grp

Gastrin-releasing peptide (GRP) is a neuropeptide that stimulates gastrin release. It binds to (Ki = 300 nM) and stimulates amylase secretion in rat pancreatic AR42J cells (EC50 = 0.3 nM). GRP increases proliferation of human liver carcinoma HepG2 and MHCC97H cells but does not affect the proliferation of normal HL-7702 liver cells at a concentration of 1 nM. In vivo, GRP (0.35 nmol/kg/h) increases both pancreatic exocrine secretion and pancreatic polypeptide (PP) release in rats. It dose-dependently stimulates gastrin, pancreatic amylase, lipase, bilirubin, and acid output and induces gallbladder contraction in humans when administered at doses ranging from 1 to 27 pmol/kg per hour.

Mammalian bombesin-like peptide neurotransmitter that is an agonist for the gastrin-releasing peptide receptor (GRPR). GRP has been reported to activate GABAergic interneurons in the amygdala leading to increased GABA release and fear suppression in mice

GRP (porcine) acetate is the gastrin-releasing peptide extracted from porcine pancreata. GRP (porcine) acetate may have a role in the parasympathetic regulation of endocrine and exocrine secretion from the pig pancreas.

Grp94 Inhibitor-1 is a potent and selective inhibitor of Grp94 with an IC50 of 2 nM.

GRP-60367 is the first small molecule rabies virus (RABV) entry inhibitor, which has nanomolar effect on some RABV strains.

Human Follicular Gonadotropin Releasing Peptide (hF-GRP) is a hormonal peptide that, in vitro, can induce the secretion of pituitary luteinizing hormone (LH) and follicle-stimulating hormone (FSH) [1] [2].

GRP-60367 hydrochloride is a novel small-molecule entry inhibitor of rabies virus (RABV), exhibiting nanomolar potency against select RABV strains. This first-in-class compound effectively targets the RABV G protein [1].

GRP (14-27) (human, porcine, canine) serves as a ligand for bombesin receptors, with specific binding inhibited by GTP and GDP, but unaffected by GMP [1].

Grp94 Inhibitor-3 (Compound C6) is a selective inhibitor of glucose-regulated protein 94 (Grp94), with an affinity of 5.52 μM. It shows potential for research in primary open-angle glaucoma and metastatic cancer.

GRP78-IN-1 displays interactions with specific residues on the GRP78 protein with a binding energy of -8.07 kcal/mol. This compound possesses potent cytotoxic and anti-proliferative effects on cancer cells, particularly demonstrating promising apoptosis in breast cancer cells and wound healing properties [1].

GRP78-IN-2 is a glucose regulatory protein 78 (GRP78) inhibitor that preferentially targets GRP78 on the cell surface and has significant anti-angiogenic and anti-cancer effects without affecting other normal cells.

GRP78-IN-3, a potent small-molecule-competitive inhibitor of Hsp70 substrate binding and is a selective Grp78 (HSPA5) inhibitor with an IC50 of 0.59 μM. GRP78-IN-3 is 7-fold selective for HspA5 compared to HspA9 (IC50 of 4.3 μM) and >20-fold selective for HspA5 compared to HspA2 (IC50 of 13.9 μM).

Grp94-IN-2 is a inhibitor of Grp94.

GRP75-IN-1 hydrochloride (compound 33) is an agent for combating endometrial cancer (EC) by inducing apoptosis. It functions by targeting GRP75 and disrupting its interaction with IP3R, resulting in reduced Ca2+ levels in the mitochondria.

Grp94 Inhibitor-2 (compound 23) is a cyclopropane analog that exhibits high affinity for Glucose Regulated Protein 94 (Grp94), with dissociation constants (Kd) of 0.48 µM for Grp94 and 0.65 µM for Hsp90α.

Anti-Human/Mouse GRP78 Antibody (C38) is a mouse IgG2b kappa isotype antibody designed for in vivo use, specifically targeting GRP78. The recommended isotype control for this antibody is Mouse IgG2b kappa, Isotype Control.

Anti-Human/Mouse GRP78 Antibody (N88) is an IgG1, κ antibody inhibitor derived from mice, designed to target human or mouse GRP78.

CGRP antagonist 1 is a potent CGRP receptor antagonist with Ki values of 35 nM and IC50 values of 57 nM, respectively.CGRP antagonist 1 can be used for the study of cardiovascular and neurovascular diseases.

α-CGRP (rat) acetate is a calcitonin gene-related peptide (CGRP). CGRP (rat) acetate is a potent vasodilator.

CGRP Antagonist 6 (Compound 23) is a potent CGRP receptor antagonist (Ki: 0.84 nM). It is utilized in the study of migraines.

PSMA/GRPR ligand 1 (compound 3) is a bispecific ligand with dual targeting capabilities for tumors that express PSMA(+) and GRPR(+).

CGRP antagonist 7 is a potent calcitonin gene-related peptide receptor (CGRP) antagonist with a Ki value of 0.029 nM. It effectively inhibits CGRP receptor-mediated cyclic adenosine monophosphate (cAMP) production, with an IC50 value of 1.5 nM. This compound is useful in migraine research.

Tyr-α-CGRP is an N-terminal extended tyrosinated analogue of α-calcitonin gene-related peptide . It binds to amylin receptors AMY1 and AMY3 in COS-7 cells expressing the human receptors (IC50s = 141 and 1.86 nM, respectively). Tyr-α-CGRP also binds to and stimulates cAMP accumulation in rat L6 myocytes (IC50 = 4 nM; EC50 = 12 nM). It also binds to rat brain and spleen membrane preparations (IC50s = 0.2 and 0.5 nM, respectively), induces positive chronotropic and inotropic effects in isolated right and left guinea pig atria (EC50s = 282 and 74 nM, respectively), and inhibits the twitch response in rat vas deferens (EC50 = 1.9 nM).

Tyr-α-CGRP (rat) is an N-terminally tyrosinated analog of the neuropeptide α-CGRP that induces a fall in resting tension of isolated opossum internal anal sphincter (IAS) with an EC50 value of 178 nM.