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Anti-infection

Antibiotic Arenavirus Bacterial CMV Enterovirus Filovirus Fungal HBV HCV HCV Protease HIV HIV Integrase HIV Protease HSV Influenza Virus Orthopoxvirus Parasite TMV Reverse Transcriptase RSV SARS-CoV Virus Protease
Apoptosis

Apoptosis Bcl-2 Family Caspase c-Myc Ferroptosis FKBP IAP Family MDM-2/p53 PKD Necroptosis Pyroptosis RIP kinase Thymidylate Synthase TNF Receptor TRADD
Autophagy

Autophagy FKBP LRRK2 Mitophagy OGA ULK
Cell Cycle/DNA Damage

Antifolate APC ATM/ATR Aurora Kinase BMI-1 Casein Kinase CDK Checkpoint Kinase (Chk) CRISPR/Cas9 Deubiquitinase DNA Alkylator/Crosslinker DNA/RNA Synthesis DNA-PK Early 2 Factor (E2F) Eukaryotic Initiation Factor (eIF) GAK G-quadruplex HDAC HSP IRE1 Kinesin LIM Kinase (LIMK) Microtubule/Tubulin Mps1 DNA Stain Nucleoside Antimetabolite/Analog Nur77 p97 PAK PARP PERK Polo-like Kinase (PLK) PPAR RAD51 Cyclin G-associated Kinase (GAK) Nucleoside Antimetabolite/AnalogOrthopoxvirus ROCK ATF6 Haspin Kinase Sirtuin SRPK Telomerase TOPK Topoisomerase Wee1
Cytoskeletal Signaling

Arp2/3 Complex Dynamin Gap Junction Protein Integrin Kinesin Microtubule/Tubulin Mps1 Myosin PAK ROCK
Endocrinology/Hormones

Adrenergic Receptor Androgen Receptor Angiotensin-converting Enzyme (ACE) Aromatase Cholecystokinin Receptor TSH Receptor Estrogen Receptor/ERR GHSR Glucocorticoid Receptor GNRH Receptor Mineralocorticoid Receptor Opioid Receptor PGD synthase PGE synthase Progesterone Receptor Thyroid Hormone Receptor
Epigenetics

AMPK Aurora Kinase DNA Methyltransferase Epigenetic Reader Domain FTO HDAC Histone Acetyltransferase Histone Demethylase Histone Methyltransferase MicroRNA PARP PKC Protein Arginine Deiminase Methionine Adenosyltransferase (MAT) Sirtuin
GPCR/G Protein

5-HT Receptor Adenosine Receptor Adenylate Cyclase (AC) Adiponectin Receptor Adrenergic Receptor Angiotensin Receptor Bombesin Receptor Bradykinin Receptor Cannabinoid Receptor CaSR CCR CGRP Receptor Cholecystokinin Receptor CRFR CXCR TSH Receptor Neuropeptide Y Receptor Dopamine Receptor EBI2/GPR183 Endothelin Receptor Formyl peptide receptor (FPR) GHSR Glucagon Receptor Glucocorticoid Receptor GNRH Receptor GPCR19 GPR109A GPR119 GPR120 GPR139 GPR27 GPR40 GPR55 GPR84 Guanylate Cyclase Histamine Receptor Imidazoline Receptor Leukotriene Receptor LPL Receptor mAChR Melanocortin Receptor Melatonin Receptor mGluR Neurokinin Receptor Neurotensin Receptor Opioid Receptor Orexin Receptor (OX Receptor) Oxytocin Receptor P2Y Receptor PKG Prostaglandin Receptor Protease-Activated Receptor (PAR) Apelin Receptor (APJ) Ras GPR88 Free Fatty Acid Receptor E3 Ligase Ligand-Linker Conjugates RGS GPR4 Secretin Receptor Mas-related G-protein-coupled Receptor (MRGPR) GPR35 GPR52 MCHR1 (GPR24) Leukotriene Receptor GLP Receptor Somatostatin Receptor Vasopressin Receptor

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E1 Activating

E1泛素激活酶

E1泛素激活酶是泛素化级联反应中的第一个酶 (E1)。在Mg ATP存在下，一个分子泛素 (Ub)被腺苷酸化形成AMP-Ub，通过非共价键与E1结合，而另一分子Ub的C端甘氨酸 (G76)的羧基与E1中的—SH形成硫酯键，从而被激活。泛素激活酶 (Uba或E1)水解 ATP ，在自身的活性位点的半胱氨酸（Cys）的和泛素C末端76号甘氨酸（Gly76）之间形成高能硫酯键，从而激活泛素的-COOH末端，为下一步亲核攻击做准备。

E1 Activating相关产品（4）

货号	产品名	产品描述
SJ-MX0243	TAK-243 (MLN7243)	TAK-243 (MLN7243) 是一种首创的，选择性的泛素激活酶，UAE (UBA1) 抑制剂 (IC50=1 nM)，其阻断了泛素结合，破坏了单泛素信号传导和全蛋白泛素化。TAK-243 (MLN7243) 诱导内质网应激 (ER) 反应，消除 NF-κB 通路活化，促进细胞凋亡。
SJ-MX2421	COH000	COH000 是共价的、不可逆的泛素样激活酶1 (E1) 的变构抑制剂，体外测得对 SUMO 化修饰的 IC50 值为 0.2 μM。
SJ-MX1800	PYR-41	PYR-41 是一种选择性，可透过细胞的泛素活化酶 E1 抑制剂，IC50 值小于10 μM，对E2和E3基本无作用。PYR-41 可诱导凋亡。
SJ-MX3708	ML-792	ML-792 是一种特异性的小泛素样修饰物 (SUMO) 活化酶 (SAE) 抑制剂。ML-792 有效选择性抑制 SAE/SUMO1 和 SAE/SUMO2，IC50 分别为 3 和 11 nM。ML-792 微弱抑制 NAE/NEDD8 和 UAE/ubiquitin，IC50 分别为 32 μM 和 >100 μM。ML-792选择性阻断总SUMO化，从而降低癌细胞增殖。