Search Result

Results for "115 mobile Inhibitors" in MCE Product Catalog:

By Targets:	ADC Cytotoxin (1) Adenosine Receptor (1) Adrenergic Receptor (1) Amyloid-β (3) Antibiotic (1) Antifolate (1) Apoptosis (3) Autophagy (3) Bacterial (4) Bcr-Abl (1) c-Met/HGFR (2) CaMK (1) Casein Kinase (1) CMV (1) COX (1) DNA Methyltransferase (1) DNA-PK (2) Drug Metabolite (1) DYRK (2) E1/E2/E3 Enzyme (1) Endogenous Metabolite (1) Ephrin Receptor (1) Epigenetic Reader Domain (1) Factor Xa (1) GLUT (1) GPCR19 (1) HIV (1) Isocitrate Dehydrogenase (IDH) (1) mAChR (1) MDM-2/p53 (1) Microtubule/Tubulin (1) MMP (1) mTOR (2) NADPH Oxidase (2) Notch (1) Opioid Receptor (2) p38 MAPK (1) p97 (1) PARP (1) Phosphatase (1) Phosphodiesterase (PDE) (2) PI3K (1) PKA (1) PKC (1) PROTAC (1) Reverse Transcriptase (1) ROCK (2) SARS-CoV (1) Sirtuin (1) Sodium Channel (1) Thrombin (1) Tyrosinase (1) VEGFR (2) Virus Protease (1) γ-secretase (1)
By Research Areas:	Cancer (20) Cardiovascular Disease (7) Endocrinology (2) Infection (7) Inflammation/Immunology (5) Metabolic Disease (3) Neurological Disease (7)

By Targets:

ADC Cytotoxin (1)

Adenosine Receptor (1)

Adrenergic Receptor (1)

Amyloid-β (3)

Antibiotic (1)

Antifolate (1)

Apoptosis (3)

Autophagy (3)

Bacterial (4)

Bcr-Abl (1)

c-Met/HGFR (2)

CaMK (1)

Casein Kinase (1)

CMV (1)

COX (1)

DNA Methyltransferase (1)

DNA-PK (2)

Drug Metabolite (1)

DYRK (2)

E1/E2/E3 Enzyme (1)

Endogenous Metabolite (1)

Ephrin Receptor (1)

Epigenetic Reader Domain (1)

Factor Xa (1)

GLUT (1)

GPCR19 (1)

HIV (1)

Isocitrate Dehydrogenase (IDH) (1)

mAChR (1)

MDM-2/p53 (1)

Microtubule/Tubulin (1)

MMP (1)

mTOR (2)

NADPH Oxidase (2)

Notch (1)

Opioid Receptor (2)

p38 MAPK (1)

p97 (1)

PARP (1)

Phosphatase (1)

Phosphodiesterase (PDE) (2)

PI3K (1)

PKA (1)

PKC (1)

PROTAC (1)

Reverse Transcriptase (1)

ROCK (2)

SARS-CoV (1)

Sirtuin (1)

Sodium Channel (1)

Thrombin (1)

Tyrosinase (1)

VEGFR (2)

Virus Protease (1)

γ-secretase (1)

By Research Areas:

Cancer (20)

Cardiovascular Disease (7)

Endocrinology (2)

Infection (7)

Inflammation/Immunology (5)

Metabolic Disease (3)

Neurological Disease (7)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Recombinant Proteins

Cat. No.	Product Name	Target	Research Areas

HY-101518

APG-115 AA-115	MDM-2/p53 E1/E2/E3 Enzyme Apoptosis	Cancer
APG-115 (AA-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC₅₀ and K_i values of 3.8 nM and 1 nM, respectively. APG-115 blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner.

HY-111534

SBI-115
GPCR19 Others

SBI-115 is a TGR5 (GPCR19) antagonist. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5.
HY-16962

CC-115
DNA-PK mTOR Cancer

CC-115 is a potent and dual DNA-PK and mTOR kinase inhibitor with IC₅₀s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.

SBI-115	GPCR19	Others
SBI-115 is a TGR5 (GPCR19) antagonist. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5.

CC-115	DNA-PK mTOR	Cancer
CC-115 is a potent and dual DNA-PK and mTOR kinase inhibitor with IC₅₀s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.

HY-16962A

*CC-115* hydrochloride**	DNA-PK mTOR	Cancer
CC-115 hydrochloride is a potent and dual DNA-PK and mTOR kinase inhibitor with IC₅₀s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.

HY-12423A

*TAS-115* mesylate** TAS-115 methanesulfonate	VEGFR c-Met/HGFR	Cancer
TAS-115 mesylate is a potent VEGFRand hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor, with IC₅₀s of 30 and 32 nM for rVEGFR2 and rMET, respectively.

HY-12423

TAS-115	VEGFR c-Met/HGFR	Cancer
TAS-115 is a potent VEGFR and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor with IC₅₀s of 30 and 32 nM for rVEGFR2 and rMET, respectively.

HY-15685

Ripasudil
K-115
ROCK Neurological Disease

Ripasudil (K-115) is a specific inhibitor of ROCK, with IC₅₀s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
HY-B0204

Pimobendan
UD-CG115
Phosphodiesterase (PDE) Cardiovascular Disease

Pimobendan (UD-CG115) is a selective inhibitor of PDE3 with IC₅₀ of 0.32 μM.

Ripasudil K-115	ROCK	Neurological Disease
Ripasudil (K-115) is a specific inhibitor of ROCK, with IC₅₀s of 19 and 51 nM for ROCK2 and ROCK1, respectively.

Pimobendan UD-CG115	Phosphodiesterase (PDE)	Cardiovascular Disease
Pimobendan (UD-CG115) is a selective inhibitor of PDE3 with IC₅₀ of 0.32 μM.

HY-120801

APX-115 Ewha-18278	NADPH Oxidase	Metabolic Disease Inflammation/Immunology
APX-115 (Ewha-18278) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with K_i values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 effectively prevents kidney injury.

HY-B0204A

Pimobendan hydrochloride UD-CG115 hydrochloride	Phosphodiesterase (PDE)	Cardiovascular Disease
Pimobendan hydrochloride (UD-CG115 hydrochloride) is a selective inhibitor of PDE3 with IC₅₀ of 0.32 μM.

HY-10995

Tozadenant
SYN115
Adenosine Receptor Neurological Disease

Tozadenant is an adenosine A_2A receptor antagonist, with K_i of 11.5 nM on human A_2A and 6 nM on rhesus A_2A.

Tozadenant SYN115	Adenosine Receptor	Neurological Disease
Tozadenant is an adenosine A_2A receptor antagonist, with K_i of 11.5 nM on human A_2A and 6 nM on rhesus A_2A.

HY-15685A

Ripasudil free base K-115 (free base)	ROCK	Neurological Disease
Ripasudil free base (K-115 free base) is a specific inhibitor of ROCK, with IC₅₀s of 19 and 51 nM for ROCK2 and ROCK1, respectively.

HY-120801A

*APX-115* free base** Ewha-18278 free base	NADPH Oxidase	Endocrinology Inflammation/Immunology
APX-115 free base (Ewha-18278 free base) is a potent, orally active pan NADPH oxidase (Nox) inhibitor with K_i values of 1.08 μM, 0.57 μM, and 0.63 μM for Nox1, Nox2 and Nox4, respectively. APX-115 free base effectively prevents kidney injury.

HY-P1046

β-Amyloid 1-15 Amyloid β-Protein (1-15)	Amyloid-β	Neurological Disease
β-Amyloid (1-15) is a fragment of β-Amyloid peptide. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.

HY-10111

TG100-115
PI3K Cardiovascular Disease Cancer

TG100-115 is a selective PI3Kγ/PI3Kδ inhibitor with IC₅₀s of 83 and 235 nM, respectively.

TG100-115	PI3K	Cardiovascular Disease Cancer
TG100-115 is a selective PI3Kγ/PI3Kδ inhibitor with IC₅₀s of 83 and 235 nM, respectively.

HY-117071

Dabuzalgron Ro 115-1240	Adrenergic Receptor	Endocrinology Cardiovascular Disease
Dabuzalgron (Ro 115-1240) is an orally active and selective α-1A adrenergic receptor agonist for the treatment of urinary incontinence. Dabuzalgron protects against Doxorubicin-induced cardiotoxicity by preserving mitochondrial function.

HY-U00439

Protein kinase inhibitors 1
DYRK Cancer

Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC₅₀ of 74 nM and K_d of 9.5 nM.
HY-119173

PBD-150
Amyloid-β Neurological Disease

PBD-150 is a human glutaminyl cyclase (hQC) Y115E-Y117E variant inhibitor, with a K_i value of 490 nM.
HY-102035

PARP-2-IN-1
PARP Cancer

PARP-2-IN-1 is a potent and selective PARP-2 inhibitor with an IC₅₀ of 11.5 nM.

*Protein kinase inhibitors* 1**	DYRK	Cancer
Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC₅₀ of 74 nM and K_d of 9.5 nM.

PBD-150	Amyloid-β	Neurological Disease
PBD-150 is a human glutaminyl cyclase (hQC) Y115E-Y117E variant inhibitor, with a K_i value of 490 nM.

PARP-2-IN-1	PARP	Cancer
PARP-2-IN-1 is a potent and selective PARP-2 inhibitor with an IC₅₀ of 11.5 nM.

HY-B1902

Diaveridine EGIS-5645	Antifolate Bacterial	Infection
Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a K_i of 11.5 nM for the wild type DHFR and also an antibacterial agent.

HY-131005

Ehp inhibitor 2
Ephrin Receptor Cancer

Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.

Ehp inhibitor 2	Ephrin Receptor	Cancer
Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.

HY-N7054

Volemitol D-Volemitol	Others	Metabolic Disease
Volemitol (D-Volemitol) is a seven-carbon sugar alcohol that fulfills several important physiological functions in certain species of the genus Primula. Volemitol is the major nonstructural carbohydrate in leaves of all stages of development. Volemitol functions as a photosynthetic product, phloem translocate (phloem-mobile), and storage carbohydrate. Volemitol biosynthesis proceeds by a novel, NADPH-dependent, ketose reductase (sedoheptulose reductase).

HY-121879

SHP836
Phosphatase Cancer

SHP836 is a SHP2 allosteric inhibitor, with an IC₅₀ of 12 μM for the full length SHP2.

SHP836	Phosphatase	Cancer
SHP836 is a SHP2 allosteric inhibitor, with an IC₅₀ of 12 μM for the full length SHP2.

HY-N1750

3-(2,4-Dihydroxyphenyl)propanoic acid	Tyrosinase	Others
3-(2,4-Dihydroxyphenyl)propanoic acid (DPPacid) is a potent and competitive tyrosinase inhibitor, inhibits L-Tyrosine and DL-DOPA with an IC₅₀ and a K_i of 3.02 μM and 11.5 μM, respectively.

HY-19373

RWJ-445167 3DP-10017	Thrombin Factor Xa	Cardiovascular Disease
RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with K_i of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.

HY-16787

ICA-121431	Sodium Channel	Cardiovascular Disease
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Na_v) blocker, shows equipotent selectivity for human Na_v1.1 and Na_v1.3 subtypes with IC₅₀ values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Na_v1.2 (IC₅₀=240 nM) and 1,000 fold selectivity against Na_v1.4, Na_v1.6, and the TTX-resistant human Na_v1.5 and Na_v1.8 channels (IC₅₀s >10 µM).

HY-U00439A

*Protein kinase inhibitors* 1 hydrochloride** (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride	DYRK	Cancer
Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC₅₀s of 136 and 74 nM for HIPK1 and HIPK2, and a K_d of 9.5 nM for HIPK2.

HY-114200

Imrecoxib BAP-909	COX	Inflammation/Immunology
Imrecoxib (BAP-909) is a novel and selective cyclooxygenase 2 (COX-2) inhibitor with an IC₅₀ value of 18 nM, it also inhibits COX1- activity with an IC₅₀ value of 115 nM. Imrecoxib (BAP-909) has anti-inflammatory effect.

HY-W012037

8-Hydroxyquinoline hemisulfate 8-Quinolinol hemisulfate	Bacterial Antibiotic	Infection
8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.

HY-N7389B

GDP-α-D-mannose disodium	Endogenous Metabolite	Metabolic Disease
GDP-α-D-mannose disodium is the donor substrate for mannosyltransferases and the precursor of GDP-β-L-fucose. GDP-α-D-mannose disodium gives a competitive inhibition with respect to GTP (K_i 14.7 μM) and an uncompetitive inhibition with respect to mannose-1-P (K_i 115 μM).

HY-135813

LtaS-IN-1	Bacterial	Infection
LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.

HY-125957

A-3 hydrochloride	PKA Casein Kinase CaMK PKC	Others
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (K_i=4.3 µM), casein kinase II (K_i=5.1 µM) and myosin light chain kinase (MLCK) (K_i=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with K_i values of 47 µM and 80 µM, respectively.

HY-136199

SIRT1-IN-1	Sirtuin CMV	Infection
SIRT1-IN-1 is a selective SIRT1 inhibitor with an IC₅₀ of 0.205 μM. SIRT1-IN-1 inhibits SIRT2 with an IC₅₀ of 11.5 μM. SIRT1-IN-1, a indole, is a cytomegalovirus (CMV) inhibitors and has antiviral activity.

HY-15945

DBeQ JRF 12	p97 Autophagy Apoptosis	Cancer
DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC₅₀ value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC₅₀ of 11.5 μM.

HY-13642

RG108 N-Phthalyl-L-tryptophan	DNA Methyltransferase	Cancer
RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC₅₀=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences.

HY-124819

D13-9001	Bacterial	Infection
D13-9001 is a potent AcrB (AcrAB-TolC efflux pump subunit) and MexB (MexAB-OprM efflux pump subunit) inhibitor with the K_D values of 1.15 μM and 3.57 μM in E. coli and P. aeruginosa, respectively. D13-9001 exhibits antibiotic activities.

HY-G0021

N-Desmethylclozapine Norclozapine; Desmethylclozapine; Normethylclozapine	mAChR Opioid Receptor Drug Metabolite Virus Protease	Infection
N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic drug Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC₅₀=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist.

HY-101918

DS-1040 Tosylate	Others	Cardiovascular Disease
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC₅₀s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.

HY-18728

STF-31
GLUT Autophagy Cancer

STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC₅₀ of 1μM^[1][2].

STF-31	GLUT Autophagy	Cancer
STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC₅₀ of 1μM^[1][2].

HY-15583

Auristatin F	Microtubule/Tubulin ADC Cytotoxin	Cancer
Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).

HY-13027

DAPT GSI-IX	γ-secretase Amyloid-β Autophagy Notch Apoptosis	Cancer Inflammation/Immunology Neurological Disease
DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC₅₀s of 115 nM and 200 nM for total amyloid-β (Aβ) and Aβ₄₂, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment.

HY-107425

MZ 1	PROTAC Epigenetic Reader Domain	Cancer
MZ 1 is a PROTAC BRD4 degrader. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2 and BRD3. K_ds of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively.

HY-19627

Naldemedine S-297995	Opioid Receptor	Neurological Disease
Naldemedine (S-297995) is an orally active, peripherally acting µ-opioid receptor antagonist. Naldemedine shows potent binding affinities (IC₅₀s = 1.15, 1.11, and 1.5 nM, repectively) and antagonist activities (IC₅₀s= 25.57, 7.09, 16.1 nM, repectively) for recombinant human μ-, δ-, and κ- opioid receptors. Naldemedine tempers opioid-induced constipation (OIC) without compromising opioid analgesia.

HY-122470

Stampidine	Reverse Transcriptase HIV	Infection
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLV_IIIB (B-envelope subtype) and primary clinical isolates with IC₅₀s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC₅₀s of 8.7 nM and 11.2 nM, respectively.

HY-11007

GNF-2
Bcr-Abl SARS-CoV Cancer

GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC₅₀ of 138 nM .

GNF-2	Bcr-Abl SARS-CoV	Cancer
GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC₅₀ of 138 nM .

HY-131312

Mutant IDH1-IN-6	Isocitrate Dehydrogenase (IDH)	Cancer
Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC₅₀s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes.

HY-122872

MKK7-COV-9	p38 MAPK	Cancer
MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC₅₀ of 4.98 μM.

HY-120944

BAY-7598	MMP	Inflammation/Immunology
BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC₅₀s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.

Cat. No.	Product Name

HY-L0051V

HTS Compound Library	2,115,979 compounds
A unique collection contains 2,115,979 diverse screening compounds for the lead identification via high-throughput screening (HTS) and high content screening (HCS).

Cat. No.	Product Name	Target	Research Area

HY-P1598

GroES mobile loop
Peptides Others

GroES mobile loop is a highly flexible region of free GroES, which binds to GroEL through the residues at the tip of the loop.