polyketide synthase 13-in-1

Polyketide synthase 13-IN-1 (compound 32) is an inhibitor of polyketide synthase 13.

GnRH Associated Peptide (GAP) (1-13), human Acetate was found to be a potent inhibitor of prolactin secretion and to stimulate the release of gonadotropins. Active immunization with peptides corresponding to GAP sequences led to greatly increased prolacti

Dynorphin B (1-13) acetate acts as an agonist on opioid κ-receptor.

Porcine dynorphin A(1-13) acetate (Dynorphin A Porcine Fragment 1-13 acetate) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations. Exposure to dynorphin A (1-13) causes acute increases in [Ca2+]i in individual neurons similar to increases seen with acute NMDA treatment.

Apelin-13 triTFA is the endogenous ligand of the APJ receptor, activating this G protein-coupled receptor with an EC50 value of 0.37 nM.

[(pF)Phe4]Nociceptin(1-13)NH2 acetate is a selective agonist of NOP receptor with a pKi of 10.68 and a pEC50 of 9.31. [(pF)Phe4]Nociceptin(1-13)NH2 acetate displays high selectivity over δ, κ, and μ opioid receptors (>3000 fold).

Nociceptin (1-13), amide is a potent agonist Opioid receptor-like1 (ORL1) receptor with a pEC50 of 7.9 for mouse vas deferens and a Ki of 0.75 nM for binding to rat forebrain membranes.

ATP synthase inhibitor 1 is an inhibitor of the c subunit of the F1/FO-ATP synthase complex. It inhibits mitochondrial permeability transition pore (mPTP) opening and does not affect ATP levels.

Polyketide synthase 13-IN-2 (comp 42) is a potent inhibitor of polyketide synthase 13 in Mycobacterium tuberculosis, demonstrating a minimum inhibitory concentration (MIC) of 0.25 μg mL [1].

1, 14-tetradecanedioic-2, 2, 13, 13-d4 acid is a deuterated compound of 1, 14-tetradecanedioic acid. 1, 14-tetradecanedioic acid has a CAS number of 821-38-5. Tetradecanedioic acid is a C14 dicarboxylic acid.

13-Acetoxy-3beta-hydroxygermacra-1(10)E,4E,7(11)-trien-12,6alpha-olide is a natural product from Artemisia myriantha.

Chitin Synthase Inhibitor 13 (compound 12g), a non-competitive antagonist of chitin synthase, demonstrates broad-spectrum antifungal activity and has an inhibition concentration (IC50) of 106.7 μM [1].

Enpp-1-IN-13 is an ectonucleotide pyrophosphatase/phosphodiesterase (ENPP) inhibitor that is able to act on ENPP1 (IC50: 1.29 μM) and ENPP3 (IC50: 20.2 μM), exhibiting anticancer effects.

[DAla2, DArg6] Dynorphin A, (1-13) (porcine) (DADAD), a derivative of dynorphin1-13 (DYN) extracted from porcine pituitary, exhibits high potency at peripheral opioid receptors GPI and MVD. Despite the rapid in vivo degradation of DYN, this compound shows increased resistance to enzymatic cleavage, enhancing its stability against peptide-degrading enzymes [1].

[Glycogen Synthase (1-12) Ala9,10, Lys11,12] is a selective substrate for protein kinase C (PKC) phosphorylation. It serves to assess PKC activity [1].

Apelin-13 is an endogenous ligand of APJ receptor, and the EC 50 value of activated G protein coupled receptor is 0.37 nM.

Galanin (1-13)-Neuropeptide Y (25-36) amide exhibits high-affinity binding to galanin receptors, comparable to that of galanin itself [1].

[Nphe1]Nociceptin(1-13)NH2 is a novel endogenous ligand for the nociceptin/orphanin FQ (NC) receptor, acting as a selective and competitive antagonist without any agonist effects. It binds specifically to recombinant nociceptin receptors with high affinity (pKi=8.4) and effectively blocks nociceptin's ability to inhibit cyclic AMP accumulation in CHO cells (pA2=6.0), showcasing potential as an analgesic agent.

Mtb ATP synthase-IN-1 (compound 6ab) is a potent inhibitor of Mycobacterium tuberculosis (Mtb) ATP synthase (MIC = 0.452-0.499 μg mL) [1] that can be used in anti-mycobacterium research, showing low cytotoxicity (Vero IC 50 > 64 μg mL) and acceptable oral bioavailability with good metabolic stability.

Dynorphin B (1-13) TFA, an agonist of the opioid κ-receptor.

Porcine dynorphin A (1-13), a potent endogenous κ opioid receptor agonist, exhibits antinociceptive properties at physiological concentrations and induces acute increases in [Ca2+]i in neurons, akin to those observed with acute NMDA treatment.

Dynorphin A (1-13) amide, an endogenous opioid peptide, counteracts the analgesic effects of morphine [1].

8alpha-(2-Methylacryloyloxy)-1-O-methylhirsutinolide 13-O-acetate is a natural product for research related to life sciences. The catalog number is TN3293 and the CAS number is 883872-71-7.

Mcl-1 Inhibitor 13 (Example 9), with a Ki of 8.2 nM, serves as an MCL-1 inhibitor suitable for cancer research [1].

Compound (S)-9, a GLP-1 receptor agonist, exhibits an EC50 of 76 nM for the glucagon GLP-1 receptor [1].

Dihydropteroate synthase-IN-1 (compound 5g) is a potent inhibitor of dihydropteroate synthase (DHPS) and cytochrome P450, and can be used as a diagnostic radiographic material.

Highly potent and selective nociceptin/orphanin FQ receptor (OP4) agonist peptide (pKi = 10.68; pEC50 = 9.80). Displays > 8000-fold selectivity over δ, κ, and μ opioid receptors and has relatively long lasting pronociceptive, hypotensive, negative inotrop

Dynorphin B (1-13) acts as an agonist on the opioid κ-receptor.

Squalene synthase-IN-1 (compound 1) is a potent antihyperlipidemic agent that inhibits Squalene Synthase, demonstrating exceptional antioxidant and anti-inflammatory activities. It significantly reduces glucose and oxidative stress levels without causing toxicity [1].

Parathyroid hormone (PTH) (1-13) is an N-terminal fragment of PTH (1-34) . In vivo, PTH (1-13) (0.003-1 μmol/kg) increases mean arterial pressure (MAP) in anesthetized rats.

Prostaglandin G H synthase 1 inhibitor (CP 74006) is a selective D5D inhibitor with an IC(50) value of 20 nM.

HIV-1 inhibitor-13 is an orally active HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) with an IC50 value of 0.14 μM against HIV-1 RT. HIV-1 inhibitor-13 is active against HIV-1 resistant strains (EC50: 2.85-18.0 nM).

GlcN-6-P Synthase-IN-1 (Compound 4d) is a potent inhibitor of Glucosamine-6-phosphate (GlcN-6-P) synthase with an IC50 of 3.47 μM. This compound exhibits remarkable antimicrobial activity, excellent central nervous system penetration, and inhibits cytochrome P450, specifically the CYP3A4 isoform [1].

This peptide is a fragment of the alpha-chain of insulin amino acids 1 to 13. The insulin a-chain epitope recognized by human T cells is posttranslationally modified.

PD-1/PD-L1-IN-13 is a potent immune checkpoint PD-1/PD-L1 inhibitor with an IC50 value of 10.2 nM for PD-1/PD- L1 interaction.PD-1/PD-L1-IN-13 promotes CD8+ T-cell activation and delays tumour growth in a Hepa1-6 homozygous mouse model.

Polyketide synthase 13-IN-3 (compound 41) is a potent inhibitor of polyketide synthase 13, with a minimum inhibitory concentration (MIC) range of 0.0625-0.125 μg mL against the M. tuberculosis strain H37Rv.

Chitin synthase inhibitor 1 is a potent and selective chitin synthase (CHS) inhibitor with an IC50 of 0.12 mM, effectively inhibiting drug-resistant fungi variants.

PROTAC CDK12 13 Degrader-1 (7f) is a potent and selective dual degrader of the cell cycle protein-dependent kinases CDK12 (DC50: 2.2 nM) and CDK13 (DC50: 2.1 nM), used in the context of breast cancer.

S.pombe lumazine synthase-IN-1 is a compound that inhibits lumazine synthases, with Ki values of 243 μM for Schizosaccharomyces pombe and 9.6 μM for Mycobacterium tuberculosis, respectively[1].

Nociceptin (1-13), amide TFA, a potent ORL1 receptor (opioid receptor-like 1 receptor, OP4) agonist, exhibits a pEC50 of 7.9 in mouse vas deferens and a Ki of 0.75 nM for rat forebrain membrane binding [1] [2].

Nociceptin (1-13), amide is a potent ORL1 (OP4) receptor agonist, exhibiting a pEC50 of 7.9 in mouse vas deferens and a Ki of 0.75 nM for rat forebrain membrane binding.

Cortistatin-29 (1-13) is a neuropeptide and cleavage product of cortistatin-29 , which is a cleavage product of procortistatin. Cortistatin-29 (1-13) corresponds to the first 13 amino acids of cortistatin-29.

1-Palmitoyl-2-13(S)-HpODE-sn-glycero-3-PC is a phospholipid featuring palmitic acid at the sn-1 position and 13(S)-HpODE at the sn-2 position.

Potent agonist of the nociceptin (ORL1) receptor, demonstrated both in vitro and in vivo. Selective, competitive antagonism at the nociceptin receptor has also been reported (pA2 = 7.02 and 6.75 in the guinea pig ileum and mouse vas deferens respectively)

Glucosylceramide synthase-IN-1 (T-036) is a potent, orally active, blood-brain barrier permeable glucosylceramide synthase (GCS) inhibitor, acting on human GCS (IC50: 31 nM) and mouse GCS (IC50: 51 nM), and can be used to study Gaucher disease.

PARP-1-IN-13 (Compound 19c) is a potent PARP-1 inhibitor with an IC50 of 26 nM, hindering DNA single-strand break repair and exacerbating double-strand breaks, leading to apoptosis in cancer cells via the mitochondrial pathway [1].

[DAla2] Dynorphin A (1-13), amide (porcine) is a peptide that potentially acts as a κ opioid receptor agonist, used in nervous system research [1].