Search Result

Results for "

Ra Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Apoptosis (3) Autophagy (2) Bacterial (3) Bcl-2 Family (2) c-Fms (1) Carbonic Anhydrase (1) CD6 (1) ClpP (1) Complement System (2) COX (3) Cytochrome P450 (3) Deubiquitinase (1) Dihydroorotate Dehydrogenase (1) Drug Metabolite (1) E1/E2/E3 Enzyme (1) Endogenous Metabolite (2) GLUT (2) Interleukin Related (2) IRAK (2) JAK (1) Keap1-Nrf2 (1) mAChR (1) MMP (1) NF-κB (1) NO Synthase (1) Nucleoside Antimetabolite/Analog (1) p38 MAPK (1) PGE synthase (1) Potassium Channel (1) Proteasome (2) Protein Arginine Deiminase (2) RAR/RXR (5) Reactive Oxygen Species (2) SGLT (2) Sigma Receptor (1) TNF Receptor (2) VEGFR (1)
By Research Areas:	Cancer (14) Cardiovascular Disease (4) Infection (6) Inflammation/Immunology (25) Metabolic Disease (6) Neurological Disease (3)

By Targets:

5-HT Receptor (1)

Apoptosis (3)

Autophagy (2)

Bacterial (3)

Bcl-2 Family (2)

c-Fms (1)

Carbonic Anhydrase (1)

CD6 (1)

ClpP (1)

Complement System (2)

COX (3)

Cytochrome P450 (3)

Deubiquitinase (1)

Dihydroorotate Dehydrogenase (1)

Drug Metabolite (1)

E1/E2/E3 Enzyme (1)

Endogenous Metabolite (2)

GLUT (2)

Interleukin Related (2)

IRAK (2)

JAK (1)

Keap1-Nrf2 (1)

mAChR (1)

MMP (1)

NF-κB (1)

NO Synthase (1)

Nucleoside Antimetabolite/Analog (1)

p38 MAPK (1)

PGE synthase (1)

Potassium Channel (1)

Proteasome (2)

Protein Arginine Deiminase (2)

RAR/RXR (5)

Reactive Oxygen Species (2)

SGLT (2)

Sigma Receptor (1)

TNF Receptor (2)

VEGFR (1)

By Research Areas:

Cancer (14)

Cardiovascular Disease (4)

Infection (6)

Inflammation/Immunology (25)

Metabolic Disease (6)

Neurological Disease (3)

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-136528

RA-9	Deubiquitinase Apoptosis	Cancer
RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells .

HY-136563

RA375	Proteasome Apoptosis Reactive Oxygen Species	Cancer
RA375 is a RPN13 (26S proteasome regulatory subunit) inhibitor. RA375 activates UPR signaling, ROS production and apoptosis. RA375 exhibits ten-fold greater activity against cancer lines than RA190, reflecting its nitro ring substituents and the addition of a chloroacetamide warhead .

HY-P99782

Opinercept	TNF Receptor	Inflammation/Immunology
Opinercept is a tumor necrosis factor-alpha (TNF-alpha) inhibitor. Opinercept can be used for the research of rheumatoid arthritis (RA) .

HY-118689

RA-2	Potassium Channel	Cardiovascular Disease Neurological Disease Inflammation/Immunology
RA-2 is a negative-gating modulator of KCa2/3 channels with an IC₅₀ of 17 nM. RA-2 inhibits bradykinin-induced endothelium-derived hyperpolarization (EDH)-type relaxation in U46619-precontracted rings. RA-2 can help to define the physiologic and pathomechanistic roles of KCa2/3 in the vasculature, central nervous system, and during inflammation .

HY-107644

AQ-RA 741	mAChR	Cardiovascular Disease
AQ-RA 741 is a potent and selective M 2 antagonist. AQ-RA 741 inhibits the vagally or agonist-induced bradycardia in rats, cats and guinea-pigs. AQ-RA 741 is used in bradycardiac disorders research .

HY-154962

Mcl-1 inhibitor 15

Bcl-2 Family Cancer

Mcl-1 inhibitor 15 (Compound (Ra)-15) is a Mcl-1 inhibitor (K_i: 0.02 nM). Mcl-1 inhibitor 15 can be used for research of cancer .

*Mcl-1 inhibitor* 15**	Bcl-2 Family	Cancer
Mcl-1 inhibitor 15 (Compound (Ra)-15) is a Mcl-1 inhibitor (K_i: 0.02 nM). Mcl-1 inhibitor 15 can be used for research of cancer .

HY-154961

*Mcl-1 inhibitor* 14**	Bcl-2 Family	Cancer
Mcl-1 inhibitor 14 (Compound (Ra)-10) is an inhibitor of myeloid cell leukemia-1 (MCL-1) with an K_i of 0.018 nM and can be used for anticancer research .

HY-106019C

Liarozole dihydrochloride R75251 dihydrochloride	Cytochrome P450 RAR/RXR	Metabolic Disease Inflammation/Immunology Cancer
Liarozole (R75251) dihydrochloride is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole dihydrochloride inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of RA (IC₅₀=7 μM), resulting in increased tissue levels of RA. Liarozole dihydrochloride shows antitumoral properties .

HY-18099A

S1RA hydrochloride 1 Publications Verification E-52862 hydrochloride	Sigma Receptor 5-HT Receptor	Neurological Disease
S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a K_i value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (K_i >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC₅₀ value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization .

HY-110275

RA839	Keap1-Nrf2	Others
RA839 is a noncovalent small molecule binder to Keap1 with a K_d of ∼6 μM and selective activator of Nrf2 signaling. RA839 prevents the induction of both inducible nitric-oxide synthase expression and nitric oxide release in response to lipopolysaccharides in macrophages. RA839 is a selective inhibitor of the Keap1/Nrf2 interaction and a useful tool compound to study the biology of Nrf2 .

HY-100739

RA190 3 Publications Verification	Proteasome	Cancer
RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.

HY-N2506

Ginsenoside Ra1

Others Cardiovascular Disease

Ginsenoside Ra1 is a component from ginseng, inhibits protein tyrosine kinase (PTK) activation induced by hypoxia/reoxygenation .

Ginsenoside Ra1	Others	Cardiovascular Disease
Ginsenoside Ra1 is a component from ginseng, inhibits protein tyrosine kinase (PTK) activation induced by hypoxia/reoxygenation .

HY-108522

PA452 1 Publications Verification	RAR/RXR	Metabolic Disease
PA452, retinoic X receptor (RXR) specific antagonist, inhibits the effect of Retinoic acid (RA) on Th1/Th2 development .

HY-135376

Atorvastatin methyl ester	Others	Metabolic Disease
Atorvastatin methyl ester (Compound 2a) is a methyl esterified derivative of Atorvastatin. Atorvastatin methyl ester inhibits the 9-cis-RA-induced Gal4 reporter activity more strongly than Atorvastatin .

HY-101671

S-methyl-KE-298 M-2	MMP Drug Metabolite	Inflammation/Immunology
S-methyl-KE-298 is an active metabolite of KE-298. KE-298 inhibits matrix metalloproteinase (MMP-1) production from rheumatoid arthritis (RA) synovial cells.

HY-P3502

Zilucoplan Ra101495; Ra3193	Complement System	Inflammation/Immunology
Zilucoplan (RA101495), a 15-amino acid macrocyclic peptide, is a potent complement component 5 (C5) inhibitor. Zilucoplan can be used in research of immune-mediated necrotising myopathy (IMNM) .

HY-P3502A

Zilucoplan TFA Ra101495 TFA; Ra3193 TFA	Complement System	Inflammation/Immunology
Zilucoplan TFA (RA101495), a 15-amino acid macrocyclic peptide, is a potent complement component 5 (C5) inhibitor. Zilucoplan TFA can be used in research of immune-mediated necrotising myopathy (IMNM) .

HY-147264

Edecesertib GS-5718	IRAK	Inflammation/Immunology
Edecesertib (GS-5718) is a selective, potent, orally active IRAK-4 inhibitor. Edecesertib has anti-inflammatory activity. Edecesertib can be used for rheumatoid arthritis (RA) and lupus erythematosus (LE) research .

HY-125415

PF-4693627	PGE synthase	Inflammation/Immunology
PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC₅₀=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA) .

HY-10291

Tarenflurbil 2 Publications Verification (R)-Flurbiprofen; MPC7869	RAR/RXR Autophagy	Neurological Disease Inflammation/Immunology
Tarenflurbil ((R)-Flurbiprofen) is the R-enantiomer of the racemate NSAID Flurbiprofen, Tarenflurbil ((R)-Flurbiprofen) inhibits the binding of [ ³H]9-cis-RA to RXRα LBD with IC₅₀ of 75 μM. Tarenflurbil can be used for Alzheimer's disease research.

HY-111532

(3R,4R)-A2-32-01 1 Publications Verification	ClpP Bacterial	Infection
(3R,4R)-A2-32-01 (compound 24(R,R)), the (R,R)-enantiomer of A2-32-01, is a Staphylococcus aureus caseinolytic protease (SaClpP) inhibitor .

HY-126114

Lupeol acetate 1 Publications Verification	COX Interleukin Related	Inflammation/Immunology
Lupeol acetate, a derivative of Lupeol, suppresses the progression of rheumatoid arthritis (RA) by inhibiting the activation of macrophages and osteoclastogenesis through downregulations of TNF-α, IL-1β, MCP-1, COX-2, VEGF and granzyme B .

HY-18300A

Filgotinib maleate GLPG0634 maleate	JAK	Inflammation/Immunology
Filgotinib (maleate) is a selective and orally active JAK1 inhibitor with IC₅₀ of 10 nM, 28 nM, 810 nM and 116 nM for JAK1, JAK2, JAK3 and TYK2, respectively. Filgotinib (maleate) can be used for rheumatoid arthritis (RA) and Crohn's disease research .

HY-110159

(E/Z)-Teriflunomide (E/Z)-A77 1726	Dihydroorotate Dehydrogenase	Infection Inflammation/Immunology
(E/Z)-Teriflunomide ((E/Z)-A77 1726) is the active metabolite of Leflunomide (HY-B0083). Leflunomide is an immunomodulatory agent that may exert effects by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase (DHODH). Leflunomide can be used for the research of rheumatoid arthritis (RA) .

HY-151472

hCAIX/XII-IN-6	Carbonic Anhydrase	Infection
hCAIX/XII-IN-6 is an orally active carbonic anhydrase (CA) inhibitor. hCAIX/XII-IN-6 inhibits human CA isoforms hCA I, II, IV, IX, and XII with K_i values of 6697 nM, 2950 nM, 4093 nM, 4.1 nM and 7.7 nM, respectively. hCAIX/XII-IN-6 can be used for the research of rheumatoid arthritis (RA) .

HY-14531

Talarozole Maximum Cited Publications 18 Publications Verification R115866	RAR/RXR Cytochrome P450 Autophagy	Inflammation/Immunology
Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC₅₀s of 5.4 and 0.46 nM, respectively.

HY-152035

Mycobacterial Zmp1-IN-1	Bacterial	Infection Inflammation/Immunology
Mycobacterial Zmp1-IN-1 is a mycobacterial zinc metalloprotease-1 (Zmp1) inhibitor. Mycobacterial Zmp1-IN-1 has anti-mycobacterial activity for Mtb H37Ra in dose-dependent inhibition. Mycobacterial Zmp1-IN-1 can be used for the research of tuberculosis (TB) .

HY-155031

MCI	Reactive Oxygen Species COX	Inflammation/Immunology
MCI alleviates inflammation by macrophage reprogramming via targeting ROS scavenging and COX-2 downregulation. MCI inhibits COX-2 with an IC₅₀ value of 1.23 μM. MCI has significant anti-inflammatory effects in collagen-induced arthritis (CIA) models. MCI can be used in research for rheumatoid arthritis (RA) .

HY-103046

UbcH5c-IN-1	E1/E2/E3 Enzyme	Inflammation/Immunology
UbcH5c-IN-1 (compound 6d) is a potent and selective small-molecule inhibitor of Ubiquitin-conjugating enzyme UbcH5c, with a K_d of 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85. A promising lead compound for the development of new antirheumatoid arthritis (RA) agent .

HY-118530

Bucillamine SA96; Thiobutarit	VEGFR	Cardiovascular Disease Inflammation/Immunology
Bucillamine (SA96) is an orally active and potent sulfhydryl donor and antioxidant. Bucillamine is also an antirheumatic agent with antiangiogenic properties. Bucillamine can protect against Ischemia/reperfusion (I/R) injury in high-risk organ transplants. Bucillamine inhibits the production of VEGF. Bucillamine can be used for the research of choroidal neovascularization (CNV) and rheumatoid arthritis (RA) .

HY-100707

IC 86621
IC 86621 is a potent DNA-dependent protein kinase (DNA-PK) inhibitor, with an IC₅₀ of 120 nM. IC 86621 also acts as a selective and reversible ATP-competitive inhibitor.IC 86621 inhibits DNA-PK mediated cellular DNA double-strand break (DSB) repair (EC₅₀=68 µM). IC 86621 increases DSB-induced antitumor activity without cytotoxic effects. IC 86621 can protects rheumatoid arthritis (RA) T cells from apoptosis .

HY-106019

Liarozole R75251	Cytochrome P450 RAR/RXR	Metabolic Disease Inflammation/Immunology Cancer
Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC₅₀=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties .

HY-P99259

Cabiralizumab FPA 008; Anti-Human CSF1R Recombinant Antibody	c-Fms	Inflammation/Immunology Cancer
Cabiralizumab (FPA 008) is an anti-CSF1R monoclonal antibody (MAb). Cabiralizumab enhances T cell infiltration and antitumor T cell immune responses. Cabiralizumab inhibits the activation of osteoclasts and blocks bone destruction, and can be used in the research of rheumatoid arthritis (RA). Cabiralizumab can combine with Nivolumab (HY-P9903) for lung cancer research .

HY-104017

DMT-2'-O-MOE-rA(Bz) phosphoramidite	Nucleoside Antimetabolite/Analog	Cancer
DMT-2'-O-MOE-rA(Bz) phosphoramidite is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277) .

HY-149581

DprE1-IN-9	Bacterial	Infection
DprE1-IN-9 (compound B18) is an effective reversible DprE1 inhibitor and can bind to the receptor cavity of DprE1. DprE1-IN-9 shows strong antimycobacterial activity not only against non-pathogenic strain H37Ra (MIC=0.18 µg/mL) but also against pathogenic H37Rv and the clinical MDR and XDR isolates .

HY-N0142

Phloretin 10+ Cited Publications NSC 407292; RJC 02792	SGLT Endogenous Metabolite GLUT	Metabolic Disease Cancer
Phloretin (NSC 407292; RJC 02792) is a flavonoid extracted from Malus pumila Mill., has anti-inflammatory activities. Phloridzin is a specific, competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). Phloretin inhibits Yeast-made GLUT1 as well as Human erythrocyte GLUT1 with IC₅₀values of 49 μM and 61 μM, respectively .Phloretin has the potential for the treatment of rheumatoid arthritis (RA) and allergic airway inflammation .

HY-P99252

Itolizumab Anti-Human CD6 Recombinant Antibody	CD6	Infection Inflammation/Immunology
Itolizumab (Anti-Human CD6 Recombinant Antibody) is a humanized recombinant anti-CD6 monoclonal antibody (MAb) targeting the extracellular SRCR distal domain 1 of CD6. Itolizumab reduces T-cell proliferation and inhibits the production of pro-inflammatory cytokines, such as INF-γ, TNFα and IL-6. Itolizumab can be used in the research of psoriasis, rheumatoid arthritis (RA), COVID-19 .

HY-125099

AFM-30a	Protein Arginine Deiminase	Inflammation/Immunology Cancer
AFM-30a is a potent protein arginine deiminase 2 (PAD2) inhibitor and has excellent PAD2-selectivity. AFM-30a binds to PAD2 with an EC₅₀ value of 9.5 μM. AFM-30a also inhibits H3 citrullination with an EC₅₀ value of 0.4 μM. AFM-30a can be used for the research of certain cancers and a variety of autoimmune diseases including rheumatoid arthritis (RA), multiple sclerosis, lupus, and ulcerative colitis .

HY-125099A

AFM-30a hydrochloride	Protein Arginine Deiminase	Inflammation/Immunology Cancer
AFM-30a hydrochloride is a potent protein arginine deiminase 2 (PAD2) inhibitor and has excellent PAD2-selectivity. AFM-30a hydrochloride binds to PAD2 with an EC₅₀ value of 9.5 μM. AFM-30a hydrochloride also inhibits H3 citrullination with an EC₅₀ value of 0.4 μM. AFM-30a hydrochloride can be used for the research of certain cancers and a variety of autoimmune diseases including rheumatoid arthritis (RA), multiple sclerosis, lupus, and ulcerative colitis .

HY-N0142R

Phloretin (Standard) NSC 407292 (Standard); RJC 02792 (Standard)	SGLT Endogenous Metabolite GLUT	Metabolic Disease Cancer
Phloretin (Standard) is the analytical standard of Phloretin. This product is intended for research and analytical applications. Phloretin (NSC 407292; RJC 02792) is a flavonoid extracted from Malus pumila Mill., has anti-inflammatory activities. Phloridzin is a specific, competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). Phloretin inhibits Yeast-made GLUT1 as well as Human erythrocyte GLUT1 with IC₅₀values of 49 μM and 61 μM, respectively .Phloretin has the potential for the treatment of rheumatoid arthritis (RA)?and allergic airway inflammation .

HY-147141

HS-276	IRAK TNF Receptor	Inflammation/Immunology
HS-276 is an orally active, potent and highly selective TAK1 inhibitor, with a K_i of 2.5 nM. HS-276 shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC₅₀ values of 8.25, 29, 33, 63, 125, 264, 270, 810, 1280, and 5585 nM, respectively. HS-276 can be used for rheumatoid arthritis (RA) research .

HY-147972

NF-κB/MAPK-IN-1	NF-κB p38 MAPK NO Synthase COX	Inflammation/Immunology
NF-κB/MAPK-IN-1 (compound 11a) is a potent inhibitor of NF-κB and MAPK pathway. NF-κB/MAPK-IN-1 shows inhibitory activity against NO production, with an IC₅₀ of 6.96 µM. NF-κB/MAPK-IN-1 suppresses LPS-induced iNOS, COX-2, ERΚ and P38 signaling activation. NF-κB/MAPK-IN-1 can prevent LPS induced inflammatory response in macrophages. NF-κB/MAPK-IN-1 can be used for rheumatoid arthritis (RA) research .

HY-15898

Y-320 3 Publications Verification	Interleukin Related Apoptosis	Inflammation/Immunology Cancer
Y-320 is a potent, orally active phenylpyrazoleanilide immunomodulator. Y-320 inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC₅₀ values of 20 to 60 nM. Y-320 enhances TP53, DMD, and COL17A1 PTC readthrough by G418 and increases cellular protein levels and protein synthesis. Y-320 concomitants use of with a low dose of Paclitaxel (HY-B0015) significantly sensitized multidrug resistance (MDR) tumors by inducing G2/M phase arrest and apoptosis. Y-320 can be used for research of rheumatoid arthritis (RA) and cancer .

Differentiation Inducing Compound Library	1436 compounds
Stem cells, which are found in all multi-cellular organisms, can divide and differentiate into diverse special cell types and can self-renew to produce more stem cells. To be useful in therapy, stem cells must be converted into desired cell types as necessary which is called induced differentiation or directed differentiation. Understanding and using signaling pathways for differentiation is an important method in successful regenerative medicine. Small molecules or growth factors induce the conversion of stem cells into appropriate progenitor cells, which will later give rise to the desired cell type. There is a variety of signal molecules and molecular families that may affect the establishment of germ layers in vivo, such as fibroblast growth factors (FGFs); the wnt family or superfamily of transforming growth factors β (TGFβ) and bone morphogenetic proteins (BMP). Unfortunately, for now, a high cost of recombinant factors is likely to limit their use on a larger scale in medicine. The more promising technique focuses on the use of small molecules. These small molecules can be used for either activating or deactivating specific signaling pathways. They enhance reprogramming efficiency by creating cells that are compatible with the desired type of tissue. It is a cheaper and non-immunogenic method. MCE Differentiation Inducing Compound Library contains a unique collection of 1436 compounds that act on signaling pathways for differentiation. These compounds are potential stimulators for induced differentiation. This library is a useful tool for researching directed differentiation and regenerative medicine.

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