substrate-competitive

K145 hydrochloride is a selective sphk2 inhibitor with substrate competitiveness and oral activity, with IC50 of 4.3 µM and Ki of 6.4 µM. K145 hydrochloride can induce apoptosis and has strong antitumor activity.

SU3327 (halicin) is a potent, selective and substrate-competitive inhibitor of JNK(IC50 of 0.7 μM).

CM-272 is a dual G9a/DNA methyltransferases (DNMTs) inhibitor.

MRT199665 is an effective and ATP-competitive, selective MARK/SIK/AMPK inhibitor (IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively). MRT199665 suppresses the phosphorylation of S

BMS-593214 is an active site-directed factor (F) VIIa inhibitor that exhibits antithrombotic and antihaemostatic properties. It acts as a direct competitive inhibitor of human FVIIa and a non-competitive inhibitor of FVIIa-activated substrate FX. Additionally, BMS-593214 effectively prevents electroinduced carotid artery thrombosis (AT) and wire-induced vena cava thrombosis (VT).

2'-O-Methylcytidine is a nucleoside derivative and an inhibitor of hepatitis C virus (HCV) non-structural protein 5B (NS5B; IC50= 3.8 μM).1It inhibits HCV replication in a replicon assay (IC50= 21.2 μM). 1.Migliaccio, G., Tomassini, J.E., Carroll, S.S., et al.Characterization of resistance to non-obligate chain-terminating ribonucleoside analogs that inhibit hepatitis C virus replication in vitroJ. Bio. Chem.278(49)49164-49170(2003)

SIRT5 inhibitor 5 is a selective and substrate-competitive SIRT5 inhibitor with an IC50 of 210 nM, which does not occupy the NAD+ binding pocket and can be used to study cancer and metabolism-related diseases.

SIRT5 inhibitor 7 (compound 58), a substrate-competitive and selective SIRT5 inhibitor with IC 50 = 310 nM, significantly attenuated renal dysfunction and pathological damage in lipopolysaccharide (LPS)- and cecum ligation/perforation (CLP)-induced septic AKI mice, and modulated proteinsuccinimidylation and proinflammatory cytokine release and pro-inflammatory cytokine release in the kidneys of acute kidney injury (AKI) mice.

SIRT5 inhibitor 8 (compound 10) is a moderately selective and substrate-competitive SIRT5 inhibitor with IC50=5.38 μM, with potential anticancer effects.

SIRT5 inhibitor 9 (compound 14) is a moderately selective and substrate-competitive SIRT5 inhibitor with IC50=4.07 μM and has potential anticancer effects.

6-Phosphogluconic acid is a potent and competitive inhibitor of phosphoglucose isomerase (PGI), with an apparent Ki of 0.048 mM for glucose 6-phosphate and 0.042 mM for fructose 6-phosphate as the substrate.

CBB1007 Hcl is a selective, reversible, and substrate competitive LSD1 inhibitor (IC50: 5.27 μM for hLSD1).

CBB1007 is a potent, reversible, and substrate competitive LSD1 inhibitor (IC50: 5.27 μM for hLSD1).

CBB1007 trihydrochloride is a selective, reversible, and substrate competitive LSD1 inhibitor (IC50: 5.27 μM for hLSD1).

GDP-α-D-mannose disodium gives a competitive inhibition with respect to GTP (Ki 14.7 μM) and an uncompetitive inhibition with respect to mannose-1-P (Ki 115 μM).GDP-α-D-mannose disodium is the donor substrate for mannosyltransferases and the precursor of

K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity. K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM.

PI-273, a Substrate-Competitive, Specific Small-Molecule Inhibitor of PI4KIIα, Inhibits the Growth of Breast Cancer Cells

BAY-707, a highly potent and selective substrate-competitive inhibitor of MTH1 (NUDT1) with an IC50 of 2.3 nM, is well-tolerated in mice and exhibits a favorable pharmacokinetic (PK) profile compared to other MTH1 compounds. However, it demonstrates a clear lack of anticancer efficacy both in vitro and in vivo[1].

UNC0379 is a selective, substrate-competitive inhibitor of the lysine methyltransferase (SETD8).

Ac-EVKKQR-pNA is a competitive chromogenic substrate targeting the P6-P1 segment at the NS2B-NS3 cleavage site's N-terminal, featuring a highly reactive, hydrolyzable para-nitroaniline (pNA) at the P1 position. This compound holds promise for research into Dengue virus type 2 and Yellow fever virus infections.

2'-Deoxy-NAD+ sodium is the sodium salt form of 2'-Deoxy-NAD+. It acts as a non-competitive inhibitor of NAD+ with a Ki of 32 μM. Additionally, '2'-Deoxy-NAD+ sodium can be utilized as a substrate for studying ADP-ribosyltransferase reactions.

II399 is a potent and selective dual-substrate inhibitor of NNMT, featuring an unconventional SAM mimic, with a Ki value of 5.9 nM. It exhibits a notable competitive inhibition pattern against NAM and can occupy both the substrate and cofactor binding pockets. II399 shows promise for research in cancer, metabolic, cardiovascular, and neurodegenerative diseases.

5'-dCMPS is an analogue of 5'-dCMP and can act as a potential substrate, competitive inhibitor, or modulator for enzymes interacting with 5'-dCMP.

7-Deazaadenosine 5'-phosphate (Tubercidin 5'-phosphate; 7-Deaza-AMP) is a potential substrate and competitive inhibitor of enzymes that interact with 5′-adenosine monophosphate. As a nucleotide derivative, 7-Deazaadenosine 5'-phosphate modulates cellular functions by influencing intracellular signaling pathways, particularly those involving AMP.