isozyme

3PO 是一种 PFKFB3 的小分子抑制剂，IC50值为22.9 μM。它抑制几种人类恶性造血和腺癌细胞系的增殖，IC50在1.4到24 μM 之间。它抑制葡萄糖摄取，并降低 Fru-2,6-BP、乳酸、ATP、NAD+ 和 NADH 的细胞内浓度。

Eriocitrin (Eriodictyol-7-O-Rutinoside) 是从柠檬中分离出来的一种黄酮类天然产物，是强效的抗氧化剂。它通过激活线粒体涉及的内在信号传导途径来触发细胞凋亡。它通过上调 p53、cyclin A、cyclin D3 和 CDK6 使 S 期细胞周期停滞，从而抑制肝癌细胞的增殖。

ZIP acetate(863987-12-6 free base) 是一种新型的细胞渗透性蛋白激酶 Mζ (PKMζ) 抑制剂，它是一种参与 LTP 维持的组成型活性非典型 PKC 同工酶。在体外选择性阻断 PKMζ 诱导的海马切片突触增强。逆转晚期 LTP (IC50 = 1 - 2.5 μM) 并在体内中央给药后导致 1 天前的空间记忆持续丧失。

(5Z,2E)-CU-3 是一种具有有效性和选择性的 DGKα 同工酶抑制剂，IC50 值为 0.6 μM，通过对竞争ATP来抑制 DGKα，Km 值为 0.48 mM。(5Z,2E)-CU-3 具有选择性，靶向 DGKα 催化区域，但不作用于调节区域。(5Z,2E)-CU-3 具有抗肿瘤和免疫原性作用，促进癌细胞的凋亡和 T 细胞的活化。

Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is the primary active metabolite of amiodarone, formed by the CYP3A isozyme. Amiodarone is an antiarrhythmic drug that inhibits ATP-sensitive potassium channels with an IC50 of 19.1 μM.

SDZ-MKS 492 is a selective type III isozyme cyclic nucleotide phosphodiesterase inhibitor.

SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner (EC50: 0.3 mM).

CP-640186 是一种有效的乙酰辅酶 A 羧化酶 (ACC)抑制剂，抑制大鼠肝脏 ACC1 和大鼠骨骼肌 ACC2 的 IC50分别为 53 nM 和 61 nM。

NEU3-IN-2（compound 963）是一种基于2-脱氧-2,3-二脱氢-N-乙酰神经氨酰（DANA）的NEU3抑制剂，采用C9联苯氨基甲酸酯为结构框架（Ki: 0.12 μM；IC50: 0.31 μM）。作为人类神经氨酸酶NEU的一种，拥有四种同工酶，NEU3-IN-2主要用于研究NEU3同工酶的功能。此外，其衍生的酰胺和三唑接头类似物对NEU1和NEU4同工酶表现出较好的选择性。

CAⅡ-IN-1 (compound 2i) 是CA Ⅱ同工酶的抑制剂，具有0.44 µM的IC50值，适用于代谢研究。

Ap4dT 是人腺苷酸激酶同工酶 1 (hAK1) 的抑制剂，抑制 ATP 和 ADP 合成的 IC50 分别为 42 μM 和 38 μM。

N-desethyl Brinzolamide is an active metabolite of the carbonic anhydrase (CA) inhibitor brinzolamide .1It inhibits CAII and CAIV activities (IC50s = 1.28 and 128 nM, respectively). 1.Kim, C.-Y., Whittington, D.A., Chang, J.S., et al.Structural aspects of isozyme selectivity in the binding of inhibitors to carbonic anhydrases II and IVJ. Med. Chem.45(4)888-893(2002)

CP-640186 hydrochloride (CP 640186 HCl) 是膜渗透性的乙酰辅酶A 羧化酶（ACC）抑制剂，抑制大鼠肝脏ACC1和大鼠骨骼肌ACC2的IC50为53 nM 和61 nM。

Ruboxistaurin hydrochloride (LY 333531 hydrochloride) 是蛋白激酶 C(PKC) 的同工酶选择性抑制剂，竞争性且可逆地抑制 PKCβI 和 PKCβII，IC50 值分别为 4.7 和 5.9 nM。

Arachidonoyl Thio-PC is a substrate for many phospholipase A2s (PLA2s) including sPLA2, cPLA2, and iPLA2. Cleavage of the sn-2 fatty acid by PLA2 results in generation of a free thiol which reacts with chromogenic reagents such as DTNB (Ellman's reagent) and DTP to allow quantitation of PLA2 activity. Isozyme-specific cPLA2 activity can be measured by excluding or inhibiting sPLA2 and iPLA2 activities in the assay.

Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium current.3 Zonisamide inhibits H. pylori recombinant carbonic anhydrase (CA) and the human CA isoforms I, II, and V with Ki values of 218, 56, 35, and 21 nM, respectively.4,5 In mice, it has anticonvulsant activity against maximal electroshock seizure (MES) and pentylenetetrazole-induced maximal, but not minimal, seizures (ED50s = 19.6, 9.3, and >500 mg kg, respectively). Zonisamide (40 mg kg, p.o.) prevents MPTP-induced decreases in the levels of dopamine , but not homovanillic acid or dihydroxyphenyl acetic acid , and increases MPTP-induced decreases in the dopamine turnover rate in mouse striatum in a model of Parkinson's disease.6 Formulations containing zonisamide have been used in the treatment of partial seizures in adults with epilepsy. |1. Masuda, Y., Ishizaki, M., and Shimizu, M. Zonisamide: Pharmacology and clinical efficacy in epilepsy. CNS Drug Rev. 4(4), 341-360 (1998).|2. Rock, D.M., Macdonald, R.L., and Taylor, C.P. Blockade of sustained repetitive action potentials in cultured spinal cord neurons by zonisamide (AD 810, CI 912), a novel anticonvulsant. Epilepsy Res. 3(2), 138-143 (1989).|3. Suzuki, S., Kawakami, K., Nishimura, S., et al. Zonisamide blocks T-type calcium channel in cultured neurons of rat cerebral cortex. Epilepsy Res. 12(1), 21-27 (1992).|4. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).|5. De Simone, G., Di Fiore, A., Menchise, V., et al. Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: Solution and X-ray crystallographic studies. Bioorg. Med. Chem. Lett. 15(9), 2315-2320 (2005).|6. Yabe, H., Choudhury, M.E., Kubo, M., et al. Zonisamide increases dopamine turnover in the striatum of mice and common marmosets treated with MPTP. J. Pharmacol. Sci. 110(1), 64-68 (2009).

Chrysophanol-1-O-β-gentiobioside, an anthraquinone glycoside obtained from the seeds of Cassia obtusifolia, exhibits targeted inhibition of hMAO-A isozyme activity with an IC50 value of 96.15 μM.

CP-610431 is a reversible, ATP-uncompetitive inhibitor of acetyl-CoA carboxylase (ACC), exhibiting isozyme nonselectivity. It inhibits both ACC1 and ACC2 with IC50 values of approximately 50 nM. CP-610431 offers potential application in metabolic syndrome research.

Sulfaphenazole (Plisulfan) 是一种 CYP2C9的特异性抑制剂，抑制 CYP2C9介导的亚油酸动脉粥样硬化和促炎症效应，增加 AP-1的氧化应激和激活。

URAT1 inhibitor 2 是一种口服具有活力的 URAT1 和 CYP isozyme 抑制剂，对 URAT1 介导的 14C-UA 吸收、CYP1A2、CYP2C9 的 IC50 值分别为 1.36 μM、16.97 μM、5.22 μM。URAT1 inhibitor 2 是一种有前途的、能够用于研究高尿酸血症和痛风的候选药物。

Pep2m, myristoylated TFA (Myr-Pep2m TFA)为具备细胞渗透性的肽。该化合物通过破坏PKMζ与其下游靶点NSF GluR2的相互作用而发挥作用，其中PKMζ为具有自主活性的PKC同工酶。

DL-Glyceraldehyde 3-phosphate diethyl acetal barium 作为一种有效的天冬氨酸转氨酶 (Aspartate Aminotransferase) 同工酶抑制剂。

Novel, cell-permeable inhibitor of protein kinase Mζ (PKMζ), a constitutively active, atypical PKC isozyme involved in LTP maintenance. Selectively blocks PKMζ-induced synaptic potentiation in hippocampal slices in vitro. Reverses late-phase LTP (IC50 = 1