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Results for "

greater selectivity

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (3) Akt (1) Apoptosis (4) Autophagy (1) Btk (1) c-Met/HGFR (2) Cannabinoid Receptor (3) Casein Kinase (2) CDK (2) Dipeptidyl Peptidase (3) DYRK (1) EGFR (1) Epigenetic Reader Domain (1) Factor Xa (1) Ferroptosis (3) HDAC (2) iGluR (1) IKK (1) Isocitrate Dehydrogenase (IDH) (1) Isotope-Labeled Compounds (3) Itk (1) JAK (2) Melatonin Receptor (2) MMP (1) Monoamine Oxidase (3) p38 MAPK (1) Phosphatase (2) PI3K (1) PI4K (1) Potassium Channel (2) PPAR (1) Raf (2) Ribosomal S6 Kinase (RSK) (1) TAM Receptor (1) TNF Receptor (1) Topoisomerase (1) γ-secretase (1)
By Research Areas:	Cancer (18) Cardiovascular Disease (6) Endocrinology (3) Inflammation/Immunology (8) Metabolic Disease (8) Neurological Disease (11)

By Targets:

5-HT Receptor (3)

Akt (1)

Apoptosis (4)

Autophagy (1)

Btk (1)

c-Met/HGFR (2)

Cannabinoid Receptor (3)

Casein Kinase (2)

CDK (2)

Dipeptidyl Peptidase (3)

DYRK (1)

EGFR (1)

Epigenetic Reader Domain (1)

Factor Xa (1)

Ferroptosis (3)

HDAC (2)

iGluR (1)

IKK (1)

Isocitrate Dehydrogenase (IDH) (1)

Isotope-Labeled Compounds (3)

Itk (1)

JAK (2)

Melatonin Receptor (2)

MMP (1)

Monoamine Oxidase (3)

p38 MAPK (1)

Phosphatase (2)

PI3K (1)

PI4K (1)

Potassium Channel (2)

PPAR (1)

Raf (2)

Ribosomal S6 Kinase (RSK) (1)

TAM Receptor (1)

TNF Receptor (1)

Topoisomerase (1)

γ-secretase (1)

By Research Areas:

Cancer (18)

Cardiovascular Disease (6)

Endocrinology (3)

Inflammation/Immunology (8)

Metabolic Disease (8)

Neurological Disease (11)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10871

Otenabant 1 Publications Verification CP-945598	Cannabinoid Receptor	Metabolic Disease
Otenabant is a potent and selective cannabinoid receptor CB1 antagonist with K_i of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.

HY-110203

R-7050 Maximum Cited Publications 12 Publications Verification TNF-α Antagonist III	TNF Receptor	Cancer
R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.

HY-12470

PF-4800567 1 Publications Verification	Casein Kinase	Others
PF-4800567 is a potent and selective inhibitor of casein kinase 1ϵ (CK1ϵ), with an IC₅₀ of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC₅₀, 711 nM).

HY-10721

PF-AKT400 AKT protein kinase inhibitor	Akt	Cancer
PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC₅₀=0.5 nM) than PKA (IC₅₀=450 nM).

HY-10871A

Otenabant Hydrochloride CP 945598 Hydrochloride	Cannabinoid Receptor	Metabolic Disease
Otenabant Hydrochloride is a potent and selective cannabinoid receptor CB1 antagonist with K_i of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.

HY-155645

Topoisomerase II inhibitor 15	Topoisomerase Apoptosis	Cancer
Topoisomerase II inhibitor 15 (compound 2g) is a Topoisomerase II inhibitor. Topoisomerase II inhibitor 15 potently is an apoptotic inducer with greater selectivity against head and neck tumors .

HY-100283

CGS 15435	Others	Inflammation/Immunology Endocrinology
CGS 15435, a potent thromboxane (TxA₂) synthetase inhibitor with an IC₅₀ of 1 nM, has a selectivity for Tx synthetase 100000-fold greater than that for cyclooxygenase, PGI₂ synthetase and lipoxygenase enzymes.

HY-19263

BMS-193884
BMS-193884 is a selective, orally active, and competitive ET_A antagonist with 10000-fold greater affinity for the human ET_A receptor (K_i=1.4 nM) than for the ET_B receptor .

HY-124264

UBP710	iGluR	Neurological Disease
UBP710 is a selective NMDA receptor modulator. UBP710 displays greater activity in potentiating GluN2B-containing receptors than those containing GluN2A .

HY-157485

Ebio1	Potassium Channel	Others
Ebio1 is a selective voltage-gated potassium channel KCNQ2 activator. Ebio1 activates KCNQ2 by generating an extended channel gate with greater conductance at a saturation voltage (+50 mV) .

HY-19972

ML243
ML243 is a selective small-molecule inhibitor of breast cancer stem cells. ML243 has 32-fold greater selective inhibition in the breast CSC-like cell line HMLE_shECad than the control cell line HMLE_shGFP .

HY-122592

Zifaxaban	Factor Xa	Cardiovascular Disease
Zifaxaban is an orally active, competitively and selective Factor Xa (FXa) inhibitor with an IC₅₀ of 11.1 nM for human FXa. Zifaxaban shows >10000-fold greater selectivity than other serine proteases. Zifaxaban can be used for the arterial and venous thrombosis research .

HY-10966

SB-590885 4 Publications Verification	Raf	Cancer
SB-590885 is a potent B-Raf inhibitor with K_i of 0.16 nM, and has 11-fold greater selectivity for B-Raf over c-Raf, without inhibition to other human kinases.

HY-15280

GSK2292767	PI3K	Inflammation/Immunology
GSK2292767 is a potent and selective inhibitor of PI3Kδ, with a pIC₅₀ of 10.1. GSK2292767 showing greater than 500-fold selective over the other PI3K isoforms. GSK2292767 can be used for the research of respiratory disease .

HY-A0023

Alogliptin Benzoate 5 Publications Verification SYR 322	Dipeptidyl Peptidase Ferroptosis	Cardiovascular Disease Metabolic Disease Inflammation/Immunology
Alogliptin Benzoate (SYR-322) is a potent, selective and orally active inhibitor of DPP-4 with an IC₅₀ of <10 nM, and exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. Alogliptin Benzoate can be used for the research of type 2 diabetes .

HY-A0023A

Alogliptin 5 Publications Verification SYR-322 free base	Dipeptidyl Peptidase Ferroptosis	Cardiovascular Disease Metabolic Disease Inflammation/Immunology
Alogliptin (SYR-322 free base) is a potent, selective and orally active inhibitor of DPP-4 with an IC₅₀ of <10 nM, and exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. Alogliptin can be used for the research of type 2 diabetes .

HY-12470A

PF-4800567 hydrochloride	Casein Kinase	Cancer
PF-4800567 hydrochloride is a potent and selective inhibitor of?casein kinase?1? (CK1?), with an?IC₅₀?of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM). PF-4800567 hydrochloride is useful in probing unique roles between these two kinases in multiple signaling pathways .

HY-141494

Pparδ agonist 5	PPAR	Metabolic Disease
Pparδ agonist 5, an orally active PPARδ-selective agonist (EC₅₀=0.335 μM), is much greater than that of the prototypical standard GW0742. Pparδ agonist 5 promotes improvements in bone density and microarchitecture in vivo .

HY-116000

Glumetinib 1 Publications Verification Gumarontinib; SCC244	c-Met/HGFR	Cancer
Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC₅₀ of 0.42 nM. Glumetinib has greater than 2400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, TyrO3. Antitumor activity .

HY-A0023AS1

Alogliptin-d3 SYR-322-d₃ free base	Isotope-Labeled Compounds Dipeptidyl Peptidase Ferroptosis	Cardiovascular Disease Metabolic Disease Inflammation/Immunology
Alogliptin-d₃ is the deuterium labeled Alogliptin. Alogliptin (SYR-322 free base) is a potent, selective and orally active inhibitor of DPP-4 with an IC50 of <10 nM, and exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. Alogliptin can be used for the research of type 2 diabetes[1][2][3].

HY-110197

6bK TFA	Others	Metabolic Disease
6bK TFA is a potent and selective insulin degrading enzyme (IDE) inhibitor with an IC₅₀ value of 50 nM. 6bK TFA increases circulating insulin in high-fat-fed mice. Acute administration of 6bK TFA enhances glucose tolerance to oral glucose, notably to a greater extent in high-fat-fed mice .

HY-150023

BI-1622	EGFR Itk PI4K Btk CDK Raf JAK	Cancer
BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC₅₀ of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile .

HY-12076

BMS 777607 5+ Cited Publications BMS 817378	c-Met/HGFR TAM Receptor	Cancer
BMS 777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC₅₀s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with more than 500-fold greater selectivity versus all other receptor and non receptor kinases .

HY-104036

IDH-305	Isocitrate Dehydrogenase (IDH)	Cancer
IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC₅₀= 27 nM (IDH1 ^R132H), 28 nM (IDH1 ^R132C), 6.14 µM (IDH1 ^WT)) .

HY-143300

BRD4-BD1-IN-2	Epigenetic Reader Domain	Cardiovascular Disease Cancer
BRD4-BD1-IN-2 is a selective BRD4-BD1 inhibitor, with an IC₅₀ of 2.51 µM (20-times greater than that of BD2). BRD4-BD1-IN-2 can be used in studies of cancer and cardiovascular diseases .

HY-103112

SB 243213 hydrochloride	5-HT Receptor	Neurological Disease
SB 243213 hydrochloride is an orally active, selective and high-affinity 5-HT_2C receptor antagonist with a pK_i of 9.37 and a pK_b of 9.8 for human 5-HT_2C receptor. SB 243213 hydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .

HY-103112A

SB 243213 dihydrochloride	5-HT Receptor	Neurological Disease
SB 243213 dihydrochloride is an orally active, selective and high-affinity 5-HT_2C receptor antagonist with a pK_i of 9.37 and a pK_b of 9.8 for human 5-HT_2C receptor. SB 243213 dihydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 dihydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .

HY-103112B

SB 243213	5-HT Receptor	Neurological Disease
SB 243213 is an orally active, selective and high-affinity 5-HT_2C receptor antagonist with a pK_i of 9.37 and a pK_b of 9.8 for human 5-HT_2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .

HY-135366

HPN-01	IKK	Inflammation/Immunology
HPN-01 is a potent and selective IKK inhibitor, with pIC₅₀ values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2 .

HY-14803

Tasimelteon BMS-214778; VEC-162	Melatonin Receptor	Neurological Disease Endocrinology
Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24) .

HY-108645

AL 8697	p38 MAPK Autophagy	Inflammation/Immunology
AL 8697 is a specific and orally active p38α MAPK inhibitor with an IC₅₀ of 6 nM. AL 8697 displays 14-fold greater inhibition of p38α compared to p38β (IC₅₀=82 nM), and 300-fold selectivity for p38α over a panel of 91 kinases. Anti-inflammatory activity .

HY-112776

BN82002	Phosphatase	Cancer
BN82002 is a potent, selective and irreversible inhibitor of CDC25 phosphatase family. BN82002 inhibits CDC25A, CDC25B2, CDC25B3, CDC25C CDC25A, and 25C-cat with IC₅₀ values of 2.4, 3.9, 6.3, 5.4, and 4.6 µM, respectively. BN82002 displays ~20-fold greater selectivity over CD45 tyrosine phosphatase .

HY-112776A

BN82002 hydrochloride 1 Publications Verification	Phosphatase	Cancer
BN82002 hydrochloride is a potent, selective and irreversible inhibitor of CDC25 phosphatase family. BN82002 hydrochloride inhibits CDC25A, CDC25B2, CDC25B3, CDC25C CDC25A, and 25C-cat with IC₅₀ values of 2.4, 3.9, 6.3, 5.4, and 4.6 µM, respectively. BN82002 hydrochloride displays ~20-fold greater selectivity over CD45 tyrosine phosphatase .

HY-161306

ITF5924	HDAC	Cancer
ITF5924 (compound 1) is a potent and highly selective HDAC6 inhibitor with an IC₅₀ of 7.7 nM. ITF5924 shows greater than 104-fold selectivity for HDAC6 over all other HDAC subtypes. ITF5924 containing a difluoromethyl-1,3,4-oxadiazole (DFMO) moiety is slow-binding substrate analog of HDAC6 that undergo an enzyme-catalyzed ring opening reaction, forming a tight and long-lived enzyme-inhibitor complex .

HY-161305

SE-7552	HDAC	Metabolic Disease Cancer
SE-7552, a 2-(difluoromethyl)-1,3,4-oxadiazole (DFMO) derivative, is an orally active, highly selective, non-hydroxamate HDAC6 inhibitor with an IC₅₀ of 33 nM. SE-7552 is greater than 850-fold selectivity versus all other known HDAC isozymes. SE-7552 is capable of blocking multiple myeloma growth in vivo. SE-7552 acts as an anti-obesity agent in diet-induced obese mice .

HY-14803S

Tasimelteon-d5 BMS-214778-d₅; VEC-162-d₅	Isotope-Labeled Compounds Melatonin Receptor	Neurological Disease Endocrinology
Tasimelteon-d₅ is the deuterium labeled Tasimelteon. Tasimelteon (BMS-214778) is an orally active and selective dual melatonin receptor agonist (DMRA). Tasimelteon has 2.1-4.4 times greater affinity for the MT2 receptor than for the MT1 receptor. Tasimelteon is a circadian regulator and has the potential for Non-24-Hour Sleep-Wake Disorder (Non-24)[1][2].

HY-122624

MMP13-IN-2	MMP	Inflammation/Immunology
MMP13-IN-2 is a potent, selective and orally active MMP-13 inhibitor. MMP13-IN-2 exhibits excellent potency for MMP-13 (IC₅₀=0.036 nM) and selectivities (greater than 1,500-fold) over MMP-1, 3, 7, 8, 9, 14, and TACE. MMP13-IN-2 has the ability to block the release of collagen from cartilage in vitro. MMP13-IN-2 has the potential for collagenase related disease research .

HY-13775

XL019 4 Publications Verification	JAK Apoptosis	Cancer
XL019 is a potent, orally active, and selective JAK2 inhibitor, with IC₅₀s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2 .

HY-101029

MBM-55
MBM-55 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC₅₀ of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC₅₀=5.4 nM) and DYRK1a (IC₅₀=6.5 nM). MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice .

HY-101257

YKL-5-124 5 Publications Verification
YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC₅₀s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status .

HY-150057

CB1R Allosteric modulator 4	Cannabinoid Receptor	Others
CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment .

HY-70057

Safinamide 2 Publications Verification FCE 26743; EMD 1195686	Monoamine Oxidase	Neurological Disease
Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC₅₀=0.098 µM) over MAO-A (IC₅₀=580 µM) . Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC₅₀=8 µM) than at resting (IC₅₀=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al .

HY-101257B

YKL-5-124 TFA 5 Publications Verification	CDK	Cancer
YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC₅₀s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status .

HY-101029A

MBM-55S	Ribosomal S6 Kinase (RSK) DYRK Apoptosis	Cancer
MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC₅₀ of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC₅₀=5.4 nM) and DYRK1a (IC₅₀=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice .

HY-70057A

Safinamide mesylate 2 Publications Verification FCE 26743 mesylate; EMD 1195686 mesylate	Monoamine Oxidase	Cardiovascular Disease Neurological Disease
Safinamide (FCE 26743; EMD 1195686) mesylate is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC₅₀=0.098 µM) over MAO-A (IC₅₀=580 nM) . Safinamide mesylate also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC₅₀=8 µM) than at resting (IC₅₀=262 µM) potentials. Safinamide mesylate has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke et.al .

HY-101396

ICA-069673 2 Publications Verification	Potassium Channel	Neurological Disease
ICA-069673 is a KCNQ2/Q3 potassium channel activator. ICA-069673 demonstrates greater selectivity for KV7.2/7.3 over KV7.3/KV7.5, with EC₅₀s of 0.69 μM and 14.3 μM, respectively. ICA-069673 inhibits spontaneous phasic and nerve-evoked contractions in guinea pig detrusor smooth muscle (DSM). ICA-069673 also decreases the global intracellular Ca(2+) concentration in DSM cells .

HY-19369

L-685458 3 Publications Verification L-685,458	γ-secretase Apoptosis	Neurological Disease Cancer
L-685458 is a potent transition state analog (TSA) γ-secretase inhibitor (GSI). L-685458 inhibits amyloid β-protein precursor γ-secretase activity with IC₅₀ of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested. L685458 inhibits γ-secretase-mediated cleavage of APP-C99 and Notch-100 with IC₅₀s of 301.3 nM and 351.3 nM, respectively. L-685458 can be used for the research of alzheimer’s disease (AD) and cancers .

HY-70057S1

Safinamide-d4-1 FCE 26743-d₄-1; EMD 1195686-d₄-1	Isotope-Labeled Compounds Monoamine Oxidase	Neurological Disease
Safinamide-d₄-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].

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