thr-1

THR-β Modulator-1 (Compound 1a) is a potent modulator of the thyroid hormone receptor β, utilized in the study of thyroid hormone receptor-associated disorders [1].

THRβ Agonist 1 is a potent and selective THRβ agonist. THRβ Agonist 1 has the potential to be used in studies of thyroid hormone receptor related disorders.

Tnrnflrfamide is a SCP (small cardioactive peptide)-like peptide found in lobster neurons; exhibits FMRFamide-like immunoreactivity.

PCO371 (2,4-Imidazolidinedione, 1-(3,5-dimethyl-4-(2-((4-oxo-2-(4-(trifluoromethoxy)phenyl)-1,3,8-triazaspiro(4.5)dec-1-en-8-yl)sulfonyl)ethyl)phenyl)-5,5-dimethyl-) is an orally active full agonist of parathyroid hormone receptor 1. It has no effect on PTH type 2 receptor.

ZK824190 is an orally available and selective inhibitor of urokinase plasminogen activator (uPA), with IC50 values of 237 nM for uPA, 1600 nM for tPA, and 1850 nM for Plasmin.

NH-3 is a potent orally active thyroid hormone receptor (THR) antagonist which exhibits reversible behavior, demonstrated by an IC 50 of 55 nM. Derived from the selective thyromi-metic GC-1, NH-3 effectively inhibits the binding of thyroid hormones to their respective receptors, resulting in hindered cofactor recruitment.

BAY-1816032 is a benzimidazole budding inhibition relieved homolog protein 1 kinase (BUB1) inhibitor with IC50 of 0.7 nM and is orally active and abolishes nocodazole-induced Thr-120 phosphorylation of histone H2A, a major BUB1 target protein, in HeLa cells with IC50 of 29 nM.

FMOC-L-THR (AZP-531) is an analogue of unacylated ghrelin designed to improve glycaemic control and reduce weight. The O-glycosidic linkage and the O-acetyl protection in this building block is stable to both piperidine and TFA, making it completely compatible with standard protocols in Fmoc solid phase peptide synthesis. The Tn antigen is a tumor-associated carbohydrate antigen that is not normally expressed in peripheral tissues or blood cells. Expression of this antigen, which is found in a majority of human carcinomas of all types, arises from a blockage in the normal O-glycosylation pathway in which glycans are extended from the common precursor GalNAcα1-O-Ser/Thr (Tn +antigen)[1].

N-Myristoyl-Lys-Arg-Thr-Leu-Arg is a protein kinase C (PKC) inhibitor (IC50 = 75 μM) that effectively inhibits IL-2 receptor induction and IL-2 production in the human leukemic cell line Jurkat [1].

Fmoc-Thr(GalNAc(Ac)3-β-D)-OH impedes cancer cell proliferation by selectively interacting with complex oncogenic pathways and enhancing the immune response [1].

ThrRS-IN-1 (Compound 30d) is a potent inhibitor of threonyl-tRNA synthetase (ThrRS) from Salmonella enterica (Se ThrRS), exhibiting an IC50 of 1.4 μM and a Kd of 1.36 μM. It uniquely targets both the tRNA Thr and L-threonine binding sites of ThrRS, demonstrating significant antibacterial activities [1].

Picornain 3C, a protease present in picornaviruses, exhibits endopeptidase activity by specifically cleaving Gln-Gly bonds within the poliovirus polyprotein and, through substitution, cleaves Glu for Gln, and Ser or Thr for Gly in other picornaviruses. This protease operates on non-terminal sequences and intermediates between serine peptidase chymotrypsin and cysteine peptidase papain, showcasing its role in viral polyprotein processing [1].

PPM1A-IN-1 (Compound IV-4) is an inhibitor of the PP2C Ser Thr protein phosphatase Mg2+ Mn2+-dependent 1A. It exhibits antibacterial activity against Mycobacterium tuberculosis.

PKCδ Peptide Substrate is a highly specific substrate for the δ-type of Protein kinase C, composed of a sequence that mirrors murine eEF-1α (422-443) and includes Thr-431 [1].

Sobetirome (IACS-010759) is a selective agonist of thyroid hormone receptor β (TRβ) and binds selectively to TRβ-1 (EC50: 0.16 μM).

Upamostat is an inhibitor of a serine protease and is a urokinase plasminogen activator (uPA) inhibitor.

Myristoyl-(Lys12,27,28)-VIP-Gly-Gly-Thr (free acid) acts as a selective and potent antagonist of the VPAC2 receptor [1].

DOTA-LM3 is a somatostatin receptor (SSTR) antagonist, with LM3 denoting the peptide sequence p-Cl-Phe-cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr-NH2. It is utilized in the isotopic labeling of tumors for in vivo tracing, notably with 177Lu-DOTA-LM3 and 68Ga-DOTA-LM3. The derivative 68Ga-DOTA-LM3 exhibits promising biodistribution, high tumor uptake, efficient tumor retention, and minimal safety concerns, while 177Lu-DOTA-LM3 is applied in research on DOTATOC-negative liver metastases including pancreatic NET and extensive tumor thrombosis [1] [2].

Pyr-Arg-Thr-Lys-Arg-AMC TFA, an AMC-tagged decapeptide, is selectively cleaved by proteases such as trypsin and thrombin, serving as a substrate for measuring protease activity and assessing enzyme inhibitor efficacy [1].

H-Val-Thr-Cys-Gly-OH is a cell attachment peptide that promotes cell adhesion and facilitates various cell interactions [1].

Compound 40, known as THR-β modulator-2, acts as a modulator for the thyroid hormone receptor β (THR-β) [1].

DOTA-LM3 TFA is a somatostatin receptor (SSTR) antagonist with the molecular structure p-Cl-Phe-cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr-NH2, used for in vivo tumor tracing via isotopic labeling, such as 177Lu-DOTA-LM3 TFA and 68Ga-DOTA-LM3 TFA. The 68Ga-labeled compound shows favorable biodistribution, high tumor uptake, good tumor retention, and minimal safety concerns, while the 177Lu-labeled variant targets DOTATOC-negative liver metastases, including pancreatic NET and extensive tumor thrombosis [1] [2].

RYTVELA TFA (H-Arg-Tyr-Thr-Val-Glu-Leu-Ala-OH) is a non-competitive metabotropic interleukin-1 receptor inhibitor with anti-inflammatory activity that inhibits upregulation of inflammation and uterine activation, and may be used for the prevention of preterm labor and for fetal protection.

Lys-Arg-Thr-Leu-Arg-Arg (KRTLRR), a hexapeptide substrate for protein kinase C associated with the EGF receptor, facilitates the determination of enzyme activity [1].

MASTL-IN-2 is a potent inhibitor of microtubule-associated serine/threonine kinase-like (MASTL). It demonstrates notable efficacy in suppressing the proliferation of human epithelial MIA PaCa cancer cells, exhibiting an IC50 value of 2.8 nM [1].

Histatin-3, a 32-amino-acid peptide, exhibits potent antimicrobial activities and serves as a substrate for proprotein convertase 1 (PC1), where it is primarily cleaved at a site carboxy-terminal to Arg25 (HRGYR↓SN). Additionally, it acts as a moderately potent, reversible, and competitive inhibitor of furin-mediated cleavage of the pentapeptide pGlu-Arg-Thr-Lys-Arg-MCA fluorogenic substrate, with an inhibition constant (Ki) estimated at 1.98 μM [1].

H-Pro-Thr-Glu-Phe-p-nitro-Phe-Arg-Leu-OH is a water-soluble polypeptide that serves as a substrate for the enzymes cathepsin D, pepsin, and pepsinogen, with potential applications in biochemical analysis [1] [2].

THR-β Agonist 6, a selective and orally active compound targeting the thyroid hormone receptor β (THR-β), demonstrates specificity with EC50 values of 0.03 μM for THR-β and 0.22 μM for THR-α. This compound boasts a remarkable liver-to-serum ratio of 93:1 in mouse models, underscoring its efficacy and potential for research in nonalcoholic steatohepatitis (NASH) [1].

THR-β agonist 5 (compound 54) is a potent THR-β agonist with an EC50 of less than 50 nM [1].

THR-18 is an 18-mer peptide derived from the sequence of human plasminogen activator inhibitor 1 (PAI-1), having the ability to bind to a site of tissue plasminogen activator (tPA) distal to its catalytic site and uncouple the beneficial clot-dissolving properties of tPA from its deleterious non-fibrinolytic effects.

CC260, a selective inhibitor for PI5P4Kα and PI5P4Kβ with Kis of 40 nM and 30 nM respectively, exhibits minimal to no inhibition against other protein kinases like Plk1 and RSK2. It is applicable in the research of cell energy metabolism, diabetes, and cancer[1].

AKTide-2T TFA, serving as an optimal in vitro substrate for AKT, demonstrates competitive inhibition of histone H2B phosphorylation with a Ki value of 12 nM. It effectively mimics the optimal phosphorylation sequence of Akt and acts as an inhibitory peptide, distinct from the wildtype AKTide due to the absence of Thr at the S22 position [1].