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Results for "

1-2-c-

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Apoptosis (7) ATTECs (1) Autophagy (3) Biochemical Assay Reagents (3) Casein Kinase (1) Cholinesterase (ChE) (1) Cytochrome P450 (2) DNA Alkylator/Crosslinker (1) DNA/RNA Synthesis (1) Dopamine Receptor (1) Drug Intermediate (2) Drug Metabolite (2) ERK (2) FAAH (1) Fluorescent Dye (1) HDAC (3) HSP (1) iGluR (1) Influenza Virus (1) Kinesin (1) Microtubule/Tubulin (1) MMP (1) Monoamine Oxidase (1) Nucleoside Antimetabolite/Analog (3) p38 MAPK (4) PARP (1) Phosphodiesterase (PDE) (2) PI3K (1) Raf (1) Reactive Oxygen Species (ROS) (2) Reference Standards (2) Topoisomerase (1) VEGFR (2) Virus Protease (1)
By Research Areas:	Cancer (17) Cardiovascular Disease (2) Infection (2) Inflammation/Immunology (4) Neurological Disease (5)
Oligonucleotides:	Nucleoside Analogs (3)

Inhibitors & Agonists

Screening Libraries

Oligonucleotides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-106509

Velaresol BW 12C; 12C79; BW 12C79	Others	Others
Velaresol (BW 12C) is a potent left-shifting anti-sickling compound in vitro . Sickle cell disease is an inherited disorder of the hemoglobin molecule. When hemoglobin molecules are exposed to a variety of environments, the red blood cell hemoglobin polymerizes, twists, and morphs into a sickle shape.

HY-106509R

Velaresol (Standard) BW 12C (Standard); 12C79 (Standard); BW 12C79 (Standard)	Reference Standards Others	Others
Velaresol (Standard) is the analytical standard of Velaresol. This product is intended for research and analytical applications. Velaresol (BW 12C) is a potent left-shifting anti-sickling compound in vitro . Sickle cell disease is an inherited disorder of the hemoglobin molecule. When hemoglobin molecules are exposed to a variety of environments, the red blood cell hemoglobin polymerizes, twists, and morphs into a sickle shape.

HY-152982

1-(2-C-β-Methyl-β-D-ribofuranosyl)-5-nitropyridine-2(1H)-one	Nucleoside Antimetabolite/Analog	Others
1-(2-C-β-Methyl-β-D-ribofuranosyl)-5-nitropyridine-2(1H)-one is a nitropyridine nucleoside analogue.

HY-161965

*MK-3168 (12C)*	FAAH	Neurological Disease
MK-3168 (12C) is a FAAH inhibitor with IC₅₀ values of 1.0, 5.5, 1.7 nM for human, rhesus, rat, respectively. MK-3168 shows good brain uptake and FAAH-specific signal. ¹¹C MK-3168 can be used as FAAH PET tracer .

HY-169985

CK2-IN-13	Casein Kinase	Cancer
CK2-IN-13 (compound 12c) is a potent inhibitor of CK2, with the IC₅₀ of 5.8 nM. CK2-IN-13 plays an important role in cancer research .

HY-147926

VEGFR-2-IN-28	VEGFR Apoptosis	Cancer
VEGFR-2-IN-28 (compound 12c) is a potent VEGFR-2 inhibitor with IC₅₀ value of 0.83 µM. VEGFR-2-IN-28 induces apoptosis and has anticancer activity .

HY-115955

Dopamine D3 receptor ligand-3	Dopamine Receptor	Neurological Disease
Dopamine D3 receptor ligand-3 (compound 12C) is a potent D3 receptor ligand with a Ki of 3.6 nM. Dopamine D3 receptor ligand-3 have high selectivity for D3 over D2 (Ki=353 nM).

HY-147801

Topoisomerase IIα-IN-3	Topoisomerase Apoptosis	Cancer
Topoisomerase IIα-IN-3 (Compound 12c) is a DNA intercalative topoisomerase-IIα inhibitor. Topoisomerase IIα-IN-3 arrests cell cycle at the G0/G1 phase and induces apoptosis .

HY-147730

HDAC6-IN-8	HDAC	Cancer
A variety of compounds were designed and synthesized by modifying cap groups. The enzyme inhibition test showed that compound 12C had broad-spectrum enzyme inhibitory activity, and compounds 9m and 9q were more inclined to inhibit HDAC6, showing a certain selective inhibitory activity among the representative subtypes.

HY-149003

PARP1-IN-10	PARP Apoptosis	Cancer
PARP1-IN-10 (compound 12c) is a no-cytotoxicity and potent PARP1 inhibitor with an IC₅₀ value of 50.62 nM in vitro. PARP1-IN-10 causes cell cycle arrest at G2/M phase and apoptosis, and enhances the cytotoxicity of temozolomide (TMZ) .

HY-160002

MAO-B-IN-27	Monoamine Oxidase	Neurological Disease
MAO-B-IN-27 (Compound 12c) is a monoamine oxidase B (MAO-B) inhibitor. MAO-B-IN-27 has potent and selective MAO-B inhibitory effect for hMAO-B with an IC₅₀ values of 8.9 nM. MAO-B-IN-27 can be used for the research of parkinson's disease (PD) .

HY-147846

AChE/PDE4-IN-1	Cholinesterase (ChE) Phosphodiesterase (PDE)	Neurological Disease
AChE/PDE4-IN-1 (compound 12c) is a potent and selective dual PDE4/AChE inhibitor, with IC₅₀s of 0.28 μM and 1.88 μM for AChE and PDE4D, respectively. AChE/PDE4-IN-1 exhibits anti-neuroinflammatory effect for the research of Alzheimer's disease .

HY-147731

HDAC6-IN-9	HDAC	Cancer
HDAC6-IN-9 (compound 12c) is a potent and selective HDAC6 inhibitor with IC₅₀ values of 11.8, 15.2, 4.2, 139.6, 21.3 nM for HDAC1,HDAC3, HDAC6, HDAC8, HDAC10, respectively. HDAC6-IN-9 shows anti-proliferative activities .

HY-157458

PDEδ autophagic degrader 1	ATTECs Phosphodiesterase (PDE) Autophagy	Cancer
PDEδ autophagic degrader 1 (compound 12c), an autophagosome-tethering compound (ATTEC). is a potent PDEδ autophagic degrader. PDEδ autophagic degrader 1 reduces the PDEδ protein level through lysosome-mediated autophagy without affecting the PDEδ mRNA expression. PDEδ autophagic degrader 1 suppresses the growth in KRAS mutant pancreatic cancer cells .

HY-147768

PI3K/AKT-IN-2	PI3K Akt Microtubule/Tubulin MMP Apoptosis	Cancer
PI3K/AKT-IN-2 (Compound 12c) is a PI3K and AKT inhibitor. PI3K/AKT-IN-2 blocks the epithelial-mesenchymal transition (EMT) and induces apoptosis. PI3K/AKT-IN-2 inhibits the polymerization of tubulin .

HY-150597

HDAC-IN-46	HDAC Apoptosis	Cancer
HDAC-IN-46 (compound 12c) is a potent HDAC inhibitor with an IC₅₀ value of 0.21 μM and 0.021 μM for HDAC1 and HDAC6, respectively. HDAC-IN-46 upregulates p-p38, and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 induces significant G2 phase arrest and apoptosis. HDAC-IN-46 can be used for researching triple-negative breast cancer (TNBC) .

HY-146325

HSP90-IN-11	HSP	Cancer
HSP90-IN-11 (Compound 12c) is a potent inhibitor of HSP90. HSP90-IN-11 displays potent HSP90α inhibition comparable to AUY-922 (Luminespib). HSP90-IN-11 shows significant antiproliferative activity in CRC and NSCLC cells in a double digit nM range. HSP90-IN-11 leads to rapid degradation of client proteins EGFR and Akt in NSCLC cells. HSP90-IN-11 induces significant accumulation of a sub-G1 phase population .

HY-W366582

*7-Methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-amine*	Drug Intermediate	Others
7-Methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-amine is a synthetic intermediate useful for pharmaceutical synthesis.

HY-Q51221

*3-Benzyl-8,9-dimethoxy-5-[(2-methylbenzyl)thio]imidazo[1,2-c]quinazolin-2(3H)-one*	Biochemical Assay Reagents	Others
3-Benzyl-8,9-dimethoxy-5-[(2-methylbenzyl)thio]imidazo[1,2-c]quinazolin-2(3H)-one is a biological molecule.

HY-W017742

Rolapitant Intermediate (3R,7aR)-3-(tert-Butyl)-1-hydroxy-7a-vinyltetrahydropyrrolo[1,2-c]oxazol-5(3H)-one	Drug Intermediate	Others
Rolapitant Intermediate ((3R,7aR)-3-(tert-Butyl)-1-hydroxy-7a-vinyltetrahydropyrrolo[1,2-c]oxazol-5(3H)-one) is a drug intermediate for synthesis of various active compounds.

HY-152770

*6-(2-O-Methyl-beta-D-ribofuranosyl)-3-(2-oxo-propyl)-6H-imidazo[1,2-c]pyrimidin-5-one*	Nucleoside Antimetabolite/Analog	Others
6-((2R,3R,4R,5R)-4-Hydroxy-5-(hydroxymethyl)-3-methoxytetrahydrofuran-2-yl)-3-(2-oxopropyl)imidazo[1,2-c]pyrimidin-5(6H)-one is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc .

HY-111297

BMVC4	Biochemical Assay Reagents	Cancer
BMVC4 is a G-quadruplex (G4) stabilizer of the human telomeric sequence d[AG3(T2AG3)3]. Screening by circular dichroism (CD) spectroscopy revealed that BMVC4 is more suitable as the core molecule of G4 stabilizers than BMVC. The results showed that BMVC4-12C and BMVC4-8C3O are better candidates for G4 stabilizers and are worthy of further study. A simple and rapid screening method based on Cu2+-induced G4 unfolding can be used to find better G4 stabilizers for potential anticancer applications. CD results showed that the trivalent cations of 9-substituted BMVC derivatives are more suitable as G4 stabilizers than the divalent cations of BMVC. In addition, by monitoring the disappearance of the 291 nm CD band of human telomeres after Cu2+ addition, it was found that the core molecule of G4 stabilizer BMVC4 has better stability.

HY-D1551

*10-(4-(Bis(2-hydroxyethyl)amino)phenyl)-5,5-difluoro-1,3,7,9-tetramethyl-5H-dipyrrolo[1,2-c:2',1'-f][1,3,2]diazaborinin-4-ium-5-uide*	Fluorescent Dye	Others
10-(4-(Bis(2-hydroxyethyl)amino)phenyl)-5,5-difluoro-1,3,7,9-tetramethyl-5H-dipyrrolo[1,2-c:2',1'-f][1,3,2]diazaborinin-4-ium-5-uide, a BODIPY derivative, is a fluorescent indicator for detecting Pb ²⁺ (Ex=504 nM, Em=510 nM) .

HY-151254

CYP2C19-IN-1	Cytochrome P450 Influenza Virus DNA/RNA Synthesis	Infection
CYP2C19-IN-1 (compound 20d) is a potent CYP2C19 inhibitor, possessing no hepatotoxicity and ames toxicity. CYP2C19-IN-1 inhibits RNA-dependent RNA polymerase (RdRP) with a K_i value of 6.16 µM. CYP2C19-IN-1 can be used in study of anti-ZIKV .

HY-149674

VEGFR-2/c-Met-IN-1	VEGFR	Cancer
VEGFR-2/c-Met-IN-1 is a dual inhibitoe of VEGFR-2 and c-Met with *IC₅₀s of 138 nM and 74 nM, respectively. VEGFR-2/c-Met-IN-1 has antitumor activity .*

HY-152718

*4-Amino-1-(2-C-methyl-β-D-ribofuranosyl)-1H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile*	Nucleoside Antimetabolite/Analog	Others
4-Amino-5-cyano-1-(2-β-C-methyl-β-D-ribofuranosyl)-7H-pyrrolo[2.3-d]pyrimidine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc .

HY-173522

KIF2C-IN-1	Kinesin	Cancer
KIF2C-IN-1 (Compound 7S9) is a selective and potent small-molecule KIF2C inhibitor. KIF2C-IN-1 stabilizes the KIF2C-tubulin interaction, blocking the depolymerization of polyglutamylated microtubules. KIF2C-IN-1 enhances the cytotoxicity of Paclitaxel (HY-B0015) in paclitaxel-resistant triple-negative breast cancer (TNBC) cells and significantly reduces tumor growth combined with Paclitaxel in mouse models .

HY-151251

CYP2C9/CYP2C19-IN-1	Cytochrome P450 Virus Protease	Infection
CYP2C9/CYP2C19-IN-1 (compound 22d) is a potent CYP2C9/CYP2C19 inhibitor, possessing no hepatotoxicity and ames toxicity. CYP2C9/CYP2C19-IN-1 can be used in study of anti-ZIKV .

HY-172121

NMDA agonist 2	iGluR	Neurological Disease
NMDA agonist 2 (compound 8d) is a potent agonist of NMDA receptor, with the EC₅₀ of 0.034 μM for *GluN1/2C*. NMDA agonist 2 plays an important role in neurological and psychiatric disorders .

HY-10542

GW 5074 5+ Cited Publications	Raf Apoptosis	Cancer
GW 5074 is a potent and selective c-Raf inhibitor with IC₅₀ of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms .

HY-144335

DNA crosslinker 2 dihydrochloride	DNA Alkylator/Crosslinker	Cancer
DNA crosslinker 2 (dihydrochloride) is a potent DNA minor groove binder with DNA binding affinity (ΔT_m) of 1.2 °C. DNA crosslinker 2 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 2 (dihydrochloride) can be used for researching anticancer .

HY-13241

Ralimetinib dimesylate Maximum Cited Publications 14 Publications Verification LY2228820 dimesylate	p38 MAPK Autophagy Apoptosis	Inflammation/Immunology Cancer
Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC₅₀s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.

HY-13241A

Ralimetinib LY2228820	p38 MAPK Autophagy	Inflammation/Immunology Cancer
Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC₅₀s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc .

HY-132994

TVD-0003510	Biochemical Assay Reagents	Others
TVD-0003510 is a carboxamide derivative, and involves in synthesis of (2-((6-(2-aminopyrimidine-5-carboxamido)-8-methoxy-3,4-dihydro-2H-pyrimido[1,2-c]quinazolin-9-yl)oxy)ethyl)piperazine-l-carboxylate (C51), as a part of tert-butyl2-(4-hydroxyphenyl)acetate .

HY-W050000

OR-1855 1 Publications Verification	Drug Metabolite Reactive Oxygen Species (ROS) ERK p38 MAPK	Cardiovascular Disease Inflammation/Immunology
OR-1855, an active metabolite of Levosimendan (HY-14286), has effect on myometrial contractility. OR-1855 exerts anti-inflammatory effects by inhibiting IL-1β-induced ROS formation and NAD(P)H oxidase-dependent superoxide radical generation in HUVECs. OR-1855 inhibits IL-1β-induced phosphorylation p38 MAPK, *ERK1/2, c-Jun* and JNK in HUVECs. OR-1855 can be used for the study of inflammation .

HY-W050000R

OR-1855 (Standard)	Drug Metabolite Reference Standards Reactive Oxygen Species (ROS) ERK p38 MAPK	Cardiovascular Disease Inflammation/Immunology
OR-1855 (Standard) is an analytical standard of OR-1855 (HY-W050000). This product is intended for research and analytical applications. OR-1855, an active metabolite of Levosimendan (HY-14286), has effect on myometrial contractility. OR-1855 exerts anti-inflammatory effects by inhibiting IL-1β-induced ROS formation and NAD(P)H oxidase-dependent superoxide radical generation in HUVECs. OR-1855 inhibits IL-1β-induced phosphorylation p38 MAPK, *ERK1/2, c-Jun* and JNK in HUVECs. OR-1855 can be used for the study of inflammation .

Cat. No.	Product Name

HY-L010

MAPK Compound Library	847 compounds
MAPK families play an important role in complex cellular programs like proliferation, differentiation, development, transformation, and apoptosis. In mammalian cells, four MAPK families have been clearly characterized: ERK1/2, C-Jun N-terminal kinse/stress-activated protein kinase (JNK/SAPK) , p38 kinase and ERK5. They respond to different signals. Each MAPK-related cascade consists of three enzymes that are activated in series: a MAPK kinase kinase (MAPKKK), a MAPK kinase (MAPKK) and a MAP kinase (MAPK). MAPK signaling pathways has been implicated in the development of many human diseases including Alzheimer's disease (AD), Parkinson's disease (PD), amyotrophic lateral sclerosis (ALS) and various types of cancers. MCE designs a unique collection of 847 MAPK signaling pathway inhibitors that act as a useful tool for MAPK-related drug screening and disease research.

MAPK Compound Library

847 compounds

MAPK families play an important role in complex cellular programs like proliferation, differentiation, development, transformation, and apoptosis. In mammalian cells, four MAPK families have been clearly characterized: ERK1/2, C-Jun N-terminal kinse/stress-activated protein kinase (JNK/SAPK) , p38 kinase and ERK5. They respond to different signals. Each MAPK-related cascade consists of three enzymes that are activated in series: a MAPK kinase kinase (MAPKKK), a MAPK kinase (MAPKK) and a MAP kinase (MAPK). MAPK signaling pathways has been implicated in the development of many human diseases including Alzheimer's disease (AD), Parkinson's disease (PD), amyotrophic lateral sclerosis (ALS) and various types of cancers.

MCE designs a unique collection of 847 MAPK signaling pathway inhibitors that act as a useful tool for MAPK-related drug screening and disease research.

1-(2-C-β-Methyl-β-D-ribofuranosyl)-5-nitropyridine-2(1H)-one		Nucleoside Analogs
1-(2-C-β-Methyl-β-D-ribofuranosyl)-5-nitropyridine-2(1H)-one is a nitropyridine nucleoside analogue.

*6-(2-O-Methyl-beta-D-ribofuranosyl)-3-(2-oxo-propyl)-6H-imidazo[1,2-c]pyrimidin-5-one*		Nucleoside Analogs
6-((2R,3R,4R,5R)-4-Hydroxy-5-(hydroxymethyl)-3-methoxytetrahydrofuran-2-yl)-3-(2-oxopropyl)imidazo[1,2-c]pyrimidin-5(6H)-one is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc .

*4-Amino-1-(2-C-methyl-β-D-ribofuranosyl)-1H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile*		Nucleoside Analogs
4-Amino-5-cyano-1-(2-β-C-methyl-β-D-ribofuranosyl)-7H-pyrrolo[2.3-d]pyrimidine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc .

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