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Allosteric Small Molecules

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Btk (1) DNA/RNA Synthesis (1) Interleukin Related (1) PI3K (1) Protease Activated Receptor (PAR) (1)
By Research Areas:	Cancer (3) Cardiovascular Disease (1) Inflammation/Immunology (2) Neurological Disease (1)

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Biochemical Assay Reagents

Targets Recommended: Small Interfering RNA (siRNA) Repulsive guidance molecule

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-123617

AZ8838	Protease Activated Receptor (PAR)	Inflammation/Immunology
AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pK_i of 6.4 for hPAR2 .

HY-148788

Osivelotor GBT-601; GBT-021601	Others	Others
Osivelotor is an orally effective small molecule. Osivelotor is an allosteric regulator of deoxyhemoglobin S (HbS). Osivelotor increases the affinity of HbS to oxygen, inhibits HbS polymerization, and thus prevents erythrocyte sickling in the blood. Osivelotor can be used for research of sickle cell disease (SCD) .

HY-154848

UCL-TRO-1938 2 Publications Verification	PI3K Akt	Cardiovascular Disease Neurological Disease Cancer
UCL-TRO-1938 is a potent small molecule allosteric activator of PI3Kα with an EC₅₀ value of approximately 60 μM. UCL-TRO-1938 can induce cell proliferation and has cardioprotective effects from ischaemia reperfusion injury and enhances nerve regeneration following nerve crush .

HY-178714

JNJ627	Interleukin Related	Inflammation/Immunology
JNJ627 is a small molecule allosteric inhibitor of IL-17A with a K_D of 92 nM. JNJ627 effectively inhibits the binding of IL-17A and IL-17RA, with an IC₅₀ value of 16 nM. JNJ627 is capable of inhibiting the secretion of G-CSF (granulocyte colony-stimulating factor) caused by IL-17A stimulation. JNJ627 can be used for the study of autoimmune diseases (such as psoriasis) .

HY-162081

BTK-IN-32	Btk	Cancer
BTK-IN-32 (compound C2) is a potent inhibitor of BTK. BTK-IN-32 activates full-length BTK and smaller multidomain BTK fragments instead of the isolated kinase domain .

HY-141520G

ART558	DNA/RNA Synthesis	Cancer
ART558 (GMP) is ART558 (HY-141520) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. ART558 is a potent, selective and allosteric DNA polymerase theta (Polθ) inhibitor (IC₅₀=7.9 nM). ART558 elicits BRCA-gene synthetic lethality and DNA damage. ART558 can be used for the research of cancer, such as breast cancer .

Cat. No.	Product Name

HY-L170

Allosteric Modulators (AMs) Compound Library	224 compounds
An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenous ligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands. MCE designs a unique collection of 224 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.

Allosteric Modulators (AMs) Compound Library

224 compounds

An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenous ligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands.

MCE designs a unique collection of 224 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.

Cat. No.	Product Name	Type

HY-141520G

ART558 (GMP)	Fluorescent Dye
ART558 (GMP) is ART558 (HY-141520) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. ART558 is a potent, selective and allosteric DNA polymerase theta (Polθ) inhibitor (IC₅₀=7.9 nM). ART558 elicits BRCA-gene synthetic lethality and DNA damage. ART558 can be used for the research of cancer, such as breast cancer .

ART558 (GMP)

Fluorescent Dye

ART558 (GMP) is ART558 (HY-141520) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. ART558 is a potent, selective and allosteric DNA polymerase theta (Polθ) inhibitor (IC₅₀=7.9 nM). ART558 elicits BRCA-gene synthetic lethality and DNA damage. ART558 can be used for the research of cancer, such as breast cancer .

Cat. No.	Product Name	Type

HY-141520G

ART558 (GMP)	Biochemical Assay Reagents
ART558 (GMP) is ART558 (HY-141520) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. ART558 is a potent, selective and allosteric DNA polymerase theta (Polθ) inhibitor (IC₅₀=7.9 nM). ART558 elicits BRCA-gene synthetic lethality and DNA damage. ART558 can be used for the research of cancer, such as breast cancer .

ART558 (GMP)

Biochemical Assay Reagents

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