synthase

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.

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].

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.

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

Ac-CoA Synthase Inhibitor1 (ACSS2 inhibitor) is the most potent and specific inhibitor of acetate-dependent acetyl-CoA synthetase 2 (ACSS2).

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

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.

FIN56, a specific inducer of ferroptosis, is identified by its IUPAC name [1,3,8-trihydroxy-6-methylanthracen-9(10H)-one].

PF-04802367 is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. It shows desirable central nervous system (CNS) properties and potency. It is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50 values of 10.0 and 9.0 nM in mobility shift assays, respectively.

5-Fluorouracil (5-FU) is a uracil analog and inhibitor of DNA synthesis, exhibiting antitumor activity by affecting pyrimidine synthesis through thymidylate synthase inhibition; it induces apoptosis and autophagy.

Rezafungin (SP-3025) is a broad-spectrum and long-lasting echinocandin with potent antifungal activity against Candida, Aspergillus and Pneumocystis.

Denifanstat (FASN-IN-2) is a fatty acid synthase (FASN) inhibitor (IC50=0.052 μM, EC50=0.072 μM) with selective and oral activity. Denifanstat has been used in studies of steatohepatitis.

TVB-3664 is an orally active, selective, reversible, and highly bioavailable fatty acid synthase inhibitor (FASN) with an IC50 for palmitate synthesis of 18 nM in human and 12 nM in mouse.Significantly inhibits microtubule protein palmitoylation and mRNA expression.

CHIR-99021 (CT99021) is an activator of the Wnt/β-catenin signaling pathway and a GSK-3α/β inhibitor (IC50=10/6.7 nM) with selective and oral activity.CHIR-99021 induces cellular autophagy, which enhances self-renewal in mouse and human embryonic stem cells.

5-O-Caffeoylshikimic acid shows anti-oxidative activity; it also shows anti-inflammatory activity, the underlying mechanism was associated with downregulation of nuclear factor-κB.

5-Iodo-indirubin-3'-monoxime is a potent inhibitor of GSK-3β, CDK5/P25, and CDK1/cyclin B, competing with ATP for binding to the catalytic site of the kinase (IC50s: 9, 20, and 25 nM).

ATB107 hydrochloride is a novel and potent inhibitor of indole-3-glycerol phosphate synthase (IGPS) with a KD of 3 μM.

BPH-1358 (NSC-50460) (NSC-50460) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor. With IC50s of 1.8 μM and 110 nM, respectively. And it is active against S. aureus in vitro (MIC ~250 ng/mL)[1][2].

FASN-in-1 is an effective, specific inhibitor of fatty acid synthase (FASN), a compound specifically designed to target and inhibit the activity of the enzyme involved in fatty acid synthesis, potentially disrupting fatty acid production and affecting various cellular processes.

GNF4877 is a potent inhibitor of DYRK1A and GSK3β (IC50s: 6 nM and 16 nM, respectively), resulting in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and increased β-cell proliferation.

Celiprolol hydrochloride (Selectrol) is a cardioselective beta-1 adrenergic antagonist that has intrinsic sympathomimetic activity. It is used in the management of ANGINA PECTORIS and HYPERTENSION.

RPR107393 free base is a selective and potent inhibitor of squalene synthase (SQS) for the study of neurological disorders and endocrine and metabolic disorders.

Terbogrel is an oral thromboxane A2 receptor antagonist (IC50 is about 10 nM) and thromboxane A2 synthase inhibitor (IC50 is about 10 nM). Terbogrel is an antiplatelet compound that inhibits platelet aggregation and is a potential compound for the prevention of blood clots.

NOS-IN-1 (2-Imino-4-methylpiperidine acetate) is a potent and orally active inhibitor of NO synthase (NOS) isoforms. NOS-IN-1 exhibits IC50s of 0.1 μM, 0.2 μM, and 1.1μM for human iNOS (hiNOS), hnNOS and heNOS, respectively.