inh-1

INH1 (IBT13131) 通过直接结合Hec1，特异性干扰 Hec1 Nek2 的相互作用。它在体内外均表现出良好的抗肿瘤活性。

ODN INH-1 是一个回文抑制性寡核苷酸，也是TLR9诱导的B细胞和巨噬细胞的有效抑制剂。

T3Inh-1 是一种有效的选择性 ppGalNAc-T3 抑制剂，IC50 为 7 µM。 T3Inh-1 可预防乳腺癌细胞。 T3Inh-1 降低组织细胞和小鼠中的 FGF23 激素水平，而不会引起任何毒副作用。

INH-13 is a Aurora inhibitor.

CFTR(inh)-172 (CFTR Inhibitor-172) 是一种不依赖电压的选择性 CFTR 抑制剂，在2分钟内可逆地抑制CFTR 短路电流的Ki 值为300 nM。

INH14 是 IKKα (IC50:8.97 μM) IKKβ (IC50:3.59 μM) 的抑制剂。它能够抑制 IKKα β 依赖性 TLR 炎症反应，抑制 TAK1 TAB1 的下游和 NF-kB 信号通路。它具有抗炎和抗癌作用。

INH154 是一种高效的 Nek2 和 Hec1 结合抑制剂，能够抑制 Hela 细胞(IC50:200 nM)、 MB468 细胞(IC50:120 nM)。

Prostaglandin H1 是 DGLA 的环氧化酶代谢物，也是一种 CRTh2 激动剂以及 1 系列抗炎前列腺素的前体物质。Prostaglandin H1 可用于炎症的研究。

MK-8712 is a monobactam beta-lactamase inhibitor.

Maximin H1是一种抗菌肽，由中华红腹蟾蜍(Bombina maxima)皮肤分泌物提取得到。该化合物对Escherichia coli ATCC 25922、Staphylococcus aureus ATCC 25923、Bacillus pyocyaneus CMCC B1010和Candida albicans ATCC 2002表现出抗菌活性，其最小抑菌浓度(MIC)值分别为9、4.5、9、4.5 μg ml。

Sanguiin h 11 is a compound purified from the plant Sanguisorba officinalis and has proven to be a potent inhibitor of chemoattractant-dependent and independent neutrophil movement.

Ajugamarin H1 是一种天然化合物，可作为天然产物对照品。

Biotin-H10，作为一种特异性抑制剂，针对前梯度蛋白2 (AGR2)，其KD值为6.4 nM。此化合物能有效抑制癌细胞活力。

Bombinin H1是Bombina variegata蛾皮肤中提取的抗菌肽。该肽对大肠杆菌D21的致死浓度为3.8μM，而对金黄色葡萄球菌Cowan 1的致死浓度为2.1μM。

OPC-167832 is a potent and orally active dprE1 Inhibitor with an IC50 of 0.258 μM. OPC-167832 has antituberculosis activity and can be used for the research of tuberculosis caused by Mycobacterium tuberculosis[1]. OPC-167832 exhibits very low MICs against laboratory strains of M. tuberculosis H37Rv (MIC: 0.0005 μg ml) and Kurono (MIC: 0.0005 μg ml) and strains with monoresistance to rifampin (RIF), isoniazid (INH), ethambutol (EMB), streptomycin (STR), and pyrazinamide (PZA) (MIC: 0.00024-0.001 μg ml). However, OPC-167832 has minimal or no activity against standard strains of nonmycobacterial aerobic and anaerobic bacteria[1].The IC90 values of OPC-167832 against intracellular M. tuberculosis strains H37Rv and Kurono are 0.0048 and 0.0027 μg ml, respectively. OPC-167832 shows bactericidal activity against intracellular M. tuberculosis at a low concentration, and the bactericidal activity is saturated at concentrations of 0.004 μg ml or higher[1]. OPC-167832 (oral administration; 0.625-10 mg kg) exhibits a good pharmacokinetic characteristic. The plasma reaches peak at 0.5 h to 1.0 h (tmax) and is eliminated with a half-life (t1 2) of 1.3 h to 2.1 h OPC-167832 distribution in the lungs is approximately 2 times higher than that in plasma, and the Cmax and AUCt of OPC-167832 in plasma and the lungs shows dose dependency[1].OPC-167832 (oral administration; 0.625-10 mg kg; 4 weeks) significantly reduces lung CFU compared to the vehicle group. The dose-dependent decrease of lung CFU is observed from 0.625 mg kg to 2.5 mg kg. In a M. tuberculosis Kurono-infected ICR female mice model. OPC-167832 combines with DMD, BDQ, or LVX via oral gavage exhibits significantly higher efficacies than each single agent alone[1].[1].OPC-167832 (oral gavage; 2.5 mg kg; combination with DCMB; 12 weeks) demonstrates the most potent efficacy when compares with DC, DCB. The lung CFU count after 6 weeks of treatment is below the detection limit, and at the end of just 8 weeks of treatment, the bacteria in the lungs of all the evaluated mice had already been eradicate[1]. [1]. Norimitsu Hariguchi, et al. OPC-167832, a Novel Carbostyril Derivative with Potent Antituberculosis Activity as a DprE1 Inhibitor.Antimicrob Agents Chemother. 2020 May 21;64(6):e02020-19.

RNF5 agonist 1 (analog-1) 是 RNF5 inhibitor inh-02 的结构类似物，也是一种有效的 RNF5 激动剂。在表达 CFBE41o- 的 F508del-CFTR 细胞中，RNF5 agonist 1 能够增加 ATG4B 的泛素化状态。

RNF5 inhibitor inh-02, a potent E3 ubiquitin ligase RNF5 RMA1 inhibitor, demonstrates significant efficacy in rescuing F508del-CFTR with an EC50 of 2.2 uM in bronchial epithelial cells homozygous for the F508del mutation. This compound is valuable for cystic fibrosis research[1].

Thiocarlide (isoxyl) is a thiourea derivative that was used in the 1960s to successfully treat tuberculosis (TB). It has considerable antimycobacterial activity in vitro and is effective against multi-drug resistant strains of Mycobacterium tuberculosis in the range of 1-10 µg ml. [1] [2] At concentrations of 10 µM, isoxyl inhibits the synthesis of M. bovis during six hours of exposure which is similar to isoniazid (INH) and ethionamide (ETH), two other predominant anti-tuberculosis drugs. Unlike INH and ETH, isoxyl also partially inhibits the synthesis of fatty acids. Isoxyl shows no acute toxicity against primary macrophage cell cultures as demonstrated by diminution of redox activity.[2]

Mtb-IN-5（化合物(-)17j）是一种异恶唑类化合物，对结核分枝杆菌(Mtb)具有活性。它能够抑制宿主巨噬细胞内Mtb的呼吸及生物膜生长，且能够增强异烟肼(INH)对耐INH Mtb突变株的抑制效果。

Mtb-IN-4（化合物17h）是一种异恶唑类化合物，显示出针对结核分枝杆菌（Mtb）的抗活性，其IC50值为0.70 μM。它能阻断巨噬细胞内Mtb的呼吸和生物膜形成，并可以增强抗生素异烟肼（INH）对耐INH Mtb突变体的抑制效果。