colonic transit, and inhibits gastric emptying in mice.2 References1. Reyes, T.M., Lewis, K., Perrin, M.H., et al. Urocortin II: A member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc. Natl. Acad. Sci. U.S.A. 98(5), 2843-2848 (2001).2. Martinez, V., Wang, L., Million, M., et al. Urocortins and the regulation of gastrointestinal motor function and visceral pain. Peptides 25(10), 1733-1744 (2004).

VX-148是一种新型、非竞争性的IMPDH抑制剂，对IMPDH II型酶具有6 nM的K(i)值。在抑制原发性人类淋巴细胞（IC(50)值约为80 nM）的增殖方面，VX-148比麦考酚酸和VX-497略为有效。外源性鸟苷的存在可以缓解VX-148的抑制活性。VX-148不抑制如成纤维细胞等非淋巴细胞类型的增殖，显示出对IMPDH活性的选择性抑制。VX-148在大鼠和小鼠中具有口服生物利用度；口服VX-148以剂量依赖性抑制小鼠的初级抗体反应，ED(50)值为38 mg kg b.i.d。在小鼠中，VX-148以100 mg kg b.i.d.的剂量显著延长皮肤移植的存活时间。