hsp90 cdc37 in 1

Hsp90-Cdc37-IN-1 is an Hsp90-Cdc37 interaction disruptor (IC50: 140 nM) that inhibits cell migration and reverses drug resistance.

Hemokinin 1 (mouse) acetate is a selective excitogen 1 receptor agonist with a Ki value of 0.175 nM for the human NK1 receptor and 560 nM for the human NK2 receptor.

Tripeptide-1 Acetate is a biologically active peptide

Glp-1(7-37) acetate is an intestinal insulin hormone that enhances glucose-induced insulin secretion.

pTH (1-37) (human), a fragment of parathyroid hormone (PTH), promotes cAMP formation and enhances alkaline phosphatase activity. Additionally, it fosters growth, elevates bone calcium content, and augments bone mineral density (BMD) in uremic animals. This compound shows promise for osteoporosis research [1] [2] [3].

HDAC6/HSP90-IN-1 is a potent and selective dual inhibitor of HDAC6 (IC50: 4.3 nM) and HSP90 (IC50: 46.8 nM).HDAC6/HSP90-IN-1 downregulates PD-L1 expression in INF-γ-treated H1975 lung cancer cells.HDAC6/HSP90-IN-1 exhibits tumor growth inhibition in H1975 xenograft mice.HDAC6/HSP90-IN-1 is a potent and selective dual inhibitor of HDAC6 (IC50: 4.3 nM) and HSP90 (IC50: 46.8 nM). 1 exhibited tumor growth inhibition in H1975 xenograft mice.

FKBP51-Hsp90-IN-1 (Compound D10) serves as a selective inhibitor targeting the FKBP51-Hsp90 protein-protein interaction, demonstrating an IC 50 value of 0.1 μM against FKBP51. It holds potential for research applications in stress-related diseases, Alzheimer's disease, and metabolic disorders [1].

Amylin (1-37) (human) (hIAPP (1-37)), a peptide hormone located in pancreatic beta-cell secretory granules, is characterized by an amidated C-terminus and a disulfide bond between cysteine residues 2 and 7 [1].

Glucagon-like peptide 1 (1-37), human acetate is a highly potent the GLP-1 receptor agonist.

PTH-Related Protein (1-37) (human, mouse, rat) is a peptide analog of parathyroid-hormone-related protein (pTHrP), which plays a role in the physiological regulation of bone formation [1].

β-Amyloid (1-37) (human) is potentially associated with mental status in Alzheimer's disease.

GLP-1 (7-37) is a truncated, bioactive form of GLP-1 that is the product of proglucagon processing in intestinal endocrine L cells.

MAO A HSP90-IN-1 (4-b) is a dual inhibitor of MAO A and HSP90, with IC50 values of 1.77 μM in glioblastoma (GBM) GL26 cells and 0.019 μM against HSP90α. This compound impairs MAO A activity, disrupts HSP90 binding, and downregulates HER2 and phospho-Akt expressions, thus inhibiting GBM growth. Additionally, it reduces PD-L1 expression, thwarting T cell activation and potential tumor immune evasion. MAO A HSP90-IN-1 (4-b) is valuable for research into brain tumor-related diseases [1].

Aha1 Hsp90-IN-1 (Compound 17) is an inhibitor of the Aha1 Hsp90 complex, effectively disrupting their interaction (IC50: 3.32 μM) and inhibiting tau protein aggregation.

HSP90/mTOR-IN-1 is an effective and orally administrable inhibitor targeting both Hsp90 and mTOR, displaying IC50 values of 69 nM and 29 nM, respectively. This compound inhibits the proliferation of SW780 cells by overly activating the PI3K/AKT/mTOR pathway and induces apoptosis and autophagy through its selective inhibition of Hsp90 and mTOR. Additionally, HSP90/mTOR-IN-1 exhibits significant anti-tumor activity in vivo and is applicable in bladder cancer research.

The truncated glucagon-like peptides GLP-1(7-37) is naturally occurring peptide product of the preproglucagon gene that are synthesized primarily in the intestine and acts as incretin that are released from the intestine into the bloodstream in response to food and stimulate insulin secretion. GLP-1(7-37) produced a dose-related enhancement of the glucose-stimulated increase in plasma insulin concentration and an increased rate of glucose infusion in Sprague-Dawley Rats at a dosing rang of 0.5, 5, or 50 pmol/min/kg. Further, infusion of GLP-1(7-37) for 60 mins produced a small transitory increase in plasma insulin concentration in fasted rats and fed rats and a slight transitory decrease in plasma glucose concentration. Moreover, GLP-1(7-37) (5 pmol/min/kg IV) infusion for 6 h in Sprague-Dawley rats produced a sustained increase in plasma insulin concentration relative to levels in rats infused with vehicle[1].

GRKs-IN-1 hydrochloride has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50: 130 nM) and GRK5 (IC50: 7.1 μM).

HIV-1 inhibitor-37 (Compound 83) is a potent HIV-1 inhibitor with significant potential as an innovative latent HIV-1 reactivating agent [1].

Glucagon-like peptide 1 (1-37), human, is a highly potent agonist of the GLP-1 receptor and a pancreatic hormone synthesized by post-translational processing of proglucagon. Unlike truncated forms of GLP-1, it neither affects food intake in rats nor enhances pancreatic insulin secretion.

Glucagon-like peptide 1 (1-37), human (TFA), is a highly potent agonist of the GLP-1 receptor and is a pancreatic hormone synthesized through post-translational processing of proglucagon.

Kaliotoxin (1-37), a toxin derived from the scorpion Androctonus mauretanicus mauretanicus, acts as a potent blocker of calcium-dependent potassium channels [1].

CAY10747 is an inhibitor of the protein-protein interaction between heat shock protein 90 (Hsp90) and cell division cycle 37 (Cdc37) and a derivative of celastrol .1It decreases protein levels of the Hsp90-Cdc37 complex and the Hsp90-Cdc37 clients phosphorylated Akt and Cdk4 in A549 cells when used at a concentration of 5 μM. CAY10747 inhibits proliferation of A549, MCF-7, HOS, and HepG2 cells (IC50s = 0.41, 0.64, 0.9, and 0.94 μM, respectively) and induces apoptosis in A549 cells. 1.Li, N., Xu, M., Wang, B., et al.Discovery of novel celastrol derivatives as Hsp90-Cdc37 interaction disruptors with antitumor activityJ. Med. Chem.62(23)10798-10815(2019)