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Search Results for " substrate-competitive "

Targets Recommended: JNK

44

抑制剂 & 化合物

1

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Cat. No.	Product Name	Target	Signaling Pathways
T13018	SU3327 halicin	JNK	MAPK
	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。
T7194	CM-272	Apoptosis; DNA Methyltransferase; Histone Methyltransferase	Apoptosis; Chromatin/Epigenetic
	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。
TQ0138	K145 hydrochloride K145盐酸盐	Apoptosis; S1P Receptor	Apoptosis; GPCR/G Protein
	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。
T5322	BCI-121	Histone Methyltransferase	Chromatin/Epigenetic
	BCI-121是一种底物竞争性 SMYD3 抑制剂，可抑制癌细胞的增殖。
T1841	UNC0379	Histone Methyltransferase	Chromatin/Epigenetic
	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。
T21507	7-Ethoxyresorufin Resorufin ethyl ether,乙氧基试卤灵	P450; NO Synthase	Immunology/Inflammation; Metabolism
	7-Ethoxyresorufin (Resorufin ethyl ether) 是细胞色素 P450 (尤其是CYP1A1) 的荧光底物和竞争性抑制剂，同时对 NO 合酶具有抑制作用。
T12454	PI-273	Apoptosis; PI4K	Apoptosis; PI3K/Akt/mTOR signaling
	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。
T9329	BRD0639	Histone Methyltransferase	Chromatin/Epigenetic
	BRD0639 是首创的PRMT5-substrate adaptor interaction 的抑制剂。BRD0639 是一种 PRMT5 结合基序 (PBM) 竞争性抑制剂，可以支持 PBM 依赖的 PRMT5 活性的研究。
T73331	GSK3-IN-3	Mitophagy; GSK-3	Autophagy; PI3K/Akt/mTOR signaling; Stem Cells
	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。
T71641	BMS-593214	Others	Others
	BMS-593214 是一种活性位点定向因子 (F)VIIa 抑制剂。BMS-593214 具有抗血栓和抗出血特性。BMS-593214 是人 FVIIa 的直接竞争性抑制，也是 VIIa 激活底物 FX 的非竞争性抑制剂。BMS-593214 预防电诱导颈动脉血栓形成 (AT)、线诱导腔静脉血栓形成 (VT)。
T38237	2′-O-Methylcytidine	Nucleoside Antimetabolite/Analog; HCV Protease	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Proteases/Proteasome
	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。
T67897	GRP78-IN-3	HSP	Cytoskeletal Signaling; Metabolism
	GRP78-IN-3(化合物8)是一种有效的Hsp70底物结合的小分子竞争性抑制剂，是一种选择性的Grp78 (HSPA5)抑制剂，IC50为0.59 μM。GRP78-IN-3对HspA5的选择性是HspA9的7倍(IC50为4.3 μM)，对HspA5的选择性是HspA2的20倍(IC50为13.9 μM)。
T8561	Apcin	APC	Cell Cycle/Checkpoint
	Apcin 是后期促进复合物/环体 (APC/C(Cdc20)) E3 连接酶活性的有效竞争性抑制剂，可通过与 Cdc20 结合并阻止底物识别竞争性地抑制 APC/C 依赖性泛素化。它占据 WD40 结构域侧面的 D-box 结合口袋，并可以延长有丝分裂。它通过阻断有丝分裂退出并通过共同添加 Ts-Arg-OMe 协同放大而起作用。
T4019	Cambinol SIRT1/2 Inhibitor IV,NSC 112546	Apoptosis; Phospholipase; Sirtuin	Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Metabolism
	Cambinol (SIRT1/2 Inhibitor IV) 是一种SIRT1和SIRT2的抑制剂，IC50值分别为 56 μM 和 59 μM。它是中性鞘磷脂酶的外泌体抑制剂。
T10699L	CBB1007	Others	Others
	CBB1007 is a potent, reversible, and substrate competitive LSD1 inhibitor (IC50: 5.27 μM for hLSD1).
T10699	CBB1007 hydrochloride (1379573-92-8 free base) CBB1007 hydrochloride	Others	Others
	CBB1007 Hcl is a selective, reversible, and substrate competitive LSD1 inhibitor (IC50: 5.27 μM for hLSD1).
T24158	ICL-SIRT078 ICLSIRT078,ICL SIRT 078,ICL SIRT078,ICL-SIRT-078	Others	Others
	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.
T10699L2	CBB1007 trihydrochloride (1379573-92-8 free base) CBB1007 trihydrochloride	Others	Others
	CBB1007 trihydrochloride is a selective, reversible, and substrate competitive LSD1 inhibitor (IC50: 5.27 μM for hLSD1).
T11992	Mefuparib hydrochloride MPH	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo. Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively.
T37910	Tenofovir diphosphate triethylamine	Others	Others
	Tenofovir diphosphate triethylamine (TFV-DP triethylamine) is a competitive inhibitor of DNA polymerases for dATP, functioning as a substrate for HIV type 1 reverse transcriptase (HIV-1 RT)[1].
T69738	GSK-2807 free base	Others	Others
	GSK2807 is a potent and selective, SAM-competitive inhibitor of SMYD3 (Ki = 14 nM). GSK2807 bridges the gap between the SAM-binding pocket and the substrate lysine tunnel of SMYD3. GSK2807 may be useful for cancer treatment.
T37909	Tenofovir diphosphate	Others	Others
	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].
T11739	K145	Others	Others
	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.
T38819	Nω-allyl-L-arginine	Others	Others
	Nω-allyl-L-arginine is a competitive and reversible inhibitor of bovine brain nitric oxide synthase (nNOS), efficiently inactivating nNOS in a time-dependent manner. Additionally, Nω-allyl-L-arginine acts as a substrate, generating L-arginine, acrolein, and H2O.
T14509	BAY-707	Others	Others
	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].
T72637	SIRT5 inhibitor 5	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	SIRT5 inhibitor5，作为一种高效SIRT5抑制剂，其IC50为0.21 µM，特点是不占据NAD+结合口袋，而是作为一种竞争性底物抑制剂。
T69776	BAY-707 acetate	Others	Others
	BAY-707 is a substrate-competitive, highly potent and selective inhibitor of MTH1. Despite superior cellular target engagement and pharmacokinetic properties, inhibition of MTH1 with BAY-707 resulted in a clear lack of in vitro or in vivo anticancer efficacy either in mono- or in combination therapies.
TP1903	PKG inhibitor peptide cGMP Dependent Kinase Inhibitor Peptide
	Competitive inhibitor of cGMP-dependent protein kinase (PKG); analog of a substrate peptide corresponding to a phosphorylation site of histone H2B. Competes with synthetic substrates (Ki = 86 mM) but does not inhibit phosphorylation of intact histones by
T63705	UNC0379 TFA	Others	Others
	UNC0379 TFA 是选择性的、底物竞争性的赖氨酸甲基转移酶 SETD8(KMT5A) 抑制剂 (IC50: 7.3 μM)，对其他 15 种甲基转移酶表现出良好的选择性。
T27395	Furamidine dihydrochloride DB 75, DB75, NSC 305831, WR199385,Furamidine HCl	Others	Others
	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
T22888	KC01	Others	Others
	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
T11382	GDP-α-D-mannose disodium	Others	Others
	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
T68192	OK-1035	Others	Others
	OK-1035 is a potent and selective DNA-PK inhibitor. When a synthetic peptide was used as a substrate, OK-1035 caused 50% inhibition of DNA-PK activity at 8 microM. OK-1035 inhibited the phosphorylation by DNA-PK of consensus peptide as well as that of recombinant human wild type-p53. Kinetic studies indicated that OK-1035 inhibited DNA-PK activity in an ATP-competitive manner.
T78802	SIRT5 inhibitor 6	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	SIRT5 Inhibitor6为一种SIRT5选择性抑制剂，表现出底物竞争性，其IC50值为3.0 μM，展现了在脓毒性AKI疗法研究中的应用潜力。
T80113	Bz-Ala-Arg	Endogenous Metabolite	Metabolism
	Bz-Ala-Arg为特定的二肽，既是人胰腺羧肽酶B又是血浆羧肽酶N的分光光度底物（0.4 M 吡啶甲酸，pH 4.25）。此外，Bz-Ala-Arg亦可用于筛选上述两种酶的竞争性抑制剂。
T69297	Leupeptin HCl	Others	Others
	Leupeptin is a naturally occurring protease inhibitor that can inhibit cysteine, serine and threonine peptidases. Leupeptin is an organic compound produced by actinomycetes. Leupeptin inhibits serine proteinases (trypsin (Ki=3.5 nM), plasmin (Ki= 3.4 nM), porcine kallikrein), and cysteine proteinases (papain, cathepsin B (Ki = 4.1 nM), endoproteinase Lys-C). It does not inhibit α-chymotrypsin or thrombin. Leupeptin is a competitive transition state inhibitor and its inhibition may be relieved by...
T16142	MRT199665	Others	Others
	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
T37967	12(S)-HEPE	Others	Others
	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.
T75810	AKTide-2T TFA
	AKTide-2T TFA 是一个优良的体外AKT 底物，可竞争性抑制组蛋白 H2B 磷酸化，其Ki 值为 12 nM。AKTide-2T TFA 模拟Akt 的磷酸化序列，是一种抑制肽，是 S22 位置中缺失了野生型 AKTide。
T78224	Histatin-3
	Histatin-3是一肽类物质，由32个氨基酸残基构成，表现出显著的抗菌活性。作为前蛋白转化酶1(PC1)的底物，Histatin-3在Arg25位点的羧基端被该蛋白酶特异性切割（HRGYR降低SN）。此外，Histatin-3亦作为中等效力的、可逆的以及具竞争性的抑制剂，能够抑制弗林蛋白酶介导的五肽pGlu-Arg-Thr-Lys-Arg-MCA荧光底物的裂解，其抑制常数Ki大约为1.98μM。
T78803	SIRT5 inhibitor 7	Sirtuin	Chromatin/Epigenetic; DNA Damage/DNA Repair
	SIRT5 inhibitor7 (compound 58) 是一种底物竞争性且选择性的SIRT5抑制剂，展现出抗炎活性。它在调节蛋白质琥珀酰化和抑制促炎细胞因子释放方面具有潜在的肾功能保护效果。此外，在LPS和CLP诱导的脓毒症相关急性肾损伤小鼠模型中，SIRT5 inhibitor7已证实具备体内有效性。
T72388	CBB1007 hydrochloride	Others	Others
	CBB1007 hydrochloride，一种可逆的、选择性的高效组蛋白去甲基化酶LSD1的底物竞争性抑制剂，其对hLSD1的IC50值为5.27 uM。
T72244	CBB1007 trihydrochloride	Others	Others
	CBB1007三盐酸盐是 LSD1选择性抑制剂，IC50值为5.27uM。
T37522	Teneligliptin	Others	Others
	Teneligliptin (MP-513) is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM. Teneligliptin (MP-513) inhibits all these DPP-4 enzymes in a concentration-dependent manner. The IC50s of Teneligliptin (MP-513) for rhDPP-4, human plasma, and rat plasma are 0.889, 1.75, and 1.35 nM, respectively. A study of enzyme inhibition kinetics is conducted for Teneligliptin (M...

化合物

Cat.No: T13018

Synonym: halicin

Target: JNK

Cat.No: T7194

Target: Apoptosis, DNA Methyltransferase, Histone Methyltransferase

K145 hydrochloride

Cat.No: TQ0138

Synonym: K145盐酸盐

Target: Apoptosis, S1P Receptor

Cat.No: T5322

Target: Histone Methyltransferase

Cat.No: T1841

Target: Histone Methyltransferase

7-Ethoxyresorufin

Cat.No: T21507

Synonym: Resorufin ethyl ether,乙氧基试卤灵

Target: P450, NO Synthase

Cat.No: T12454

Target: Apoptosis, PI4K

Cat.No: T9329

Target: Histone Methyltransferase

Cat.No: T73331

Target: Mitophagy, GSK-3

Cat.No: T71641

Target: Others

2′-O-Methylcytidine

Cat.No: T38237

Target: Nucleoside Antimetabolite/Analog, HCV Protease

Cat.No: T67897

Target: HSP

Cat.No: T8561

Target: APC

Cat.No: T4019

Synonym: SIRT1/2 Inhibitor IV,NSC 112546

Target: Apoptosis, Phospholipase, Sirtuin

Cat.No: T10699L

Target: Others

CBB1007 hydrochloride (1379573-92-8 free base)

Cat.No: T10699

Synonym: CBB1007 hydrochloride

Target: Others

Cat.No: T24158

Synonym: ICLSIRT078,ICL SIRT 078,ICL SIRT078,ICL-SIRT-078

Target: Others

CBB1007 trihydrochloride (1379573-92-8 free base)

Cat.No: T10699L2

Synonym: CBB1007 trihydrochloride

Target: Others

Mefuparib hydrochloride

Cat.No: T11992

Synonym: MPH

Target: PARP

Tenofovir diphosphate triethylamine

Cat.No: T37910

Target: Others

GSK-2807 free base

Cat.No: T69738

Target: Others

Tenofovir diphosphate

Cat.No: T37909

Target: Others

Cat.No: T11739

Target: Others

Nω-allyl-L-arginine

Cat.No: T38819

Target: Others

Cat.No: T14509

Target: Others

SIRT5 inhibitor 5

Cat.No: T72637

Target: Sirtuin

BAY-707 acetate

Cat.No: T69776

Target: Others

PKG inhibitor peptide

Cat.No: TP1903

Synonym: cGMP Dependent Kinase Inhibitor Peptide

Cat.No: T63705

Target: Others

Furamidine dihydrochloride

Cat.No: T27395

Synonym: DB 75, DB75, NSC 305831, WR199385,Furamidine HCl

Target: Others

Cat.No: T22888

Target: Others

GDP-α-D-mannose disodium

Cat.No: T11382

Target: Others

Cat.No: T68192

Target: Others

SIRT5 inhibitor 6

Cat.No: T78802

Target: Sirtuin

Cat.No: T80113

Target: Endogenous Metabolite

Cat.No: T69297

Target: Others

Cat.No: T16142

Target: Others

Cat.No: T37967

Target: Others

Cat.No: T75810

Cat.No: T78224

SIRT5 inhibitor 7

Cat.No: T78803

Target: Sirtuin

CBB1007 hydrochloride

Cat.No: T72388

Target: Others

CBB1007 trihydrochloride

Cat.No: T72244

Target: Others

Cat.No: T37522

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T10185	6-Phosphogluconic acid	Others; Endogenous Metabolite	Metabolism; Others
	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。

天然产物

6-Phosphogluconic acid

Cat.No: T10185

Target: Others, Endogenous Metabolite

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