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IRE1α/XBP1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	IRE1 (15) Antibiotic (1) Apoptosis (3) Arrestin (1) Autophagy (1) c-Kit (1) Caspase (1) CDK (1) CHIKV (1) Ferroptosis (3) FGFR (1) Fungal (1) Glutathione Peroxidase (3) HIV (1) Isotope-Labeled Compounds (1) Keap1-Nrf2 (3) MyD88 (1) PDGFR (1) Pyroptosis (1) Reactive Oxygen Species (ROS) (1) Reference Standards (1) Toll-like Receptor (TLR) (1)
By Research Areas:	Cancer (9) Infection (3) Inflammation/Immunology (2) Metabolic Disease (3) Neurological Disease (1)
Oligonucleotides:	CpG ODNs (1)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Oligonucleotides

Targets Recommended: IRE1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-103248

Toyocamycin 5+ Cited Publications Vengicide	IRE1 Fungal Antibiotic Apoptosis CDK	Infection Cancer
Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an *XBP1* inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC₅₀ value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC₅₀ value of 79 nM ^[1] .

HY-W018161

Hexadecanedioic acid 1 Publications Verification Thapsic acid	IRE1 Ferroptosis Keap1-Nrf2 Glutathione Peroxidase	Metabolic Disease
Hexadecanedioic acid (Thapsic acid) is an orally active metabolite produced by B. uniformis. Hexadecanedioic acid inhibits *IRE1α-XBP1s*-mediated flipogenesis and ferroptosis. Hexadecanedioic acid downregulates XBP1 and Hrd1 expression, activates the Nrf2/SLC7A11/GPX4 pathway. Hexadecanedioic acid can be used for the research of metabolic-associated fatty liver disease ^[1].

HY-18509

IRE1α kinase-IN-2 1 Publications Verification	IRE1	Cancer
IRE1α kinase-IN-2 is a potent IRE1α kinase inhibitor, with an EC₅₀ of 0.82 μM. IRE1α kinase-IN-2 inhibits IRE1α kinase autophosphorylation (IC₅₀=3.12 μM). IRE1α kinase-IN-2 inhibits XBP1 mRNA splicing in the WT cell lines ^[1].

HY-160229

ssRNA40 sodium R-1075 sodium	Toll-like Receptor (TLR) MyD88 Caspase Reactive Oxygen Species (ROS) Autophagy Pyroptosis HIV	Infection Neurological Disease
ssRNA40 sodium (R-1075 sodium) is a single-stranded RNA40 derived from HIV-1. ssRNA40 sodium activates the TLR7, TLR8, TLR2, RIG-I, MDA5, MyD88, Caspase-3, *IRE1α, NLRP3* inflammasome and IRF7 signaling pathways. ssRNA40 sodium alters mRNA expression in neutrophils, induces pro-inflammatory cytokines, ROS, autophagy (autophagy), pyroptosis (pyroptosis), neuronal death, neurodegeneration, aggregate formation and NK cell activation. ssRNA40 sodium activates the expression of CD62L, CD11b, CD69, *MX1, OAS1, ATG7, LC3B* and *XBP1* in immune cell and neuronal populations. ssRNA40 sodium causes cortical neuron loss and axonal damage in mice in a TLR7-dependent manner. ssRNA40 sodium can be used in research on *HIV-1* infection, neurodegeneration, COVID-19 and HIV-associated neurological disorders ^[1] .

HY-145425

PAIR2	IRE1 Apoptosis FGFR	Inflammation/Immunology
PAIR2 is a highly selective inhibitor targeting the kinase domain of human *IRE1α, with a K_i* value of 8.8 nM against human *IRE1α. PAIR2 fully occupies the ATP-binding site of the IRE1α* kinase domain, partially antagonizes the ribonuclease activity of IRE1α, specifically inhibits regulated IRE1α-dependent decay (RIDD) and its mediated substrate cleavage, while preserving the splicing function of *Xbp1* mRNA. PAIR2 also promotes the differentiation of B cells into plasma cells, blocks IRE1α-induced cell apoptosis, and restores the expression of Fgfr2 mRNA in AT2 cells. PAIR2 effectively reaches a steady-state concentration in the lung tissues of Mus musculus, and serves as an important tool for investigating the function of the IRE1α signaling pathway in diseases such as pulmonary fibrosis ^[1] .

HY-178946

IA107	IRE1	Cancer
IA107 is a potent, selective, and allosteric *IRE1α* RNase (IC₅₀ = 16 nM (non phosphorylated), IC₅₀ = 9 nM (phosphorylated)) inhibitor. IA107 can inhibit endoplasmic reticulum stress-induced XBP1 mRNA splicing and protein expression, and has no cytotoxicity ^[1].

HY-161672

G-5758	IRE1	Cancer
G-5758 is a selective and orally effective *IRE1α* inhibitor with an IC₅₀ of 38 nM (detected by the XBP1s luciferase reporter cell assay). G-5758 is still well tolerated in rats at oral doses up to 500 mg/kg. G-5758 can be used in the research of multiple myeloma ^[1].

HY-124646

KIRA-7	IRE1	Inflammation/Immunology
KIRA-7, an imidazopyrazine compound, binds the IRE1α kinase (IC₅₀ of 110 nM) to allosterically inhibit its RNase activity. KIRA-7 has an anti-fibrotic effect ^[1].

HY-U00460

3,6-DMAD hydrochloride 1 Publications Verification	IRE1	Cancer
3,6-DMAD hydrochloride, an acridine derivative, is a potent *IRE1α-XBP1s* pathway inhibitor. 3,6-DMAD hydrochloride promotes IL-6 secretion via the IRE1α-XBP1s pathway. 3,6-DMAD hydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD hydrochloride can be used for research of cancer ^[1] .

HY-158386

IRE1a-IN-1	IRE1	Cancer
IRE1a-IN-1 (Compound 10) is an *IRE1α* inhibitor, with an IC₅₀ of less than 100 nM for XBP1 mRNA. IRE1a-IN-1 can be used for the research of cancer ^[1].

HY-U00460B

3,6-DMAD dihydrochloride	IRE1	Cancer
3,6-DMAD dihydrochloride, an acridine derivative, is a potent *IRE1α-XBP1s* pathway inhibitor. 3,6-DMAD dihydrochloride promotes IL-6 secretion via the IRE1α-XBP1s pathway. 3,6-DMAD dihydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD dihydrochloride can be used for research of cancer ^[1] .

HY-158393

IRE1a-IN-2	IRE1	Cancer
IRE1a-IN-2 (Compound 30) is an *IRE1α* inhibitor, with an IC₅₀ of over than 200 nM for XBP1 mRNA. IRE1a-IN-2 can be used for the research of cancer ^[1].

HY-181886

AK177	IRE1 PDGFR c-Kit	Others
AK177 is an allosteric activator of *IRE1α* ribonuclease, with values of 480 nM and 180 nM against non-phosphorylated and phosphorylated IRE1α, respectively. AK177 promotes IRE1α-mediated cleavage of XBP1 mRNA probe in a concentration-dependent manner and binds stably to its kinase domain. However, AK177 shows poor kinase selectivity, and due to poor membrane permeability at the cellular level, it induces no significant downstream pathway activation or antiproliferative activity ^[1].

HY-W018161R

Hexadecanedioic acid (Standard) Thapsic acid (Standard)	Reference Standards IRE1 Ferroptosis Keap1-Nrf2 Glutathione Peroxidase	Metabolic Disease
Hexadecanedioic acid (Thapsic acid) (Standard) is the analytical standard of Hexadecanedioic acid (HY-W018161). This product is intended for research and analytical applications. Hexadecanedioic acid is an orally active metabolite produced by B. uniformis. Hexadecanedioic acid inhibits *IRE1α-XBP1s*-mediated flipogenesis and ferroptosis. Hexadecanedioic acid downregulates XBP1 and Hrd1 expression, activates the Nrf2/SLC7A11/GPX4 pathway. Hexadecanedioic acid can be used for the research of metabolic-associated fatty liver disease ^[1].

HY-W018161S

Hexadecanedioic acid-d28	Isotope-Labeled Compounds IRE1 Ferroptosis Keap1-Nrf2 Glutathione Peroxidase	Metabolic Disease
Hexadecanedioic acid-d₂₈ is the deuterium labeled Hexadecanedioic acid (HY-W018161). Hexadecanedioic acid (Thapsic acid) is an orally active metabolite produced by B. uniformis. Hexadecanedioic acid inhibits *IRE1α-XBP1s*-mediated flipogenesis and ferroptosis. Hexadecanedioic acid downregulates XBP1 and Hrd1 expression, activates the Nrf2/SLC7A11/GPX4 pathway. Hexadecanedioic acid can be used for the research of metabolic-associated fatty liver disease ^[1].

HY-123996

3-Ethoxy-5,6-dibromosalicylaldehyde	IRE1 Apoptosis Arrestin CHIKV	Infection Cancer
3-ethoxy-5,6-dibromosalicylaldehyde is a potent, non-competitive, selective *IRE1* (including IRE1α) inhibitor (IC₅₀s: ∼0.12 μM for hIRE1α-cyto; 6 μM for yeast Ire1). 3-ethoxy-5,6-dibromosalicylaldehyde inhibits *XBP-1* splicing. 3-ethoxy-5,6-dibromosalicylaldehyde induces Apoptosis. 3-ethoxy-5,6-dibromosalicylaldehyde upregulates the mRNA expression level of TXNIP, while downregulating the expression level of TXN. 3-ethoxy-5,6-dibromosalicylaldehyde exhibits anticancer activity against pancreatic cancer. 3-ethoxy-5,6-dibromosalicylaldehyde significantly inhibits chikungunya virus replication ^[1] .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-103248

Toyocamycin 5+ Cited Publications Vengicide	Infection Microorganisms Classification of Application Fields Antibiotics Antibacterial Disease Research Disease Research Fields Other Antibiotics Source Classification	IRE1 Fungal Antibiotic Apoptosis CDK
Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an *XBP1* inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC₅₀ value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC₅₀ value of 79 nM ^[1] .

HY-W018161

Hexadecanedioic acid 1 Publications Verification Thapsic acid	Structural Classification Human Gut Microbiota Metabolites Classification of Application Fields Ketones, Aldehydes, Acids Other Diseases Endogenous metabolite Disease Research Fields Source Classification	IRE1 Ferroptosis Keap1-Nrf2 Glutathione Peroxidase
Hexadecanedioic acid (Thapsic acid) is an orally active metabolite produced by B. uniformis. Hexadecanedioic acid inhibits *IRE1α-XBP1s*-mediated flipogenesis and ferroptosis. Hexadecanedioic acid downregulates XBP1 and Hrd1 expression, activates the Nrf2/SLC7A11/GPX4 pathway. Hexadecanedioic acid can be used for the research of metabolic-associated fatty liver disease ^[1].

HY-W018161R

Hexadecanedioic acid (Standard) Thapsic acid (Standard)	Structural Classification Human Gut Microbiota Metabolites Microorganisms Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	Reference Standards IRE1 Ferroptosis Keap1-Nrf2 Glutathione Peroxidase
Hexadecanedioic acid (Thapsic acid) (Standard) is the analytical standard of Hexadecanedioic acid (HY-W018161). This product is intended for research and analytical applications. Hexadecanedioic acid is an orally active metabolite produced by B. uniformis. Hexadecanedioic acid inhibits *IRE1α-XBP1s*-mediated flipogenesis and ferroptosis. Hexadecanedioic acid downregulates XBP1 and Hrd1 expression, activates the Nrf2/SLC7A11/GPX4 pathway. Hexadecanedioic acid can be used for the research of metabolic-associated fatty liver disease ^[1].

Cat. No.	Product Name	Chemical Structure

HY-W018161S

Hexadecanedioic acid-d28
Hexadecanedioic acid-d₂₈ is the deuterium labeled Hexadecanedioic acid (HY-W018161). Hexadecanedioic acid (Thapsic acid) is an orally active metabolite produced by B. uniformis. Hexadecanedioic acid inhibits *IRE1α-XBP1s*-mediated flipogenesis and ferroptosis. Hexadecanedioic acid downregulates XBP1 and Hrd1 expression, activates the Nrf2/SLC7A11/GPX4 pathway. Hexadecanedioic acid can be used for the research of metabolic-associated fatty liver disease ^[1].

Hexadecanedioic acid-d28

Hexadecanedioic acid-d₂₈ is the deuterium labeled Hexadecanedioic acid (HY-W018161). Hexadecanedioic acid (Thapsic acid) is an orally active metabolite produced by B. uniformis. Hexadecanedioic acid inhibits IRE1α-XBP1s-mediated flipogenesis and ferroptosis. Hexadecanedioic acid downregulates XBP1 and Hrd1 expression, activates the Nrf2/SLC7A11/GPX4 pathway. Hexadecanedioic acid can be used for the research of metabolic-associated fatty liver disease ^[1].

Cat. No.	Product Name		Classification

HY-160229

ssRNA40 sodium R-1075 sodium		CpG ODNs
ssRNA40 sodium (R-1075 sodium) is a single-stranded RNA40 derived from HIV-1. ssRNA40 sodium activates the TLR7, TLR8, TLR2, RIG-I, MDA5, MyD88, Caspase-3, *IRE1α, NLRP3* inflammasome and IRF7 signaling pathways. ssRNA40 sodium alters mRNA expression in neutrophils, induces pro-inflammatory cytokines, ROS, autophagy (autophagy), pyroptosis (pyroptosis), neuronal death, neurodegeneration, aggregate formation and NK cell activation. ssRNA40 sodium activates the expression of CD62L, CD11b, CD69, *MX1, OAS1, ATG7, LC3B* and *XBP1* in immune cell and neuronal populations. ssRNA40 sodium causes cortical neuron loss and axonal damage in mice in a TLR7-dependent manner. ssRNA40 sodium can be used in research on *HIV-1* infection, neurodegeneration, COVID-19 and HIV-associated neurological disorders ^[1] .

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