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non-catalytic

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) Aurora Kinase (2) Bcl-2 Family (1) COX (1) Deubiquitinase (2) Endogenous Metabolite (2) FAK (1) Histone Methyltransferase (1) HIV (1) HIV Integrase (1) LRRK2 (1) Mitosis (1) Phosphatase (1) PIN1 (1) Polo-like Kinase (PLK) (1) PROTACs (4) Reference Standards (1) STAT (1)
By Research Areas:	Cancer (6) Infection (1) Inflammation/Immunology (6) Metabolic Disease (1) Neurological Disease (3)

Inhibitors & Agonists

Screening Libraries

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Antibodies

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-148030

XL01126	PROTACs LRRK2	Neurological Disease
XL01126 is a potent LRRK2 PROTAC (DC₅₀: 14 nM (G2019S LRRK2) and 32 nM (WT LRRK2)) composed of the VHL ligand VH 101, thiol (HY-47851, blue part) and the LRRK2 inhibitor HG-10-102-01 (HY-13488, red part). XL01126 crosses the blood-brain barrier and is used as a degradation probe in Parkinson's disease research. XL01126 can be used to study the non-catalytic and framework functions of LRRK2 .

HY-113357

m-Coumaric acid	Endogenous Metabolite	Neurological Disease Metabolic Disease Inflammation/Immunology
m-Coumaric acid is a polyphenol metabolite from caffeic acid, formed by the gut microflora and the amount in human biofluids is diet-dependant. m-Coumaric acid is a BBB-penetrant metabolite of chlorogenic acid. m-Coumaric acid stimulates the cerebral nerves in vitro. m-Coumaric acid can evoke neurite outgrowth in hippocampal neuronal cells. m-Coumaric acid can promote neuronal differentiation. m-Coumaric acid increases spontaneous locomotor activity in mice by acting on the central nervous system. m-Coumaric acid inhibits the oxidation of L-dopa by epidermis tyrosinase. m-Coumaric acid attenuates non-catalytic protein glycosylation in retinas of diabetic rats .

HY-143345

EN523	Deubiquitinase	Cancer
EN523 is a OTUB1 recruiter. EN523 targets a non-catalytic allosteric cysteine C23 in the K48-ubiquitin-specific deubiquitinase OTUB1 .

HY-141512

JB170 3 Publications Verification	PROTACs Aurora Kinase	Cancer
JB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC₅₀=28 nM) by linking Alisertib, to the Cereblon-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC₅₀=193 nM) over AURORA-B (EC₅₀=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase .

HY-18595

BI 224436 5+ Cited Publications	HIV HIV Integrase	Infection
BI 224436 is a novel HIV-1 noncatalytic site integrase inhibitor with EC₅₀ values of less than 15 nM against different HIV-1 laboratory strains.

HY-113357R

m-Coumaric acid (Standard)	Reference Standards Endogenous Metabolite	Neurological Disease Inflammation/Immunology
m-Coumaric acid (Standard) is the analytical standard of m-Coumaric acid. This product is intended for research and analytical applications. m-Coumaric acid is a polyphenol metabolite from caffeic acid, formed by the gut microflora and the amount in human biofluids is diet-dependant. m-Coumaric acid is a BBB-penetrant metabolite of chlorogenic acid. m-Coumaric acid stimulates the cerebral nerves in vitro. m-Coumaric acid can evoke neurite outgrowth in hippocampal neuronal cells. m-Coumaric acid can promote neuronal differentiation. m-Coumaric acid increases spontaneous locomotor activity in mice by acting on the central nervous system. m-Coumaric acid inhibits the oxidation of L-dopa by epidermis tyrosinase. m-Coumaric acid attenuates non-catalytic protein glycosylation in retinas of diabetic rats .

HY-158038

AurkA allosteric-IN-1	Aurora Kinase Mitosis	Cancer
AurkA allosteric-IN-1 (compound 6h) is an Aurora A (AurkA) inhibitor (IC₅₀: 6.50 μM) that inhibits the catalytic activity and non-catalytic functions of Aurora A. Aurora A regulates the assembly of the bipolar mitotic spindle and the fidelity of chromosome segregation during mitosis and has non-catalytic functions. AurkA allosteric-IN-1 blocks the interaction of AurkA with the activator TPX2 by binding to the Y pocket of AurkA .

HY-160550

DPM-1003	Phosphatase	Inflammation/Immunology
DPM-1003 is a PTP1B conformational inhibitor that targets the non-catalytic, disordered segment at the C-terminus of the PTP1B protein, showing improvement in lung inflammation in mice .

HY-175459

PROTAC FAK degrader 3	PROTACs FAK	Inflammation/Immunology Cancer
PROTAC FAK degrader 3 is a selective FAK PROTAC degrader (DC₅₀ = 1.08 nM). PROTAC FAK degrader 3 induces FAK degradation dependent on the ubiquitin-proteasome system and its binding to FAK and CRBN. PROTAC FAK degrader 3 upregulates MHC-I gene transcription and tumor cell surface expression by inhibiting the non-catalytic activity of FAK, leading to increased antigen presentation and activation of cytotoxic CD8 T cells. PROTAC FAK degrader 3 enhances in vivo anti-tumor activity by promoting MHC-I expression and enhancing T cell activation. PROTAC FAK degrader 3 can be used in cancer research targeting FAK degradation in ovarian cancer, hepatocellular carcinoma, and other cancers. (Pink: FAK-IN-3:HY-143407, Blue: Thalidomide-4-OH:HY-103596, Blue + Black: FAK ligand-3: HY-W939883, Black: Linker) .

HY-123564

Mcl1-IN-7	Bcl-2 Family	Others
Mcl1-IN-7 (compound 11) is a reversible covalent inhibitor of Mcl-1 with the activity of inhibiting Mcl-1. By covalently targeting the non-catalytic lysine side chain of Mcl-1, it has higher potency than non-covalent counterparts and can be used to develop Mcl-1 inhibitory compounds and study related biological phenomena.

HY-116220

Mcl1-IN-14	Others	Others
Mcl1-IN-14 (compound 5) is a reversible covalent inhibitor of Mcl-1 with the activity of inhibiting Mcl-1. Mcl1-IN-14 covalently targets the non-catalytic lysine side chain of Mcl-1 and has higher potency than non-covalent counterparts, which can be used to develop Mcl-1 inhibitory compounds and study related biological phenomena.

HY-W339645

Naproxen ethyl ester (S)-Naproxen ethyl ester	COX	Inflammation/Immunology
Naproxen ethyl ester ((S)-Naproxen ethyl ester) is a nonsteroidal anti-inflammatory drug with activity in relieving pain, fever, swelling and stiffness. Naproxen ethyl ester exerts its effects by inhibiting non-selective cyclooxygenase (COX). The R-(-)-isomer of Naproxen ethyl ester shows stronger immunogenicity, and the Michaelis-Menten parameter of its catalytic reaction is K(M)=6.67 mM, and the catalytic efficiency is 5.8 x 10^4 times higher than that of the non-catalytic reaction .

HY-12135

Poloxipan	Polo-like Kinase (PLK) PIN1 STAT	Cancer
Poloxipan is a pan-specific polo-like kinase (PLK) inhibitor that can inhibit a non-catalytic region at the C-terminus called the Polo-box domain (PBD) found in kinases. The IC₅₀ values for Poloxipan against the PBDs of PLK-1/2/3 are 3.2 μM, 1.7 μM, and 3.0 μM, respectively. Poloxipan also inhibits other phospho-tyrosine binding domains, such as the forkhead-associated (FHA) domain of CHK-2, the WW domain of peptidyl-prolyl cis/trans isomerase (PIN1), and the phospho-tyrosine binding domains of STAT1/3/5 and lymphocyte-specific protein tyrosine kinase's SH2 domain. Poloxipan can be used in cancer research .

HY-179499

PROTAC EZH2 Degrader-9	PROTACs Histone Methyltransferase Apoptosis	Cancer
PROTAC EZH2 Degrader-9 is orally active EZH2 PROTAC degrader degrading EZH2 via the ubiquitin-proteasome pathway. PROTAC EZH2 Degrader-9 downregulates PRC2 core subunits and potent inhibition of H3K27me3 without affecting common CRBN neosubstrates while it was selective over GSp'T1 and ikZF1/3. PROTAC EZH2 Degrader-9 exhibits potent antiproliferative activity against multiple cancer cell lines by inducing cell cycle and apoptosis. PROTAC EZH2 Degrader-9 reverses PRC2-mediated gene silencing and inhibiting EZH2 non-catalytic target gene activation. PROTAC EZH2 Degrader-9 can be used for leukemia, lymphoma, and non-small cell lung cancer research .

HY-183724

MS8572	Deubiquitinase	Inflammation/Immunology
MS8572 is a selective OTUB1 covalent ligand. MS8572 covalently modifies the noncatalytic cysteine 23 residue of OTUB1 and does not inhibit OTUB1 deubiquitinase activity. MS8572 can be used for development of deubiquitinase-targeting chimeras for targeted protein stabilization .

Cat. No.	Product Name

HY-L914

Serine/Threonine Focused Covalent Fragment Library	3,208 compounds
In the research of covalent inhibitors targeting serine and threonine, scientists have found that the nucleophilicity of these hydroxyl groups is significantly enhanced due to the influence of their surrounding environment. This results in higher activity during catalytic reactions. Aspirin, which targets the non-catalytic domain serine (Ser529 in human COX1) of cyclooxygenase, exerts its anti-inflammatory effect through covalent binding. β-lactam antibiotics, which targets the catalytic domain serine of penicillin-binding proteins, interferes with bacterial cell wall synthesis. Through careful selection, we constructed a structural filter containing over 110 electrophilic groups. By analyzing the electrophilic fragments selected by the structural filter, we removed any molecules with trivial or undesirable structural features. Ultimately, we obtained 3,300 fragment molecules which can target serine and threonine residues and can be used for fragment-based covalent drug discovery.

Serine/Threonine Focused Covalent Fragment Library

3,208 compounds

In the research of covalent inhibitors targeting serine and threonine, scientists have found that the nucleophilicity of these hydroxyl groups is significantly enhanced due to the influence of their surrounding environment. This results in higher activity during catalytic reactions. Aspirin, which targets the non-catalytic domain serine (Ser529 in human COX1) of cyclooxygenase, exerts its anti-inflammatory effect through covalent binding. β-lactam antibiotics, which targets the catalytic domain serine of penicillin-binding proteins, interferes with bacterial cell wall synthesis.

Through careful selection, we constructed a structural filter containing over 110 electrophilic groups. By analyzing the electrophilic fragments selected by the structural filter, we removed any molecules with trivial or undesirable structural features. Ultimately, we obtained 3,300 fragment molecules which can target serine and threonine residues and can be used for fragment-based covalent drug discovery.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-113357

m-Coumaric acid	Structural Classification Monophenols Classification of Application Fields Ketones, Aldehydes, Acids Phenols Endogenous metabolite Inflammation/Immunology Disease Research Fields Source Classification	Endogenous Metabolite
m-Coumaric acid is a polyphenol metabolite from caffeic acid, formed by the gut microflora and the amount in human biofluids is diet-dependant. m-Coumaric acid is a BBB-penetrant metabolite of chlorogenic acid. m-Coumaric acid stimulates the cerebral nerves in vitro. m-Coumaric acid can evoke neurite outgrowth in hippocampal neuronal cells. m-Coumaric acid can promote neuronal differentiation. m-Coumaric acid increases spontaneous locomotor activity in mice by acting on the central nervous system. m-Coumaric acid inhibits the oxidation of L-dopa by epidermis tyrosinase. m-Coumaric acid attenuates non-catalytic protein glycosylation in retinas of diabetic rats .

HY-113357R

m-Coumaric acid (Standard)	Structural Classification Monophenols Microorganisms Ketones, Aldehydes, Acids Phenols Endogenous metabolite Source Classification	Reference Standards Endogenous Metabolite
m-Coumaric acid (Standard) is the analytical standard of m-Coumaric acid. This product is intended for research and analytical applications. m-Coumaric acid is a polyphenol metabolite from caffeic acid, formed by the gut microflora and the amount in human biofluids is diet-dependant. m-Coumaric acid is a BBB-penetrant metabolite of chlorogenic acid. m-Coumaric acid stimulates the cerebral nerves in vitro. m-Coumaric acid can evoke neurite outgrowth in hippocampal neuronal cells. m-Coumaric acid can promote neuronal differentiation. m-Coumaric acid increases spontaneous locomotor activity in mice by acting on the central nervous system. m-Coumaric acid inhibits the oxidation of L-dopa by epidermis tyrosinase. m-Coumaric acid attenuates non-catalytic protein glycosylation in retinas of diabetic rats .

Host:	Mouse (1) Rabbit (1)
Reactivity:	Human (2) Rat (2) Mouse (2) Monkey (1)
Application:	IHC-P (2) ICC/IF (1) IP (2) WB (2) FC (1)
Isotype:	IgG (1)
Conjugation:	Non-conjugated (2)
Clonality:	Polyclonal (1) Monoclonal (1)
Modification:	Unmodified (2)

Cat. No.	Compare	Product Name	Application	Reactivity	Image

HY-P85578

	AMPK beta 1 Antibody (YA5270) 1300015D22Rik; 5 AMP activated protein kinase subunit beta 1; 5''-AMP-activated protein kinase subunit beta-1; AAKB1_HUMAN; AMP-ACTIVATED PROTEIN KINASE, noncatalytic, BETA-1; AMP-activated, noncatalytic, beta-1; AMPK; AMPK beta 1 chain; AMPK subunit beta-1; AMPK-BETA-1; AMPKb; AU021155; E430008F22; HAMPKb; MGC17785; PRKAB1.	WB, ICC/IF, IP, IHC-P	Human, Mouse, Rat, Monkey
	AMPK beta 1 Antibody (YA5270) is a Mouse-derived and non-conjugated monoclonal antibody, targeting to AMPK beta 1.

HY-P80542

	AMPK beta 1 Antibody 5' ' -AMP-activated protein kinase subunit beta-1; AMP-activated; noncatalytic; beta-1; AMPK; AMPK beta 1 chain; AMPK subunit beta-1; AMPK-BETA-1; AMPKb; HAMPKb; PRKAB1	WB, IHC-P, FC, IP	Human, Mouse, Rat
	AMPK beta 1 Antibody is a Rabbit-derived and non-conjugated IgG polyclonal antibody, targeting to AMPK beta 1.

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