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Results for "

substrate-competitive

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Amyloid-β (1) Apoptosis (4) DNA Methyltransferase (1) DNA/RNA Synthesis (1) GSK-3 (2) Histone Demethylase (3) Histone Methyltransferase (7) JNK (2) Mitophagy (1) PARP (1) Sirtuin (3) SphK (2)
By Research Areas:	Cancer (17) Inflammation/Immunology (5) Metabolic Disease (2) Neurological Disease (2)

Inhibitors & Agonists

Peptides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-122661

Mefuparib hydrochloride MPH	PARP Apoptosis	Cancer
Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC₅₀s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo .

HY-114209

MRK-740	Histone Methyltransferase	Cancer
MRK-740 is a potent, selective and substrate-competitive PRDM9 histone methyltransferase inhibitor with an IC₅₀ of 80 nM. MRK-740 is more selective for PRDM9 than other histone methyltransferases and other non-epigenetic targets. MRK-740 reduces PRDM9-dependent trimethylation of H3K4 (IC₅₀ = 0.8 µM) .

HY-15779A

K145 hydrochloride Maximum Cited Publications 6 Publications Verification	SphK Apoptosis	Cancer
K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC₅₀ of 4.3 µM and a K_i of 6.4 µM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity .

HY-107597

Halicin 1 Publications Verification SU3327	JNK	Metabolic Disease Inflammation/Immunology
Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC₅₀ of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC₅₀ of 239 nM. Halicin shows less active against p38α and Akt kinase .

HY-15779

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

HY-112080

BAY-6035	Histone Methyltransferase	Cancer
BAY-6035 is a potent, selective and substrate-competitive inhibitor of SMYD3. BAY-6035 inhibits methylation of MEKK2 peptide with an IC₅₀ of 88 nM .

HY-101925

CM-272 1 Publications Verification	Histone Methyltransferase DNA Methyltransferase Apoptosis	Cancer
CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC₅₀s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death .

HY-152214

SIRT5 inhibitor 5	Sirtuin	Cancer
SIRT5 inhibitor 5 is a potent SIRT5 inhibitor with an IC₅₀ value of 0.21 µM. SIRT5 inhibitor 5 does not occupy the NNAD ⁺ -binding pocket and acts as a substrate-competitive inhibitor .

HY-149425

SIRT5 inhibitor 6	Sirtuin	Inflammation/Immunology Cancer
SIRT5 Inhibitor 6 is a potent, substrate-competitive and selective SIRT5 inhibitor with an IC₅₀ of 3.0 μM. SIRT5 Inhibitor6 has a therapeutic potential against septic AKI in vivo .

HY-12335

UNC0379 5 Publications Verification	Histone Methyltransferase	Inflammation/Immunology Cancer
UNC0379 is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC₅₀ of 7.3 μM, K_D value of 18.3 μM. UNC0379 can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma .

HY-12335A

UNC0379 TFA	Histone Methyltransferase	Inflammation/Immunology Cancer
UNC0379 TFA is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC₅₀ of 7.3 μM, K_D value of 18.3 μM. UNC0379 TFA can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma .

HY-112081

BAY-707	DNA/RNA Synthesis	Cancer
BAY-707 is a substrate-competitive, highly potent and selective inhibitor of MTH1(NUDT1) with an IC₅₀ of 2.3 nM. BAY-707 has a good pharmacokinetic (PK) profile to other MTH1 compounds and is well-tolerated in mice, but shows a clear lack of in vitro or in vivo anticancer efficacy .

HY-P1173

L803-mts Myristoylated L 803; GSK-3β Inhibitor XIII	GSK-3 Amyloid-β	Neurological Disease
L803-mts (Myristoylated L 803) is a selective and substrate-competitive GSK-3 peptide inhibitor (IC₅₀: 40 μM). L803-mts also reduces Aβ deposits and ameliorates cognitive deficits in 5XFAD mice. L803-mts shows antidepressive effect in the forced swimming test .

HY-100201

A-196 4 Publications Verification	Histone Methyltransferase	Cancer
A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC₅₀ values of 25 nM and 144 nM, respectively. A-196 inhibits SUV4-20 biochemically in a substrate-competitive manner. A-196 represents a first-in-class chemical probe of SUV4-20 to investigate the role of histone methyltransferases in genomic integrity .

HY-149426

SIRT5 inhibitor 7	Sirtuin	Inflammation/Immunology
SIRT5 inhibitor 7 (compound 58) is a substrate-competitive and selective SIRT5 inhibitor with anti-inflammatory activity. SIRT5 inhibitor 7 has renal protective effects and regulates protein succinylation and the release of pro-inflammatory cytokines. SIRT5 inhibitor 7 has in vivo activity in AKI mouse models of lipopolysaccharide (LPS) and cecal ligation/perforation (CLP)-induced sepsis-related acute kidney injury .

HY-110196

(S)-PFI-2 hydrochloride	Others	Others
(S)-PFI-2 hydrochloride is an inhibitor of lysine methyltransferase SETD7 and is approximately 500-fold more active than its enantiomer (R)-PFI-2. (R)-PFI-2 is a cofactor-dependent and substrate-competitive inhibitor. (R)-PFI-2 can occupy the substrate peptide binding groove of SETD7 (including the catalytic lysine binding channel) and interact with the cofactor The donor methyl group is in direct contact. However, (S)-PFI-2 was not observed to have the same interaction as (R)-PFI-2 .

HY-10366

BI-78D3

1 Publications Verification

JNK Metabolic Disease Cancer

BI-78D3 functions as a substrate competitive inhibitor of JNK, inhibit the JNK kinase activity (IC₅₀=280 nM).

BI-78D3 1 Publications Verification	JNK	Metabolic Disease Cancer
BI-78D3 functions as a substrate competitive inhibitor of JNK, inhibit the JNK kinase activity (IC₅₀=280 nM).

HY-15313

CBB1007	Histone Demethylase	Cancer
CBB1007 is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).

HY-15313B

CBB1007 hydrochloride	Histone Demethylase	Cancer
CBB1007 Hcl is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).

HY-15313C

CBB1007 trihydrochloride 1 Publications Verification	Histone Demethylase	Cancer
CBB1007 trihydrochloride is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).

HY-153089

GSK3-IN-3 1 Publications Verification	GSK-3 Mitophagy	Neurological Disease
GSK3-IN-3 is a mitophagy inducer, inducing Parkin-dependent mitophagy. GSK3-IN-3 is also a GSK-3 inhibitor with an IC₅₀ value of 3.01 μM. GSK3-IN-3 is non-ATP nor substrate competitive and is neuroprotective against 6-OHDA .

HY-134828

AZ506 1 Publications Verification	Histone Methyltransferase	Cancer
AZ506 is a potent SMYD2 inhibitor with an IC₅₀ of 17 nM. AZ506 inhibits SMYD2 methyltransferase activity in cells, leading to a decrease in the SMYD2-mediated methylation signal .

L803-mts Myristoylated L 803; GSK-3β Inhibitor XIII	GSK-3 Amyloid-β	Neurological Disease
L803-mts (Myristoylated L 803) is a selective and substrate-competitive GSK-3 peptide inhibitor (IC₅₀: 40 μM). L803-mts also reduces Aβ deposits and ameliorates cognitive deficits in 5XFAD mice. L803-mts shows antidepressive effect in the forced swimming test .

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