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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T11631	iFSP1	Ferroptosis	Apoptosis
	iFSP1 是一种强效、选择性和谷胱甘肽独立的铁死亡抑制蛋白 1 (FSP1) (AIFM2) 抑制剂，具有EC50 为 103 nM。它能够使多种人类癌细胞系对铁死亡诱导剂敏感，例如 (1S,3R)-RSL3。它在过表达 FSP1 的 GPX4 敲除细胞中选择性地诱导铁死亡。
T2121	SW033291	Dehydrogenase	Metabolism
	SW033291 是有效的15-PGDH 抑制剂，与15-PGDH 亲和力高，Ki 为 0.1 nM。它增加骨髓和其他组织中前列腺素 PGE2 的水平。它还可促进组织再生。
T3722	MK-1064 Urokinase inhibitor 1,MK 1064	OX Receptor	GPCR/G Protein; Neuroscience
	MK-1064 (Urokinase inhibitor 1) 是一种选择性食欲素 2 (2-SORA)受体拮抗剂，可用于失眠患者的研究。
T10087	24-Norursodeoxycholic acid nor-UDCA	Others	Others
	24-Norursodeoxycholic acid (nor-UDCA) 是一种侧链缩短的 UDCA 的 C23 同系物，表现出有效的抗胆汁淤积，抗炎和抗纤维化活性。
T27957	LY-465608 LY 465608
	LY-465608, a PPAR Agonist, inhibits macrophage activation and atherosclerosis in apolipoprotein E knockout mice.
T37023	MB 0223
	Dynamin-related GTPase DRP1 partial inhibitor (IC50 = 1.2 μM). Selective for DRP1 over other dynamin-related GTPases, OPA1 and DYN1. Increases mitochondrial DNA levels in mfn1- knockout MEFs deficient in mitochondrial fusion. Mallat et al (2018) Discovery and characterization of selective small molecule inhibitors of the mammalian mitochondrial division dynamin, DRP1. Biochem.Biophys.Res.Commun. 499 556 PMID:29601815
T70340	JHU-58
	JHU-58 is a novel dipeptide MrgC agonist. JHU-58 inhibited both mechanical and heat hypersensitivity in rats after an L5 spinal nerve ligation (SNL). JHU58 attenuated the evoked excitatory postsynaptic currents in substantia gelatinosa (SG) neurons in wild-type mice, but not in Mrg knockout mice, after peripheral nerve injury.
T78898	Lysyl hydroxylase 2-IN-2	Monoamine Oxidase	Neuroscience
	Lysyl hydroxylase 2-IN-2（compound 13）为一高效Lysyl hydroxylase 2 (LH2)抑制剂，其IC50约为500 nM。该化合物能够抑制344SQ野生型细胞迁移，而对于LH2敲除的344SQ细胞迁移则无影响。
T71845	Lockdown
	Lockdown is a reversible and non-competitive PPM1F inhibitor. Lockdown is selective for PPM1F, because this compound does not inhibit other protein phosphatases in vitro and does not induce additional phenotypes in PPM1F knockout cells. Lockdown acts in a dose-dependent, allosteric manner with high selectivity for PPM1F
T36260	NR 7h
	Potent and selective p38α and p38β degrader (DC50 < 50 nM). Displays no significant degradation of p38γ, p38δ, JNK1/2 or ERK1/2. Inhibits phosphorylation of MK2 in UV-treated cancer cells and LPS-stimulated bone marrow-derived macrophages (BMDM). Exhibits similar effect to p38α gene knockout in BBL358 cells. Active in vivo.
T38172	RO 5263397 hydrochloride
	Potent trace amine 1 (TA1) receptor agonist (EC50 values are 0.12, 35 and 17-85 nM for mouse, rat and human receptors, respectively). Increases wakefulness and reduces REM and NREM sleep duration in wild type mice. Inhibits spontaneous locomotor activity in dopamine transport (DAT) knockout mice. Espinoza et al (2018) Biochemical and functional characterization of the trace amine-associated receptor 1 (TAAR1) agonist RO5263397. Front.Pharmacol. 9 645 PMID:29977204 \|Galley et al (2015) Discovery ...
T37112	YNT-185 dihydrochloride
	Potent and selective orexin OX2 receptor agonist (EC50 = 28 nM at human OX2 expressed in CHO cells). Displays approximately 100-fold selectivity for OX2 over OX1 (EC50 = 2.75 μM at human OX1 expressed in CHO cells). Depolarizes OX2-expressing histaminergic neurons in mouse brain slices. Increases wake time in wild type mice. Suppresses cataplexy-like symptoms in OX knockout mice. Nagahara et al (2015) Design and synthesis of non-peptide, selective orexin receptor 2 agonists. J.Med.Chem. 58 7931 ...
T37845	Taurocholic Acid 3-sulfate (sodium salt)
	Taurocholic acid 3-sulfate (TCA3S) is a metabolite of the conjugated bile acid taurocholic acid .1Plasma levels of TCA3S are elevated in wild-type andSortilin 1(Sort1) knockout mice at 6 hours following bile duct ligation (BDL) and are further elevated inSort1knockout mice at 24 hours post-BDL.2 1.Lefebvre, P., Cariou, B., Lien, F., et al.Role of bile acids and bile acid receptors in metabolic regulationPhysiol. Rev.89(1)147-191(2009) 2.Li, J., Woolbright, B.L., Zhao, W., et al.Sortilin 1 loss-o...
T80248	PKCε (85-92)	PKC	Chromatin/Epigenetic; Cytoskeletal Signaling
	PKCε(85-92) 是一种具有生物活性的肽，其作为 e-PKC 特异性激活剂，能够促进野生型细胞中的 MARCKS 磷酸化作用，对基因敲除小鼠来源的细胞中的 MARCKS 磷酸化则无影响。
T38160	STING Agonist 1a
	STING agonist 1a is an agonist of stimulator of interferon genes (STING).1It induces expression of an IRF-inducible SEAP reporter gene in a cell-based assay (EC50= 16.77 μM). STING agonist 1a (12.5-100 μM) induces expression of IFN-β, IL-6, and chemokine (C-X-C motif) ligand 10 (CXCL10) in THP-1 cells, an effect that can be reversed by STING knockout or the STING inhibitor H-151 . 1.Hou, H., Yang, R., Liu, X., et al.Discovery of triazoloquinoxaline as novel STING agonists via structure-based vir...
T78241	Asfotase alfa ENB-0040
	Asfotase alfa (ENB-0040) 是一款针对骨骼的基因重组糖蛋白。该药物提升了Akp2−/−基因敲除小鼠的存活率、骨矿化及骨骼生长，并且缓解了脚部、胸部、下肢及颌骨矿化缺损。它主要用于对围产期、婴幼儿及青少年型低磷酸酶血症(HPP)进行研究。
T82719	Cisd2 agonist 2
	Cisd2 agonist 2（compound 6）是Cisd2激活剂，具有191 nM的EC50值，其中Cisd2水平与NAFLD相关。在Cisd2hKO-het小鼠（杂合子肝细胞特异性Cisd2敲除）中，Cisd2 agonist 2未显示出显著的体内毒性。
T37487	1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-PE
	1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-PE is a phospholipid that contains stearic acid at the sn-1 position and 15(S)-HpETE at the sn-2 position. It is produced via oxidation of 1-stearoyl-2-arachidonoyl-sn-glycero-3-PE by 15-lipoxygenase (15-LO). 1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-PE (0.6 and 0.9 μM) increases ferroptotic cell death in wild-type and Acsl4 knockout Pfa1 mouse embryonic fibroblasts (MEFs) treated with the GPX4 inhibitor RSL3.
T74743	M47
	M47 是一种小分子，可选择性地破坏隐花色素 1 (CRY1) 的稳定性并增加细胞核中 CRY1 的降解。M47 增强Ras 转化的 P53 缺陷小鼠皮肤成纤维细胞系的细胞凋亡，并延长 p53 基因敲除小鼠的寿命。M47 可用于癌症研究。
T36380	GLP-1 (1-36) amide (human, rat) (trifluoroacetate salt)
	GLP-1 amide is a peptide hormone cleaved from proglucagon in the pancreas.1,2 Mice lacking the glucagon receptor (Gcgr-/-) have approximately nine-fold higher levels of total GLP-1 amide, including GLP-1 (1-36) amide and truncated GLP-1 (7-36) amide , in pancreatic tissue compared to wild-type mice.2References1. Schjoldager, B.T., Mortensen, P.E., Christiansen, J., et al. GLP-1 (glucagon-like peptide 1) and truncated GLP-1, fragments of human proglucagon, inhibit gastric acid secretion in humans...
T36461	CAY10748 CAY10748
	CAY10748 is an agonist of stimulator of interferon genes (STING; IC50= 0.3794 μM in a competition binding assay).1It activates STING in STING-expressing, but not STING knockout, THP-1 cells (EC50s = 0.287 and >100 μM, respectively, in a reporter assay). It induces phosphorylation of STING at the serine in position 366, as well as phosphorylation of TBK1 and IFN regulatory factor 3 (IRF3), indicating activation of the STING-TBK1-IRF3 signaling pathway. CAY10748 increases the secretion of IFN-β an...
T37980	N-methyl Leukotriene C4 N-methyl Leukotriene C4
	Produced by neutrophils, macrophages, mast cells, and by transcellular metabolism in platelets, leukotriene C4 (LTC4) is the parent cysteinyl leukotriene formed by the LTC4 synthase-catalyzed conjugation of glutathione to LTA4. It is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) and exhibits potent smooth muscle contracting activity. LTC4, however, is rapidly metabolized to LTD4 and LTE4, which makes the characterization of LTC4 pharmacology difficult. N-methyl Leukot...
T83676	Tianeptine Metabolite MC5 sodium
	Tianeptine metabolite MC5是一种来自非典型抗抑郁化合物tianeptine的活性代谢物，通过β-氧化形成。此代谢物在使用表达人类μ-阿片受体（MOR）而非人类δ-阿片受体（DOR；EC50s = 0.454和 >100 µM, 分别）的HEK293T细胞进行的生物发光共振能量转移(BRET)试验中，特异性诱导G蛋白激活。在野生型小鼠上，30 mg/kg剂量的Tianeptine metabolite MC5可减少强迫游泳测试中的静止时间，但在MOR敲除小鼠中则不会，表明其具有MOR依赖的抗抑郁样活性。
T83825	Trofinetide acetate NNZ-2566
	Trofinetide是一种衍生自具有神经保护作用的三肽Gly-Pro-Glu的化合物，后者是胰岛素样生长因子-1（IGF-1）的N-端序列。在10 nM的浓度下使用时，它能减少由蛋白磷酸酶抑制剂奥卡达酸在原代大鼠胚胎纹状体神经元中引起的细胞死亡。Trofinetide在一种由穿透性弹道样脑损伤引起的大鼠神经炎症模型中减少了编码IL-1β、TNF-α、IL-6和E-selectin的mRNA的脑表达。在通过中脑动脉闭塞（MCAO）引起的大鼠脑损伤模型中，以30和60 mg/kg的剂量给药时，它减少了皮层和纹状体梗塞区域。Trofinetide（每天100 mg/kg）减少了树突棘的数量，并逆转了在fmr1-/-敲除小鼠脆性X综合征模型中的社交识别和情景恐惧条件反射的缺陷，同时也减少了睾丸重量的增加。含有Trofinetide的制剂已被用于治疗Rett综合征。
T36722	Deltorphin II (trifluoroacetate salt)
	Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid...

化合物

Cat.No: T11631

Target: Ferroptosis

Cat.No: T2121

Target: Dehydrogenase

Cat.No: T3722

Synonym: Urokinase inhibitor 1,MK 1064

Target: OX Receptor

24-Norursodeoxycholic acid

Cat.No: T10087

Synonym: nor-UDCA

Target: Others

Cat.No: T27957

Synonym: LY 465608

Cat.No: T37023

Cat.No: T70340

Lysyl hydroxylase 2-IN-2

Cat.No: T78898

Target: Monoamine Oxidase

Cat.No: T71845

Cat.No: T36260

RO 5263397 hydrochloride

Cat.No: T38172

YNT-185 dihydrochloride

Cat.No: T37112

Taurocholic Acid 3-sulfate (sodium salt)

Cat.No: T37845

Cat.No: T80248

Target: PKC

STING Agonist 1a

Cat.No: T38160

Cat.No: T78241

Synonym: ENB-0040

Cisd2 agonist 2

Cat.No: T82719

1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-PE

Cat.No: T37487

Cat.No: T74743

GLP-1 (1-36) amide (human, rat) (trifluoroacetate salt)

Cat.No: T36380

Cat.No: T36461

Synonym: CAY10748

N-methyl Leukotriene C4

Cat.No: T37980

Synonym: N-methyl Leukotriene C4

Tianeptine Metabolite MC5 sodium

Cat.No: T83676

Trofinetide acetate

Cat.No: T83825

Synonym: NNZ-2566

Deltorphin II (trifluoroacetate salt)

Cat.No: T36722

Cat. No.	Product Name	Target	Signaling Pathways
T83913	Mitraciliatine
	Mitraciliatine是一种在M. speciosa（泰国称为Kratom）中发现的生物碱，是μ-阿片受体（MOR）部分激动剂和κ-阿片受体（KOR）激动剂。该化合物对MOR和KOR具有选择性，与δ-阿片受体（DOR; EC50s分别为228, 218, 和 >1,000 nM，针对小鼠受体在GTPγS结合实验中的表现）。Mitraciliatine（100 nmol/动物，脑室内注射）在小鼠的热水尾部缩回实验中延长了撤回潜伏期，这一效果可以通过敲除MOR而非KOR来逆转。与吗啡不同，Mitraciliatine不会诱发过度活动或呼吸抑制。

天然产物

Cat.No: T83913

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