Search Result

Results for "

cell-based assay

" in MedChemExpress (MCE) Product Catalog:

By Targets:	11β-HSD (1) Anaplastic lymphoma kinase (ALK) (5) Autophagy (4) c-Met/HGFR (6) Constitutive Androstane Receptor (1) E3 Ligase Ligand-Linker Conjugates (5) Fatty Acid Synthase (FASN) (1) FXR (1) Glucocorticoid Receptor (1) HCV (2) HCV Protease (2) Isotope-Labeled Compounds (2) MAGL (1) MAPKAPK2 (MK2) (1) PARP (1) Phosphatase (1) Phosphodiesterase (PDE) (1) Protease Activated Receptor (PAR) (1) RIP kinase (1) ROS Kinase (5) SARS-CoV (2) STING (1) TAM Receptor (1) Trk Receptor (4) VEGFR (1)
By Research Areas:	Cancer (17) Cardiovascular Disease (1) Endocrinology (1) Infection (3) Inflammation/Immunology (3) Metabolic Disease (5) Neurological Disease (5)

By Targets:

11β-HSD (1)

Anaplastic lymphoma kinase (ALK) (5)

Autophagy (4)

c-Met/HGFR (6)

Constitutive Androstane Receptor (1)

E3 Ligase Ligand-Linker Conjugates (5)

Fatty Acid Synthase (FASN) (1)

FXR (1)

Glucocorticoid Receptor (1)

HCV (2)

HCV Protease (2)

Isotope-Labeled Compounds (2)

MAGL (1)

MAPKAPK2 (MK2) (1)

PARP (1)

Phosphatase (1)

Phosphodiesterase (PDE) (1)

Protease Activated Receptor (PAR) (1)

RIP kinase (1)

ROS Kinase (5)

SARS-CoV (2)

STING (1)

TAM Receptor (1)

Trk Receptor (4)

VEGFR (1)

By Research Areas:

Cancer (17)

Cardiovascular Disease (1)

Endocrinology (1)

Infection (3)

Inflammation/Immunology (3)

Metabolic Disease (5)

Neurological Disease (5)

Inhibitors & Agonists

Screening Libraries

Peptides

Isotope-Labeled Compounds

Targets Recommended: Biochemical Assay Reagents Itk TOPK NAMPT ALCAM/CD166 GDNF Receptor BCL6 Tim3

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-129634

TrkA-IN-1	Trk Receptor	Neurological Disease
TrkA-IN-1 is a potent and selective Tropomyosin-related kinase A (TrkA) inhibitor with an IC₅₀ of 99 nM in a cell-based assay. TrkA-IN-1 has analgesic activity .

HY-112476

PRL-3 Inhibitor I

Phosphatase Cancer

PRL-3 Inhibitor I is a potent PRL-3 inhibitor with an IC₅₀ of 0.9 μM. PRL-3 Inhibitor I shows a reduced invasion in cell-based assay .

PRL-3 Inhibitor I	Phosphatase	Cancer
PRL-3 Inhibitor I is a potent PRL-3 inhibitor with an IC₅₀ of 0.9 μM. PRL-3 Inhibitor I shows a reduced invasion in cell-based assay .

HY-112437

PF-06737007	Trk Receptor	Neurological Disease
PF-06737007 is a potent pan-Trk inhibitor in cell-based assays with IC₅₀s of 7.7 nM, 15 nM and 3.9 nM for TrkA, TrkB and TrkC, respectively . Anti-hyperalgesic effect .

HY-161352

NPI52	Others	Infection
NPI52 (Compound E1) is a foot-and-mouth disease virus 3C protease (FMDV 3Cpro) inhibitor, with IC₅₀ values of 0.05 and 0.11 µM in FRET and cell-based assay, respectively .

HY-112434

PF-06733804	Trk Receptor	Neurological Disease
PF-06733804 is a potent pan-Trk inhibitor in cell-based assays with IC₅₀s of 8.4 nM, 6.2 nM and 2.2 nM for TrkA, TrkB and TrkC, respectively . Anti-hyperalgesic effect .

HY-109042

Relacorilant CORT 125134	Glucocorticoid Receptor	Cardiovascular Disease Endocrinology
Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a K_i of 7.2 nM in HepG2 TAT assay, and also shows K_is of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively. Relacorilant has the potential for Cushing’s syndrome treatment.

HY-10237

Boceprevir 25+ Cited Publications EBP 520; SCH 503034	HCV Protease HCV SARS-CoV	Infection
Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a K_i of 14 nM in both enzyme assay and an EC₉₀ of 350 nM in cell-based replicon assay . Boceprevir inhibits SARS-CoV-2 3CL ^pro activity .

HY-112436

PF-6683324 Trk-IN-4	Trk Receptor	Neurological Disease
PF-6683324 (Trk-IN-4) is a potent pan-Trk inhibitor in cell-based assays with IC₅₀s of 1.9 nM, 2.6 nM and 1.1 nM for TrkA, TrkB and TrkC, respectively . Anti-hyperalgesic effect .

HY-10237S

Boceprevir-d9 EBP 520-d₉; SCH 503034-d₉	Isotope-Labeled Compounds HCV Protease HCV SARS-CoV	Infection
Boceprevir-d₉ is the deuterium labeled Boceprevir. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay[1][2][3][4][5]. Boceprevir inhibits SARS-CoV-2 3CLpro activity[6].

HY-10555

AMG-221	11β-HSD	Metabolic Disease
AMG-221 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with a K_i of 12.8 nM in vitro biochemical scintillation proximity assay (SPA) and an IC₅₀ of 10.1 nM in cell-based assays . AMG-221 can be used for the research of type 2 diabetes .

HY-110267

DY268	FXR	Metabolic Disease
DY268 is a farnesoid X receptor (FXR) antagonist (IC₅₀=7.5 nM). It inhibits FXR transactivation in a cell-based assay with an IC₅₀ value of 468 nM. DY268 can be used in the study of drug-induced liver injury (DILI) .

HY-111538

MAGL-IN-1	MAGL	Cancer
MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC₅₀ of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays .

HY-110134

S07662	Constitutive Androstane Receptor	Metabolic Disease
S07662 is a human constitutive androstane receptor (hCAR) inhibitor with an IC₅₀ of 0.7 μM. S07662 recruits the corepressor NCoR in cell-based assays and attenuate the expression of CYP2B6 mRNA in human primary hepatocytes induced by phenytoin (HY-B0448) and CITCO (HY-103244) .

HY-151193

NNMT-IN-3	Others	Metabolic Disease Cancer
NNMT-IN-3 (compound 14) is a potent and selective nicotinamide N-methyltransferase NNMT inhibitor with IC₅₀ values of 1.1 nM and 0.4 μM in cell-free and cell-based assays, respectively. NNMT-IN-3 can be used to research obesity, type 2 diabetes, alcohol-related liver disease, cancer, sarcopenia and so on .

HY-115510

SPR inhibitor 3 SPRi3	Others	Inflammation/Immunology
SPR inhibitor 3 (SPRi3) is a potent sepiapterin reductase (SPR) inhibitor. SPR inhibitor 3 (SPRi3) displays high binding affinity to human SPR in a cell-free assay (IC₅₀=74 nM) and efficiently reduces biopterin levels in a cell-based assay (IC₅₀=5.2 μM). SPR inhibitor 3 (SPRi3) reduces neuropathic and inflammatory pain through a reduction of BH4 levels .

HY-111551

FT113 1 Publications Verification	Fatty Acid Synthase (FASN)	Cancer
FT113 is a potent and orally active fatty acid synthase (FASN) inhibitor, with an IC₅₀ of 213 nM for full-length recombinant human FASN enzyme. In cell-based assay, FT113 blocks FASN activity in BT474 cells (IC₅₀, 90 nM). FT113 shows anti-proliferative activity, and exhibits anti-cancer activity both in vitro and in vivo .

HY-138696

Zanzalintinib 1 Publications Verification XL092	TAM Receptor c-Met/HGFR VEGFR	Cancer
Zanzalintinib (XL092) is an orally active, ATP-competitive inhibitor of multiple receptor tyrosine kinases (RTKs) including MET, VEGFR2, AXL and MER, with IC₅₀s in cell-based assays of 15 nM, 1.6 nM, 3.4 nM, 7.2 nM respectively. Zanzalintinib exhibits anti-tumor activity. Zanzalintinib has the potential for kinase-dependent diseases and conditions research .

HY-151813

NNMT-IN-4	Others	Cancer
NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC₅₀ values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT .

HY-155151

RIPK2/3-IN-1	RIP kinase	Inflammation/Immunology
RIPK2/3-IN-1 is a potent dual RIPK2/3 kinases inhibitor with IC₅₀ values of 3 nM and 117 nM, respectively. RIPK2/3-IN-1 is against RIPK2 with IC₅₀ value 14 nM in 14-TriLAN-Gly/NOD1 THP-1 cell-based NF-κB reporter assay .

HY-50878

Crizotinib Maximum Cited Publications 61 Publications Verification PF-02341066	Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy	Cancer
Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .

HY-50878B

Crizotinib acetate PF-02341066 acetate	Anaplastic lymphoma kinase (ALK) ROS Kinase c-Met/HGFR	Cancer
Crizotinib (PF-02341066) acetate is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib acetate inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. Crizotinib acetate is also a ROS1 inhibitor. Crizotinib acetate has effective tumor growth inhibition .

HY-50878S

Crizotinib-d5 PF-02341066-d₅	Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy	Cancer
Crizotinib-d₅ is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .

HY-163343

Enpp-1-IN-20	Phosphodiesterase (PDE) STING	Cancer
Enpp-1-IN-20 (Compound 31) is an ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) inhibitor, with an IC₅₀ of 0.09 nM. Enpp-1-IN-20 has strongest inhibitory activity in the cell-based assay, with an IC₅₀ of 8.8 nM. Enpp-1-IN-20 has significant potency in both ENPP1 inhibition and STING pathway stimulation in vitro. Enpp-1-IN-20 can be used for the research of cancer .

HY-50878A

Crizotinib hydrochloride Maximum Cited Publications 61 Publications Verification PF-02341066 hydrochloride	Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy	Cancer
Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .

HY-103608

(S,R,S)-AHPC-(C3-PEG)2-C6-Cl VHL Ligand-Linker Conjugates 11; E3 ligase Ligand-Linker Conjugates 11	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-(C3-PEG)2-C6-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-(C3-PEG)2-C6-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .

HY-117427

D5D-IN-326	Others	Metabolic Disease
D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC₅₀s of 72 and 22 nM for rat and human D5D in enzymic and cell-based assays, respectively, has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in diet-induced obese C57BL/6J mice .

HY-50878AS

Crizotinib-d9 hydrochloride PF-02341066-d₉ hydrochloride	c-Met/HGFR Autophagy Anaplastic lymphoma kinase (ALK) ROS Kinase Isotope-Labeled Compounds	Cancer
Crizotinib-d₉ hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .

HY-103606

(S,R,S)-AHPC-PEG6-C4-Cl VH032-PEG6-C4-Cl; VHL Ligand-Linker Conjugates 10; E3 ligase Ligand-Linker Conjugates 9	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-PEG6-C4-Cl is a conjugate of ligands for E3 and 25-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-PEG6-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and 6-unit PEG linker. (S,R,S)-AHPC-PEG6-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .

HY-112495

VH032-PEG5-C6-Cl HaloPROTAC 2	E3 Ligase Ligand-Linker Conjugates	Cancer
VH032-PEG5-C6-Cl (HaloPROTAC 2) is a conjugate of ligands for E3 and 21-atom-length linker. The connector of linker is Halogen group. VH032-PEG5-C6-Cl incorporates the VH032 based VHL ligand and 5-unit PEG linker. VH032-PEG5-C6-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .

HY-103607

(S,R,S)-AHPC-PEG2-C4-Cl VH032-PEG2-C4-Cl; VHL Ligand-Linker Conjugates 7; E3 ligase Ligand-Linker Conjugates 10	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-PEG2-C4-Cl (VH032-PEG2-C4-Cl) is a conjugate of ligands for E3 and 13-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-PEG2-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-PEG2-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .

HY-P5372

Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2	Protease Activated Receptor (PAR)	Others
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a biological active peptide. (Protease activated receptor 1 (PAR-1) belongs to a subfamily of G-protein coupled receptors and is known to mediate the cellular effects of thrombin. This peptide is a PAR-1 selective agonist displaying a high level of specificity to PAR-1 over PAR-2. The specificity of peptide was evaluated in cell-based calcium signaling assay using HEK293 cells. PAR-1 selective agonists can be used to study PAR-1 activation in vivo. In addition to its varied cellular effects of thrombin, PAR-1 has also been shown to coordinate with PAR-4 and regulate thrombin-induced hepatocellular carcinoma harboring thrombin formation within the tumor environment classified as 'coagulation type'.)

HY-103605

(S,R,S)-AHPC-C6-PEG3-C4-Cl VH032-C6-PEG3-C4-Cl; VHL Ligand-Linker Conjugates 12; E3 ligase Ligand-Linker Conjugates 8	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-C6-PEG3-C4-Cl (VH032-C6-PEG3-C4-Cl) is a conjugate of ligands for E3 and 20-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-C6-PEG3-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-C6-PEG3-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .

HY-105253

PARP-2/1-IN-2	PARP	Neurological Disease
PARP-2/1-IN-2 (Compound 4a), the enantiomer of Veliparib (HY-10129), is a potent PARP inhibitor with K_is of 2 and 5 nM against PARP-2 and PARP-1, respectively. PARP-2/1-IN-2 has an EC₅₀ of 3 nM in a cell based assay of PARP activity .

HY-139504

Gamcemetinib CC-99677	MAPKAPK2 (MK2)	Inflammation/Immunology
Gamcemetinib (CC-99677) is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC₅₀=156.3 nM) and cell based assays (EC₅₀=89 nM). Gamcemetinib is extracted from patent WO2020236636, compound 1 .

Novel Bioactive Compound Library	1220 compounds
MCE Novel Bioactive Compound Library consists of 1220 bioactive compounds with validated bioactivities tested by cell-based assays or biochemical assays. All compounds in this library are structurally novel and bioactivity diverse which makes it easier to discover new lead compounds. MCE Novel Bioactive Compound Library, as a supplement of MCE bioactive compound library (HY-L001), is a useful tool to screen new lead compounds.

Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2	Protease Activated Receptor (PAR)	Others
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a biological active peptide. (Protease activated receptor 1 (PAR-1) belongs to a subfamily of G-protein coupled receptors and is known to mediate the cellular effects of thrombin. This peptide is a PAR-1 selective agonist displaying a high level of specificity to PAR-1 over PAR-2. The specificity of peptide was evaluated in cell-based calcium signaling assay using HEK293 cells. PAR-1 selective agonists can be used to study PAR-1 activation in vivo. In addition to its varied cellular effects of thrombin, PAR-1 has also been shown to coordinate with PAR-4 and regulate thrombin-induced hepatocellular carcinoma harboring thrombin formation within the tumor environment classified as 'coagulation type'.)

Crizotinib-d5
Crizotinib-d₅ is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .

Boceprevir-d9
Boceprevir-d₉ is the deuterium labeled Boceprevir. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay[1][2][3][4][5]. Boceprevir inhibits SARS-CoV-2 3CLpro activity[6].

Crizotinib-d9 hydrochloride
Crizotinib-d₉ hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: