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Non-catalytic

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Amine N-methyltransferase (1) Aurora Kinase (2) COX (1) HIV (1) HIV Integrase (1) LRRK2 (1) PIN1 (1) Polo-like Kinase (PLK) (1) PROTACs (2) STAT (1)
By Research Areas:	Cancer (4) Infection (1) Inflammation/Immunology (1) Neurological Disease (1)

Inhibitors & Agonists

Screening Libraries

Antibodies

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-143345

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

HY-141512

JB170 1 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-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-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-158038

AurkA allosteric-IN-1	Aurora Kinase	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-123564

Mcl1-IN-7	Others	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-W093017

4-Chloropyridine	Amine N-methyltransferase	Others
4-Chloropyridine is an inhibitor of nicotinamide N-methyltransferase (NNMT). It can act as a substrate for NNMT and, during its catalytic reaction, enhances the electrophilicity of the C4 position by methylating the nitrogen atom of the pyridine ring. This promotes an aromatic nucleophilic substitution reaction with the non-catalytic cysteine (C159) in NNMT, ultimately leading to the suicide inhibition of NNMT's activity. 4-Chloropyridine holds potential for the development of NNMT activity-based probes .

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 .

Cat. No.	Product Name

HY-L914

Serine/Threonine Focused Covalent Fragment Library	3,300 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

3,300 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.	Compare	Product Name	Application	Reactivity

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 non-conjugated and Rabbit origined polyclonal antibody about 30 kDa, targeting to AMPK beta 1. It can be used for WB,IHC-P,FC,IP assays with tag free, in the background of Human, Mouse, Rat.

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