sensitization

GQ-16 是 PPARγ 的部分激动剂，Ki 为 160 nM。 GQ-16 可减少脂肪生成作用并促进胰岛素敏化而不会增加体重。

JBSNF-000028 是一种具有口服活性和有效性的烟酰胺 N-甲基转移酶 (NNMT) 抑制剂，对人 NNMT (hNNMT)、猴 NNMT (mkNNMT) 和小鼠 NNMT (mNNMT) 具有抑制作用， IC50 分别为 0.033 μM、0.19 μM 和 0.21 μM。JBSNF-000028 可驱动胰岛素敏化、葡萄糖调节和体重减，可用于研究代谢紊乱。

AMN082 是一种可透过血脑屏障且具有口服活性和选择性的 mGluR7 激动剂，具有抗抑郁作用。AMN082 对创伤性脑损伤大鼠神经元凋亡的神经保护作用，可减弱可卡因和吗啡诱导的小鼠运动致敏和交叉致敏。

Ragaglitazar(NNC-61-0029) 是一种有效的 PPARγ 和 PPARα的双重激活剂，在动物模型中显示出更好的胰岛素增敏和降脂潜力并且可用于研究 2 型糖尿病。

alpha-Hexylcinnamaldehyde是一种衍生自肉桂醛的化合物，具有潜在的抗诱变和化学增敏特性，被广泛用作许多个人护理品的成分，以及食品和制药行业的添加剂。

Methylchloroisothiazolinone Methylisothiazolinone Mixture(Kathon 886MW)是一种异噻唑啉酮类防腐剂，广泛用于化妆品，能够抑制细菌、酵母和真菌的生长，同时可能引起接触性皮肤过敏。Methylisothiazolinone 可以激活人支气管上皮细胞中的基质金属蛋白酶 (MMPs) 来诱导细胞凋亡和炎症反应。

Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride 可能会引起致敏作用。 Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride 促进 HepG2 （IC50= 62μM）和SK-Hep1（IC50= 151μM）细胞凋亡且对蛋白磷酸酶2A具有抑制作用。

3,7-dimethyloct-6-en-3-ol (3,7-Dimethyl-6-octen-3-ol) 是一种 RIFM 香料，目前未检测出皮肤致敏问题。

Olodanrigan (EMA401) 是具有口服活性、高选择性及外周受限的血管紧张素 Ⅱ 类型 2 受体(AT2R)拮抗剂。它的缓解疼痛的机制可能是：抑制增强的 AngII AT2R 诱导的 p38 和 p42 p44 MAPK 激活，进而阻碍 DRG 神经元的过度兴奋性及 DRG 神经元的萌发。它可用于研究神经性疼痛。

TAT-GluA2 3Y acetate 是AMPA 受体内吞作用的抑制剂。在d-安非他明诱导期全身给药Tat-GluA2(3Y)阻断大鼠行为致敏维持，减弱神经化学致敏维持。

EOAI3402143 是一种去泛素化酶抑制剂，以剂量依赖性抑制 Usp9x Usp24和 Usp5，增加肿瘤细胞凋亡。

Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin.Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM.

YHO-13351 是多药物转运蛋白 （ABCG2） 抑制剂，是丙烯腈衍生物，诱导癌症干细胞 起始样侧群体细胞对伊立替康敏感。

AZD8797 (KAND567) 是一种可口服且具有选择性和有效性的人 CX3CR1 变构拮抗剂，对 CX3CR1 和 CXCR2 具有抑制作用，对SARS-CoV-2诱导的神经元损伤有潜在的保护作用，可防止癫痫发作后偏头痛模型大鼠痛觉过敏和小胶质细胞活化的恶化。

Bcl-2-IN-22（compound 1）是一种具有抗癌活性的金(I) NHC配合物。该化合物通过线粒体途径促使细胞发生凋亡(apoptosis)，其IC50值达到了0.014 μM。针对BCL-2家族成员，Bcl-2-IN-22对过度表达BCL-2的多药耐药白血病细胞显示出促进凋亡(apoptosis)及再敏化的效果。

4-(2-Octylamino)diphenylamine 是一种芳香胺抗氧化剂，对V. fischeri的毒性表现为IC50值为0.68 mg mL。在小鼠局部淋巴结试验中，它会引起皮肤致敏和接触性皮炎。此化合物还用于橡胶添加剂。

18-Methoxycoronaridine is a nicotinic α3β4 antagonist. 18-Methoxycoronaridine slows the rate of induction of behavioral sensitization to nicotine. 18-MC inhibits α3β4 nicotinic acetylcholine receptors which are densely expressed in the medial habenula and

ORM-3819 is a potent and selective PDE III inhibitor. ORM-3819 promotes cardiac contractility through Ca(2+) sensitization.

SW203668 is an irreversible inhibitor of stearoyl-CoA desaturase (IC50 = 54 nM). It is selectively cytotoxic to H2122, H460, HCC44, and HCC95 cell lines that express cytochrome P450 (CYP) isoform CYP4F11 over eight other cancer cell lines that lack CYP4F11 in vitro (IC50s = 22-116 and >10,000 nM, respectively) and ectopic expression of CYP4F11 in SW203668-insensitive H1155 cells results in sensitization to SW203668. In vivo, SW203668 reduces tumor growth rate without reducing sebocyte production in the H2122 wild-type and nonobese diabetic severe combined immunodeficiency (NOD-SCID) mouse xenograft models when administered at doses of 20 and 6 mg kg, respectively.

AZD 1152 is an orally bioavailable prodrug of AZD 1152-HQPA, a selective inhibitor of Aurora kinase B (IC50= 0.36 nM).1AZD 1152 is converted to AZD 1152-HQPA in plasma. Inhibition of Aurora B results in disruption of spindle checkpoint functions and chromosome alignment, resulting in inhibition of cytokinesis followed by apoptosis.2,3AZD 1152 inhibits tumor xenograft growthin vivo.4,5 1.Mortlock, A.A., Foote, K.M., Heron, N.M., et al.Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinaseJ. Med. Chem.50(9)2213-2224(2007) 2.Popescu, R., Heiss, E.H., Ferk, F., et al.Ikarugamycin induces DNA damage, intracellular calcium increase, p38 MAP kinase activation and apoptosis in HL-60 human promyelocytic leukemia cellsMutation Research709-71060-66(2011) 3.Moore, A.S., Blagg, J., Linardopoulos, S., et al.Aurora kinase inhibitors: Novel small molecules with promising activity in acute myeloid and Philadelphia-positive leukemiasLeukemia24(4)671-678(2010) 4.Wilkinson, R.W., Odedra, R., Heaton, S.P., et al.AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosisClin. Cancer. Res13(12)3682-3688(2007) 5.Yang, J., Ikezoe, T., Nishioka, C., et al.AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivoBlood110(6)2034-2040(2007)

MI-223 is an inhibitor of Mcl-1-stimulated homologous recombination (HR) DNA repair, which leads to sensitization of cancer cells to hydroxyurea- or olaparib-induced DNA replication stress.

GPI-15427 is a potent PARP-1 inhibitor capable of crossing the blood-brain barrier, which can significantly increased the antitumor activity of the methylating agent TMZ against malignant melanoma, glioblastoma multiforme, or lymphoma growing at the CNS site. GPI-15427 acts as a potent inhibitor of the enzyme, being capable of inhibiting the activity of purified PARP-1 at nanomolar concentrations. GPI-15427 induced significant sensitization to radiotherapy, representing a promising new treatment in the management of HNSCC.

SU-11752 is a potent and selective DNA-PK inhibitor. Inhibition kinetics and a direct assay for ATP binding showed that SU11752 inhibited DNA-PK by competing with ATP. SU11752 inhibited DNA double-strand break repair in cells and gave rise to a five-fold sensitization to ionizing radiation. At concentrations of SU11752 that inhibited DNA repair, cell cycle progression was still normal and ATM kinase activity was not inhibited.

RK33 (RK 33) 是 DDX3（一种 RNA 解旋酶）的一流小分子抑制剂，可导致 G1 细胞周期停滞，诱导细胞凋亡，并促进 DDX3 过表达细胞的辐射增敏。