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Results for "

small G-proteins

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apelin Receptor (APJ) (2) Apoptosis (1) Autophagy (1) Cannabinoid Receptor (1) Complement System (1) Endogenous Metabolite (1) Exosomes (1) G Protein-coupled Receptor Kinase (GRK) (1) GGTase (1) GPR35 (1) Mas-related G-protein-coupled Receptor (MRGPR) (1) mRNA (1) Opioid Receptor (1) Prostaglandin Receptor (1) RABV (1) Ras (1) Reference Standards (1)
By Research Areas:	Cancer (2) Cardiovascular Disease (2) Endocrinology (1) Infection (1) Inflammation/Immunology (3) Metabolic Disease (2) Neurological Disease (2)
Oligonucleotides:	Chemokine & Receptors (1) mRNA (1)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Oligonucleotides

Targets Recommended: Small Interfering RNA (siRNA)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100197

Synaptamide 1 Publications Verification N-Docosahexaenoyl ethanolamine (DHEA); Docosahexaenoyl ethanolamide	Cannabinoid Receptor	Neurological Disease
Synaptamide (Dehydroepiandrosteron; DHEA) is an endogenous metabolite and structural analogue of Anandamide. Synaptamide binds to both the cannabinoid-1 and 2 (CB1 and CB2) cannabinoid receptors and has anti-inflammatory properties. Synaptamide is the first small-molecule endogenous ligand of an adhesion G protein-coupled receptor (aGPCR) .

HY-103080

CMF019	Apelin Receptor (APJ)	Cardiovascular Disease
CMF019 is an orally active, potent and small molecule agonist at Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse, respectively. CMF019 mimics the beneficial cardiovascular actions of apelin in rodents . Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin. CMF019 is promising for research of chronic diseases, such as, pulmonary arterial hypertension .

HY-117992

BR103	Complement System	Inflammation/Immunology
BR103 is a C3aR-specific small molecule ligand. BR103 can be used to measure ligand affinity for a G protein-coupled receptor for saturation and competitive binding .

HY-133735A

GRP-60367 hydrochloride 1 Publications Verification	RABV	Infection
GRP-60367 hydrochloride is a first-in-class small-molecule rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains. GRP-60367 hydrochloride specifically targets the RABV G protein .

HY-114810

Prostaglandin F2α serinol amide	Prostaglandin Receptor	Endocrinology
Prostaglandin F2α serinol amide is a serinolamide G protein-coupled receptor that increases calcium levels in human non-small cell lung cancer cells. Prostaglandin F2α is also a luteinizing hormone in sheep and may be a nociceptive mediator in the spinal cord .

HY-173003

EP-3945	Mas-related G-protein-coupled Receptor (MRGPR)	Inflammation/Immunology
EP-3945 is a potent agonist of Mas-related G protein-coupled receptor (MRGPR), more effective than the MRGPRD small molecule agonist β-Alanine (HY-N0230). MRGPR plays a crucial role in inflammatory pruritus and pain sensation. Additionally, MRGPR binds to Gq (MRGPRX2, MRGPRX4, MRGPRX1 couple with Gq; MRGPRX2, MRGPRD couple with Gi), with EP-3945 measured EC₅₀ for Gq being 211.6 nM .

HY-113225B

Guanosine triphosphate tritris GTP tritris	Endogenous Metabolite Exosomes	Cancer
Guanosine triphosphate tritris (GTP tritris) serves as a vital enhancer of myogenic cell differentiation and plays a critical role in modulating miRNA-myogenic regulator factors. It also facilitates the release of exosomes enriched with guanosine and guanosine-derived molecules, and is regarded as an activated precursor for RNA synthesis. In mitochondrial function, GTP participates in the import of proteins into the matrix, which is essential for various regulated pathways, and is involved in initiating peptide synthesis through the binding of formylmethionyl-tRNA to the ribosome, as well as polypeptide chain elongation. Additionally, GTP acts as a phosphate and pyrophosphate carrier that channels chemical energy into specific biosynthetic pathways. It activates signal transducing G proteins that regulate cellular processes such as proliferation and differentiation, and its hydrolysis by small GTPases, including Ras and Rho, is integral to both proliferation and apoptosis. Furthermore, the small GTPase Rab is instrumental in vesicle docking, fusion, and formation. Beyond signal transduction, GTP is an energy-rich precursor in the enzymatic biosynthesis of DNA and RNA.

HY-121532

(-)-Rasfonin	Ras Apoptosis Autophagy	Cancer
(-)-Rasfonin is a fungal secondary metabolite and inhibits small G proteins Ras. (-)-Rasfonin induces apoptosis, necrosis and autophagy in ACHN cells (a renal carcinoma cell line) .

HY-159923

BPRMU191	Opioid Receptor	Neurological Disease
BPRMU191 is a μ-opioid receptor (MOR) modulator that converts small-molecule morphinan antagonists into G protein-biased MOR agonists, thereby inducing MOR-dependent activation and analgesic effects. Co-administration of BPRMU191 with morphinan antagonists provides analgesia while reducing side effects such as gastrointestinal dysfunction, antinociceptive tolerance, and dependency-related adverse effects. BPRMU191, in combination with morphinan antagonists, offers a potential strategy for studying severe pain management and G protein-coupled receptor modulation .

HY-12976

DS-1558	G Protein-coupled Receptor Kinase (GRK)	Metabolic Disease
DS-1558 is an orally active small molecule G protein-coupled receptor 40 agonist. DS-1558 not only increases the glucose-stimulated insulin secretion by glucagon like peptide-1 (GLP-1) but also potentiated the maximum insulinogenic effects of GLP-1 after an intravenous glucose injection in normal Sprague Dawley rats. DS-1558 is promising for research of type 2 diabetes .

HY-174744

Human CCR4 mRNA	mRNA	Inflammation/Immunology
Human CCR4 mRNA encodes the human C-C motif chemokine receptor 4 (CCR4) protein, a member of G protein-coupled receptors family. CCR4 is a receptor for the CC chemokine - MIP-1, RANTES, TARC and MCP-1. Chemokines are a group of small polypeptide, structurally related molecules that regulate cell trafficking of various types of leukocytes. The chemokines also play fundamental roles in the development, homeostasis, and function of the immune system, and they have effects on cells of the central nervous system as well as on endothelial cells involved in angiogenesis or angiostasis.

HY-178725

ML301	GPR35	Others
ML301 is a small molecule *G-protein* agonist. ML301 can be inhibited by SR142948A with an IC₅₀ of around 63 nM. ML301 fully competes for ¹²⁵I-NT binding .

HY-103080R

CMF019 (Standard)	Apelin Receptor (APJ) Reference Standards	Cardiovascular Disease
CMF019 (Standard) is the analytical standard of CMF019 (HY-103080). This product is intended for research and analytical applications. CMF019 is an orally active, potent and small molecule agonist at Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ with pK_i values of 8.58, 8.49 and 8.71 for human, rat, and mouse, respectively. CMF019 mimics the beneficial cardiovascular actions of apelin in rodents . Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin. CMF019 is promising for research of chronic diseases, such as, pulmonary arterial hypertension .

HY-114159

GGTI-2166	GGTase	Metabolic Disease
GGTI-2166 is a geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2166 blocks geranylgeranylation modification of target proteins. GGTI-2166 inhibits RANKL- or TNF-α-induced pre-osteoclast formation and TRAP activity. GGTI-2166 is applicable to research on osteoclast differentiation .

Cat. No.	Product Name

HY-L006

GPCR/G Protein Compound Library	3,389 compounds
GPCRs are a large family of cell surface receptors that respond to a variety of external signals. Binding of a signaling molecule to a GPCR results in G protein activation, which in turn triggers the production of any number of second messengers. GPCRs play an important role in the human body, and increased understanding of these receptors has greatly affected modern medicine. In fact, researchers estimate that between one-third to one-half of all approved drugs act by binding to GPCRs. GPCRs are a large group of drug targets in drug discovery. MCE provides a unique collection of 3,389 small molecules targeting GPCRs that can be used in the screening for various GPCRs-related research and drug development projects.

GPCR/G Protein Compound Library

3,389 compounds

GPCRs are a large family of cell surface receptors that respond to a variety of external signals. Binding of a signaling molecule to a GPCR results in G protein activation, which in turn triggers the production of any number of second messengers. GPCRs play an important role in the human body, and increased understanding of these receptors has greatly affected modern medicine. In fact, researchers estimate that between one-third to one-half of all approved drugs act by binding to GPCRs. GPCRs are a large group of drug targets in drug discovery.

MCE provides a unique collection of 3,389 small molecules targeting GPCRs that can be used in the screening for various GPCRs-related research and drug development projects.

HY-L928

GPCR Targeted Diversity Library	7,113 compounds
G protein-coupled receptors (GPCRs) are membrane proteins in humans and one of the most important targets in drug discovery. Approximately 35% of launched drugs are targeted GPCRs, making them a crucial class of targets in drug discovery. The orthosteric site of a GPCR is its endogenous ligand’s (such as neurotransmitters or hormones) binding site. This site plays a central role in signal transduction. Small molecules binding to this site typically contain a protonatable amino group, enabling the formation of salt bridges or hydrogen bonds with acidic residues in the binding pocket. In contrast, the allosteric site does not directly initiate signaling but modulates the signal intensity of the GPCR by altering or stabilizing the conformation of the orthosteric site. Small molecules binding to the allosteric site often contain multiple aromatic rings to occupy hydrophobic pockets and achieve their functional effects. MCE has collected over 7,113 reported bioactive molecules targeting GPCRs, covering Class A, B, and C GPCRs. These small molecules were subjected to AI representation to extract 2D and 3D features. Subsequently, we do screening by AI score based on similarity to identify molecules in diversity library highly similar to the reported bioactive molecules in both 2D and 3D, with a threshold greater than 0.7. Further screening based on cLogP was applied to select molecules with good lipophilicity, which facilitates the binding of small molecules to GPCRs. This diversity library can be widely applied to the discovery of compounds targeting GPCR proteins.

GPCR Targeted Diversity Library

7,113 compounds

G protein-coupled receptors (GPCRs) are membrane proteins in humans and one of the most important targets in drug discovery. Approximately 35% of launched drugs are targeted GPCRs, making them a crucial class of targets in drug discovery.

The orthosteric site of a GPCR is its endogenous ligand’s (such as neurotransmitters or hormones) binding site. This site plays a central role in signal transduction. Small molecules binding to this site typically contain a protonatable amino group, enabling the formation of salt bridges or hydrogen bonds with acidic residues in the binding pocket. In contrast, the allosteric site does not directly initiate signaling but modulates the signal intensity of the GPCR by altering or stabilizing the conformation of the orthosteric site. Small molecules binding to the allosteric site often contain multiple aromatic rings to occupy hydrophobic pockets and achieve their functional effects.

MCE has collected over 7,113 reported bioactive molecules targeting GPCRs, covering Class A, B, and C GPCRs. These small molecules were subjected to AI representation to extract 2D and 3D features. Subsequently, we do screening by AI score based on similarity to identify molecules in diversity library highly similar to the reported bioactive molecules in both 2D and 3D, with a threshold greater than 0.7. Further screening based on cLogP was applied to select molecules with good lipophilicity, which facilitates the binding of small molecules to GPCRs. This diversity library can be widely applied to the discovery of compounds targeting GPCR proteins.

HY-L132

Chemokine Compound Library	239 compounds
Chemokines, or chemotactic cytokines, are small cytokines or signaling proteins secreted by cells. They are a component of intercellular communication, controlling the directional movement of immune cells especially leukocytes, as well as other cell types, for instance, endothelial and epithelial cells, which are essential to maintain human health and the function of the immune system. The biological effects of chemokines are achieved by binding to chemokine receptors, which are G protein-coupled receptors found on the surface of leukocytes. Some chemokine receptors are involved in directing tumor metastasis and over-expression by certain tumors. So inhibiting the interaction between chemokine and chemokine receptors on the surface of tumor cells may be a new possible therapeutic approach. Some chemokine receptors are coreceptors for HIV entry, and related inhibitors have been approved by the FDA to treat patients with HIV. Obviously, chemokines and chemokine receptors have become new targets for studying cancer, HIV, inflammation, and other diseases. MCE supplies a unique collection of 239 chemokine or chemokine receptor inhibitors and activators, all of which have the identified inhibitory or activated effect on chemokine or chemokine receptors. MCE Chemokine Library is a useful tool for drug research related to cancer, AIDS, and wound therapy.

Chemokine Compound Library

239 compounds

Chemokines, or chemotactic cytokines, are small cytokines or signaling proteins secreted by cells. They are a component of intercellular communication, controlling the directional movement of immune cells especially leukocytes, as well as other cell types, for instance, endothelial and epithelial cells, which are essential to maintain human health and the function of the immune system.

The biological effects of chemokines are achieved by binding to chemokine receptors, which are G protein-coupled receptors found on the surface of leukocytes. Some chemokine receptors are involved in directing tumor metastasis and over-expression by certain tumors. So inhibiting the interaction between chemokine and chemokine receptors on the surface of tumor cells may be a new possible therapeutic approach. Some chemokine receptors are coreceptors for HIV entry, and related inhibitors have been approved by the FDA to treat patients with HIV. Obviously, chemokines and chemokine receptors have become new targets for studying cancer, HIV, inflammation, and other diseases.

MCE supplies a unique collection of 239 chemokine or chemokine receptor inhibitors and activators, all of which have the identified inhibitory or activated effect on chemokine or chemokine receptors. MCE Chemokine Library is a useful tool for drug research related to cancer, AIDS, and wound therapy.

(-)-Rasfonin	Monophenols Microorganisms Classification of Application Fields Phenols Disease Research Fields Cancer Source Classification	Ras Apoptosis Autophagy
(-)-Rasfonin is a fungal secondary metabolite and inhibits small G proteins Ras. (-)-Rasfonin induces apoptosis, necrosis and autophagy in ACHN cells (a renal carcinoma cell line) .

Cat. No.	Product Name		Classification

HY-174744

Human CCR4 mRNA		mRNA Chemokine & Receptors
Human CCR4 mRNA encodes the human C-C motif chemokine receptor 4 (CCR4) protein, a member of G protein-coupled receptors family. CCR4 is a receptor for the CC chemokine - MIP-1, RANTES, TARC and MCP-1. Chemokines are a group of small polypeptide, structurally related molecules that regulate cell trafficking of various types of leukocytes. The chemokines also play fundamental roles in the development, homeostasis, and function of the immune system, and they have effects on cells of the central nervous system as well as on endothelial cells involved in angiogenesis or angiostasis.

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