substrate-competitive

K145 hydrochloride 是选择性的，底物竞争性的和口服有效的SphK2抑制剂，IC50为 4.3 µM，Ki 为 6.4 µM。它可诱导细胞凋亡，显示出强大的抗肿瘤活性。

SU3327 (halicin) 是具有底物竞争性的 JNK 选择性抑制剂，IC50为 0.7 μM。它还抑制 JNK 和 JIP 之间的蛋白相互作用，IC50值为 239 nM。

CM-272 是一种可逆底物竞争性双重G9a DNA 甲基转移酶选择性抑制剂，具有抗肿瘤活性。它抑制细胞增殖并促进细胞凋亡，诱导干扰素刺激的基因和免疫原性细胞死亡。它抑制G9a、DNMT1、DNMT3A、DNMT3B 和GLP，IC50分别为 8 nM、382 nM、85 nM、1200 nM 和 2 nM。

BMS-593214 是一种选择性活性位点定向因子 VIIa 抑制剂，也是 VIIa 激活底物 FX 的非竞争性抑制剂，具有抗血栓形成和抗出血活性。BMS-593214 可用于研究电诱导颈动脉血栓形成 (AT)和线诱导腔静脉血栓形成 (VT)。

2'-O-Methylcytidine 是 2'-代核苷，可抑制 HCV 复制。 它在体外抑制 NS5B 催化的 RNA 合成，其抑制方式是与底物核苷三磷酸竞争。

SIRT5 inhibitor 7 (compound 58) 是底物竞争性和选择性的 SIRT5 抑制剂，IC 50 = 310 nM，显著减轻了脂多糖（LPS）和盲肠结扎 穿孔（CLP）诱导的脓毒性AKI小鼠的肾功能障碍和病理损伤，调节急性肾损伤（AKI）小鼠肾脏中蛋白琥珀酰化和促炎细胞因子的释放。

MRT199665 is an effective and ATP-competitive, selective MARK SIK AMPK inhibitor (IC50s of 2 2 3 2 nM, 10 10 nM, and 110 12 43 nM for MARK1 MARK2 MARK3 MARK14, AMPKα1 AMPKα2, and SIK1 SIK2 SIK3, respectively). MRT199665 suppresses the phosphorylation of S

UNC0379 是一种选择性的、底物竞争性的赖氨酸甲基转移酶 SETD8 抑制剂，IC50值为 7.3 μM，也选择性抑制其他 15 种甲基转移酶。

GSK3-IN-3 是一种线粒体自噬 (mitophagy) 诱导剂和GSK-3 抑制剂（IC50 ： 3.01 μM），可诱导帕金依赖性线粒体自噬。 GSK3-IN-3 具有非 ATP 和非底物竞争性，对 6-OHDA 有神经保护作用。

6-Phosphogluconic acid 是竞争性的磷酸葡萄糖异构酶抑制剂，对6-磷酸果糖和6-磷酸葡萄糖和的 Ki 分别为 42 μM 和 48 μM。它属于人内源性代谢物。

CBB1007 Hcl is a selective, reversible, and substrate competitive LSD1 inhibitor (IC50: 5.27 μM for hLSD1).

CBB1007 is a potent, reversible, and substrate competitive LSD1 inhibitor (IC50: 5.27 μM for hLSD1).

CBB1007 trihydrochloride is a selective, reversible, and substrate competitive LSD1 inhibitor (IC50: 5.27 μM for hLSD1).

GDP-α-D-mannose disodium gives a competitive inhibition with respect to GTP (Ki 14.7 μM) and an uncompetitive inhibition with respect to mannose-1-P (Ki 115 μM).GDP-α-D-mannose disodium is the donor substrate for mannosyltransferases and the precursor of

K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity. K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM.

PI-273 是一种可逆的特异性磷脂酰肌醇 4-激酶抑制剂，IC50为 0.47 μM。它可抑制乳腺癌细胞的增殖，阻断细胞周期并诱导细胞凋亡。

BAY-707, a highly potent and selective substrate-competitive inhibitor of MTH1 (NUDT1) with an IC50 of 2.3 nM, is well-tolerated in mice and exhibits a favorable pharmacokinetic (PK) profile compared to other MTH1 compounds. However, it demonstrates a clear lack of anticancer efficacy both in vitro and in vivo[1].

Ac-EVKKQR-pNA是一种针对NS2B-NS3切割位点P6-P1段的竞争性对硝基苯胺底物，该底物在P1位置采用了更易反应的可水解偏硝基苯胺。此化合物对于研究登革热2型病毒和黄病毒感染具有重要的应用潜力。

KC01 is an effective and selective inhibitor of ABHD16A. By measuring competitive gel-based ABPP (IC50 values of inhibition of ABHD16A by KC01 and KC02: ~0.2–0.5 μM and >10 μM, respectively). Testing by a PS substrate assay, IC50 values of inhibition of h

ICL-SIRT078 is a highly selective inhibitor of substrate-competitive SIRT2 that acts by displaying a significant neuroprotective effect in a lactacystin-induced model of Parkinsonian neuronal cell death in the N27 cell line.

Chloramphenicol succinate(琥珀酸氯霉素)是一种水溶性的Chloramphenicol前药，是一种抑菌抗生素，与细菌核糖体结合阻止其翻译。CPSA是琥珀酸脱氢酶（SDH）的竞争性底物和抑制剂。在体外，Kemicetine succinate可以被琥珀酸脱氢酶氧化，释放出氯霉素。

Furamidine is a cell-permeable, selective inhibitor of protein arginine methyltransferase 1 (PRMT1). Furamidine binds to strings of AT base pair sequences in DNA′s minor groove. Furamidine targets the enzyme active site and is primarily competitive with t

Tenofovir diphosphate (TFV-DP) is a competitive inhibitor of DNA polymerases, specifically targeting dATP, and it serves as a substrate for the reverse transcriptase (RT) of human immunodeficiency virus type 1 (HIV-1)[1].

12(S)-HEPE is a monohydroxy fatty acid synthesized from EPA by the action of 12-LO. Unstimulated neutrophils metabolize 12(S)-HEPE to 12(S),20-diHEPE, whereas stimulated neutrophils produce 5(S),12(S)-HEPE via the 5-lipoxygenase pathway. The competitive action of 12(S)-HEPE with arachidonic acid as a substrate for 5-LO in the formation of leukotrienes may provide a basis for the anti-inflammatory potential of ω-3 fatty acids.