Ubiquitin activating enzyme

Pathways Recommended:	Metabolic Enzyme/Protease

By Targets:	E1/E2/E3 Enzyme (10) NEDD8-activating Enzyme (2) Androgen Receptor (1) Apoptosis (7) Autophagy (1) Biochemical Assay Reagents (1) Carbonic Anhydrase (2) Ferroptosis (1) Heme Oxygenase (HO) (1) HSP (1) Keap1-Nrf2 (1) MDM-2/p53 (1) Microtubule/Tubulin (1) Mitophagy (1) NF-κB (2) Reactive Oxygen Species (ROS) (1) Reference Standards (1)
By Research Areas:	Cancer (11) Infection (1) Metabolic Disease (2) Neurological Disease (1)

Targets Recommended: E1/E2/E3 Enzyme NEDD8-activating Enzyme Peroxidase Enzyme FLAP ATF6 Platelet-activating Factor Receptor (PAFR) Carnosine-cleaving Enzyme Proteolytic Enzyme Endothelin-Converting Enzyme (ECE) Angiotensin-converting Enzyme (ACE) IRE1 PACAP Receptor IDE TET Protein

Art. -Nr.	Produktname	Target	Forschungsgebiete	Chemical Structure

HY-100487

TAK-243 Maximum Cited Publications 83 Publications Verification MLN7243	E1/E2/E3 Enzyme NF-κB Apoptosis	Cancer
TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC₅₀=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis .

HY-13296

PYR-41 20+ Cited Publications	E1/E2/E3 Enzyme Apoptosis	Cancer
PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC₅₀ of < 10 μM, with little activity at E2 and E3.

HY-128586

TAS4464 5+ Cited Publications	Apoptosis Carbonic Anhydrase NEDD8-activating Enzyme	Cancer
TAS4464 is a long-acting, highly selective covalent inhibitor targeting *NEDD8*-activating enzyme (NAE) (IC₅₀=0.955 nM), and also inhibits CAII with an IC₅₀ of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC₅₀ values of TAS4464 against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 has a wide selcetive window, without obvious toxicity. TAS4464 can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .

HY-13811

NSC697923 5+ Cited Publications	E1/E2/E3 Enzyme Apoptosis	Cancer
NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity .

HY-114304

COH000 2 Publications Verification	E1/E2/E3 Enzyme	Cancer
COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC₅₀ of 0.2 μM for SUMOylation in vitro .

HY-13297

PYZD-4409 2 Publications Verification	E1/E2/E3 Enzyme	Cancer
PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC₅₀ of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells .

HY-128586A

TAS4464 hydrochloride 5+ Cited Publications	NEDD8-activating Enzyme Carbonic Anhydrase Apoptosis	Cancer
TAS4464 hydrochloride is a long-acting, highly selective covalent inhibitor targeting *NEDD8*-activating enzyme (NAE) (IC₅₀=0.955 nM), and also inhibits CAII with an IC₅₀ of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC₅₀ values of TAS4464 hydrochloride against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 hydrochloride targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 hydrochloride exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 hydrochloride has a wide therapeutic window, without obvious toxicity. TAS4464 hydrochloride can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .

HY-149127

Rosolutamide ASC-JM17; ALZ-003	Keap1-Nrf2 Androgen Receptor HSP Mitophagy Ferroptosis Apoptosis Reactive Oxygen Species (ROS) Autophagy	Metabolic Disease
Rosolutamide (ASC-JM17) is an orally active Nrf1/Nrf2 activator. Rosolutamide activates Hsf1 pathways, upregulates proteasome subunits and antioxidant enzymes, induces proteasome complex structural rearrangement, and enhances ubiquitin-proteasome system-mediated degradation. Rosolutamide reduces mutant androgen receptor and ataxin-3 aggregates, restores mitochondrial function, attenuates reactive oxygen species (ROS) levels, induces apoptosis and ferroptosis, and inhibits cancer cell growth. Rosolutamide can be used for the research of spinal and bulbar muscular atrophy, Huntington’s disease, and temozolomide-resistant glioblastoma .

HY-178458

UBA5-IN-2	E1/E2/E3 Enzyme	Metabolic Disease Cancer
UBA5-IN-2 (Compound 50) is a potent ubiquitin-like modifier activating enzyme 5 (UBA5) inhibitor (IC₅₀=0.063 μM). UBA5-IN-2 is promising for research of cancers and protein homeostasis-related diseases .

HY-169796

Panepophenanthrin	E1/E2/E3 Enzyme	Cancer
Panepophenanthrin is a compound that can be isolated from the mushroom strain, Panus rudis Fr. IFO 8994. Panepophenanthrin is a **ubiquitin-activating enzyme** inhibitor .

HY-125660

Leucettamol A	E1/E2/E3 Enzyme MDM-2/p53	Infection
Leucettamol A is an inhibitor of Ubc13 (ubiquitin E2 enzyme)-Uev1A interaction, with an IC₅₀ of 50 μg/mL. Leucettamol A can potentially activate the expression of cancer suppressor p53 and is a precursor of anticancer agents. Leucettamol A can be isolated from a marine sponge, Leucetta aff. Microrhaphis .

HY-163105

Tubulin/NEDDylation-IN-1	Microtubule/Tubulin	Cancer
Tubulin/NEDDylation-IN-1 (compound C11) is a dual inhibitor of tubulin (Microtubule/Tubulin)-NEDDylation (IC₅₀ for tubulin=2.40 μM), which has strong anti-proliferative activity. Neddylation is a protein post-translational modification that covalently tags the ubiquitin-like protein NEDD8 to target proteins. Tubulin/NEDDylation-IN-1 forms hydrogen bonds with residues of tubulin and E1 NEDD8 activating enzyme (NAE) through methoxy and dithiocarbamate groups and inhibits NEDDylation and microtubulin in an ATP-dependent manner. tube polymerization .

HY-W679138

N,N-dimethyldithiocarbamate potassium	E1/E2/E3 Enzyme Heme Oxygenase (HO)	Neurological Disease
N,N-dimethyldithiocarbamate potassium is a ubiquitin-activating enzyme E1 inhibitor. N,N-dimethyldithiocarbamate potassium inhibits the activation of E1 and reduces the level of activated ubiquitinated E1 (ub-E1). N,N-dimethyldithiocarbamate potassium increases intracellular copper levels, enhances oxidative stress, elevates protein carbonyl levels, and upregulates the expression of HO-1 . N,N-dimethyldithiocarbamate potassium is applicable to research related to Parkinson's disease .

HY-E71082

(E3-independent) E2 Ubiquitin-conjugating enzyme	Biochemical Assay Reagents	Others
(E3-independent) E2 ubiquitin-conjugating enzyme (EC 2.3.2.24) transfers a single ubiquitin directly from an ubiquitinated E1 ubiquitin-activating enzyme to itself, and on to a lysine residue of the acceptor protein without involvement of E3 ubiquitin transferases.

HY-100487R

TAK-243 (Standard) MLN7243 (Standard)	E1/E2/E3 Enzyme Reference Standards NF-κB Apoptosis	Cancer
TAK-243 (Standard) is the analytical standard of TAK-243 (HY-100487). This product is intended for research and analytical applications. TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis .

Art. -Nr.	Produktname

HY-L050

Ubiquitination Compound Library	486 compounds
Protein ubiquitination is an enzymatic post-translational modification in which an ubiquitin protein is attached to a substrate protein. Ubiquitination involves three main steps: activation, conjugation, and ligation, performed by ubiquitin-activating enzymes (E1s), ubiquitin-conjugating enzymes (E2s), and ubiquitin ligases (E3s), respectively. Ubiquitination affects cellular processes such as apoptosis, cell cycle, DNA damage repair, and membrane transportation, etc. by regulating the degradation of proteins (via the proteasome and lysosome), altering the cellular localization of proteins, affecting proteins activity, and promoting or preventing protein-protein interactions. Deregulation of ubiquitin pathway leads to many diseases such as neurodegeneration, cancer, infection and immunity, etc. MCE offers a unique collection of 486 small molecule modulators with biological activity used for ubiquitination research. Compounds in this library target the key enzymes in ubiquitin pathway. MCE Ubiquitination Compound Library is a useful tool for the research of ubiquitination regulation and the corresponding diseases.

Ubiquitination Compound Library

486 compounds

Protein ubiquitination is an enzymatic post-translational modification in which an ubiquitin protein is attached to a substrate protein. Ubiquitination involves three main steps: activation, conjugation, and ligation, performed by ubiquitin-activating enzymes (E1s), ubiquitin-conjugating enzymes (E2s), and ubiquitin ligases (E3s), respectively. Ubiquitination affects cellular processes such as apoptosis, cell cycle, DNA damage repair, and membrane transportation, etc. by regulating the degradation of proteins (via the proteasome and lysosome), altering the cellular localization of proteins, affecting proteins activity, and promoting or preventing protein-protein interactions. Deregulation of ubiquitin pathway leads to many diseases such as neurodegeneration, cancer, infection and immunity, etc.

MCE offers a unique collection of 486 small molecule modulators with biological activity used for ubiquitination research. Compounds in this library target the key enzymes in ubiquitin pathway. MCE Ubiquitination Compound Library is a useful tool for the research of ubiquitination regulation and the corresponding diseases.

Art. -Nr.	Produktname	Category	Target	Chemical Structure

HY-169796

Panepophenanthrin	Natürliche Produkte Microorganisms Source Classification	E1/E2/E3 Enzyme
Panepophenanthrin is a compound that can be isolated from the mushroom strain, Panus rudis Fr. IFO 8994. Panepophenanthrin is a **ubiquitin-activating enzyme** inhibitor .

Species:	Human (6)
Tag:	His (5) Tag Free (1) Strep (2) GST (1)
Source:	sf9 insect cells (1) Sf9 insect cells (4) E. coli (1)

Art. -Nr.	Compare	Produktname	Species	Source	Image

HY-P79454

	ISG15 E1/UBE1L Protein, Human (sf9, His, StrepⅡ) Ubiquitin-like modifier-activating enzyme 7; UBA7; Ubiquitin-activating enzyme 7; D8; Ubiquitin-activating enzyme E1 homolog; UBE1L; UBE2	Human	Sf9 insect cells
	The ISG15 E1/UBE1L protein initiates ubiquitination by adenylating the C-terminal glycine of ubiquitin with ATP to form a thioester bond with its cysteine residue. This produces ubiquitin-E1 thioester and free AMP. ISG15 E1/UBE1L Protein, Human (sf9, His, Strep) is the recombinant human-derived ISG15 E1/UBE1L protein, expressed by Sf9 insect cells , with N-8*His, N-Strep labeled tag.

HY-P71395

	UBA5 Protein, Human (His) Ubiquitin-like modifier-activating enzyme 5; ThiFP1; UFM1-activating enzyme; Ubiquitin-activating enzyme E1 domain-containing protein 1; UBE1DC1; UBA5	Human	E. coli
	The UBA5 protein activates UFM1 in ufmylation, linking the C-terminal glycine residue of UFM1 to a cysteine residue in E1. UBA5 Protein, Human (His) is the recombinant human-derived UBA5 protein, expressed by E. coli , with N-6*His labeled tag.

HY-P701353

	UBE1L2/UBA6 Protein, Human (sf9, His, StrepII) UBA6; Ubiquitin-like modifier-activating enzyme 6; Ubiquitin-activating enzyme 6; Monocyte protein 4; MOP-4; Ubiquitin-activating enzyme E1-like protein 2; E1-L2	Human	Sf9 insect cells
	The ubiquitin E1 enzyme initiates ubiquitination by adenylating ubiquitin with ATP and forming a thioester bond with the E1 enzyme. It exhibits specificity for ubiquitin and excludes ubiquitin-like peptides. UBE1L2/UBA6 Protein, Human (sf9, His, Strep) is the recombinant human-derived UBE1L2/UBA6 protein, expressed by sf9 insect cells , with N-Strep, N-8*His labeled tag.

HY-P705503

	UBA1 Protein, Human (sf9) Ubiquitin-like modifier-activating enzyme 1; Protein A1S9; UBA1; A1S9T; UBE1	Human	Sf9 insect cells
	The UBA1 protein initiates ubiquitin conjugation, marking proteins for degradation in the ubiquitin-proteasome system. UBA1 Protein, Human (sf9) is the recombinant human-derived UBA1 protein, expressed by Sf9 insect cells , with no tag.

HY-P704950

	UBA1 Protein, Human (sf9, His) Ubiquitin-like modifier-activating enzyme 1; Protein A1S9; UBA1; A1S9T; UBE1	Human	sf9 insect cells

HY-P74485

	UBA1 Protein, Human (sf9, His-GST) 2 Publications Verification Ubiquitin-like modifier-activating enzyme 1; Protein A1S9; UBA1; A1S9T; UBE1	Human	Sf9 insect cells
	The UBA1 protein initiates ubiquitin conjugation, marking proteins for degradation in the ubiquitin-proteasome system. UBA1 Protein, Human (sf9, His-GST) is the recombinant human-derived UBA1 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.

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Host:	Rabbit (10)
Reactivity:	Human (10) Rat (9) Mouse (9)
Application:	IHC-P (7) ICC/IF (6) IF-Tissue (1) IP (4) IHC-F (1) WB (10) FC (4) ELISA (1)
Isotype:	IgG (10)
Conjugation:	Non-conjugated (10)
Clonality:	Monoclonal (7) Recombinant (6)
Modification:	Unmodified (7)

Art. -Nr.	Compare	Produktname	Application	Reactivity	Image

HY-P811091

	UBA5 Antibody UBE1DC1, UBA5, Ubiquitin-like modifier-activating enzyme 5, Ubiquitin-activating enzyme 5, ThiFP1, UFM1-activating enzyme, Ubiquitin-activating enzyme E1 domain-containing protein 1	WB, IHC-P	Human, Mouse, Rat
	UBA5 Antibody is a Rabbit-derived and non-conjugated IgG Polyclonal antibody, targeting to UBA5.

HY-P85405

	UBE1L Antibody (YA5097) UBA7; UBE1L; UBE2; Ubiquitin-like modifier-activating enzyme 7; Ubiquitin-activating enzyme 7; D8; Ubiquitin-activating enzyme E1 homolog	WB, IHC-P, IHC-F, FC, IF-Tissue	Human, Mouse, Rat
	UBE1L Antibody (YA5097) is a Rabbit-derived and non-conjugated monoclonal antibody, targeting to UBE1L.

HY-P82072

	*E1 Ubiquitin* Activating Enzyme 1/UBA1 Antibody (YA1817)** UBA1; A1S9T; UBE1; Ubiquitin-like modifier-activating enzyme 1; Protein A1S9; Ubiquitin-activating enzyme E1	WB, IHC-P, ICC/IF, FC	Human, Mouse, Rat
	E1 Ubiquitin Activating Enzyme 1/UBA1 Antibody (YA1817) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to E1 Ubiquitin Activating Enzyme 1/UBA1.

HY-P80365

	*E1 Ubiquitin* Activating Enzyme 1/UBA1 Antibody (YA020)**	WB, ICC/IF, IHC-P, FC	Human, Mouse
	E1 Ubiquitin Activating Enzyme 1/UBA1 Antibody (YA020) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to E1 Ubiquitin Activating Enzyme 1/UBA1.

HY-P86509

	ATG7 Antibody (YA6201) Ubiquitin-like modifier-activating enzyme ATG7; ATG12-activating enzyme E1 ATG7; Autophagy-related protein 7; APG7-like; hAGP7; Ubiquitin-activating enzyme E1-like protein;	WB, IHC-P, ICC/IF, IP, ELISA	Human, Mouse, Rat
	ATG7 Antibody (YA6201) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to ATG7.

HY-P82102

	SAE1 Antibody (YA1847) SAE1; AOS1; SUA1; UBLE1A; SUMO-activating enzyme subunit 1; Ubiquitin-like 1-activating enzyme E1A	WB, ICC/IF, IP, FC	Human, Rat
	SAE1 Antibody (YA1847) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to SAE1.

HY-P80559

	ATG7 Antibody (YA598) hAGP7; Ubiquitin-activating enzyme E1-like protein; APG7L	WB	Human, Mouse, Rat
	ATG7 Antibody (YA598) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to ATG7.

HY-P82584

	UBA2 Antibody (YA2329) UBA2; SAE2; UBLE1B; HRIHFB2115; SUMO-activating enzyme subunit 2; Anthracycline-associated resistance ARX; Ubiquitin-like 1-activating enzyme E1B	WB, IHC-P, ICC/IF, IP	Human, Mouse, Rat
	UBA2 Antibody (YA2329) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to UBA2.

HY-P80559A

	ATG7 Antibody (YA598)(PBS only) hAGP7; Ubiquitin-activating enzyme E1-like protein; APG7L	WB	Human, Mouse, Rat
	ATG7 Antibody (YA598) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to ATG7.

HY-P82584A

	UBA2 Antibody (YA2329)(PBS only) UBA2; SAE2; UBLE1B; HRIHFB2115; SUMO-activating enzyme subunit 2; Anthracycline-associated resistance ARX; Ubiquitin-like 1-activating enzyme E1B	WB, IHC-P, ICC/IF, IP	Human, Mouse, Rat
	UBA2 Antibody (YA2329) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to UBA2.

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