434

PD98059

434 Publications Verification

Cat. No.: HY-12028

CAS No.: 167869-21-8

Purity: 98.89%

Target:

MEK ERK Aryl Hydrocarbon Receptor Autophagy

Research Areas:

Cancer

PD98059 is a potent and selective MEK inhibitor with an IC₅₀ of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC₅₀ of 2-7 µM) and MEK2 (IC₅₀ of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC₅₀ of 4 μM) and AHR transformation (IC₅₀ of 1 μM). PD98059 also inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy ^[1] .

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163

Mirdametinib

163 Cited Publications

Cat. No.: HY-10254

CAS No.: 391210-10-9

Purity: 99.95%

Synonyms: PD0325901; PD325901

Target:

MEK Autophagy Apoptosis

Research Areas:

Cancer

Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC₅₀ of 0.33 nM. Mirdametinib exhibits a K_i ^app of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts ^[1] .

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154

Erlotinib Hydrochloride

154 Cited Publications

Cat. No.: HY-12008

CAS No.: 183319-69-9

Purity: 99.94%

Synonyms: CP-358774 hydrochloride; NSC 718781 hydrochloride; OSI-774 hydrochloride

Target:

EGFR OAT ERK GSK-3 β-catenin

Research Areas:

Endocrinology Cancer

Erlotinib (CP-358774) Hydrochloride is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib Hydrochloride also acts as a substrate and inhibitor of OATP2B1, with an IC₅₀ of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib Hydrochloride blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib Hydrochloride inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib Hydrochloride is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib Hydrochloride can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis ^[1] .

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154

Erlotinib

154 Cited Publications

Cat. No.: HY-50896

CAS No.: 183321-74-6

Synonyms: CP-358774; NSC 718781; OSI-774

Target:

EGFR OAT ERK GSK-3 β-catenin

Research Areas:

Endocrinology Cancer

Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC₅₀ of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, fibronectin, α-SMA, collagen deposition, and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, pancreatic cancer, renal fibrosis, and other conditions ^[1] .

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114

Tauroursodeoxycholate

114 Cited Publications

Cat. No.: HY-19696

CAS No.: 14605-22-2

Synonyms: Tauroursodeoxycholic acid; TUDCA; UR 906

Category:

Endogenous metabolite Disease Research Fields Cancer Steroids

Target:

ERK Caspase Endogenous Metabolite Apoptosis

Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an orally active endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK .

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103

Selumetinib

103 Cited Publications

Cat. No.: HY-50706

CAS No.: 606143-52-6

Synonyms: AZD6244; ARRY-142886

Target:

MEK Apoptosis

Research Areas:

Neurological Disease Metabolic Disease Inflammation/Immunology Cancer

Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC₅₀ of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation. Selumetinib can penetrate the blood brain barrier (BBB) ^[1] .

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103

Selumetinib sulfate

103 Cited Publications

Cat. No.: HY-50706A

CAS No.: 943332-08-9

Synonyms: AZD6244 sulfate; ARRY-142886 sulfate

Target:

MEK Apoptosis

Research Areas:

Neurological Disease Metabolic Disease Inflammation/Immunology Cancer

Selumetinib (AZD6244) sulfate is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC₅₀ of 14 nM for MEK1. Selumetinib (AZD6244) sulfate inhibits ERK1/2 phosphorylation. Selumetinib sulfate can penetrate the blood brain barrier (BBB) ^[1] .

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70

Leupeptin hemisulfate

70 Cited Publications

Cat. No.: HY-18234A

CAS No.: 103476-89-7

Category:

Natural Products Microorganisms Disease Research Fields Inflammation/Immunology

Target:

Ser/Thr Protease Cathepsin Autophagy SARS-CoV Atg8/LC3 NO Synthase COX p62 Arginase PTEN NF-κB PI3K Akt p38 MAPK ERK Reactive Oxygen Species (ROS)

Leupeptin hemisulfate is a broad-spectrum protease inhibitor . By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin hemisulfate significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin hemisulfate inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin hemisulfate can be used in research on chronic inflammatory diseases and skin tumorigenesis ^[1] .

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57

Ulixertinib hydrochloride

57 Cited Publications

Cat. No.: HY-15816A

CAS No.: 1956366-10-1

Purity: 99.89%

Synonyms: BVD-523 hydrochloride; VRT752271 hydrochloride

Target:

ERK

Research Areas:

Cancer

Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC₅₀ of <0.3 nM against ERK2. Ulixertinib hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line ^[1] .

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57

Ulixertinib

57 Cited Publications

Cat. No.: HY-15816

CAS No.: 869886-67-9

Purity: 99.95%

Synonyms: BVD-523; VRT752271

Target:

ERK

Research Areas:

Cancer

Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC₅₀ of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line ^[1] .

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52

Ravoxertinib

52 Cited Publications

Cat. No.: HY-15947

CAS No.: 1453848-26-4

Synonyms: GDC-0994

Target:

ERK Lactate Dehydrogenase Hexokinase c-Myc

Research Areas:

Cancer

Ravoxertinib (GDC-0994) is an orally active ERK1/2 inhibitor. Ravoxertinib inhibits the ERK1/2 MAPK signaling pathway and reduces the expression levels of c-Myc, HK2 and LDHA. Ravoxertinib decreases mammosphere formation, and exerts additive and/or superadditive cytotoxicity when combined with Ipatasertib (HY-15186) in 3D tumor sphere models. Ravoxertinib can be used in research related to various cancers including breast cancer, melanoma, head and neck cancer, non-small cell lung cancer, ovarian cancer and Merkel cell carcinoma ^[1] .

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52

Ravoxertinib hydrochloride

52 Cited Publications

Cat. No.: HY-15947A

CAS No.: 2070009-58-2

Synonyms: GDC-0994 hydrochloride

Target:

ERK Lactate Dehydrogenase Hexokinase c-Myc

Research Areas:

Cancer

Ravoxertinib hydrochloride (GDC-0994 hydrochloride) is an orally active ERK1/2 inhibitor. Ravoxertinib hydrochloride inhibits the ERK1/2 MAPK signaling pathway and reduces the expression levels of c-Myc, HK2 and LDHA. Ravoxertinib hydrochloride decreases mammosphere formation, and exerts additive and/or superadditive cytotoxicity when combined with Ipatasertib (HY-15186) in 3D tumor sphere models. Ravoxertinib hydrochloride can be used in research related to various cancers including breast cancer, melanoma, head and neck cancer, non-small cell lung cancer, ovarian cancer and Merkel cell carcinoma ^[1] .

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52

Idasanutlin

52 Cited Publications

Cat. No.: HY-15676

CAS No.: 1229705-06-9

Purity: 99.93%

Synonyms: RG7388

Target:

MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Pyroptosis Reactive Oxygen Species (ROS) Caspase

Research Areas:

Neurological Disease Cancer

Idasanutlin (RG7388) is an orally bioavailable MDM2 inhibitor with an IC₅₀ of 6 nM. Idasanutlin disrupts MDM2-p53 binding, stabilizes and activates p53, triggering cell cycle arrest, apoptosis, and reduced cancer cell viability. Idasanutlin reduces EGFR protein expression and phosphorylation, suppresses downstream SHP2, MEK1/2, ERK1/2, AKT, mTOR, p70(S6K1), and S6 signaling. Idasanutlin induces mitochondrial ROS production, drives p38 MAPK phosphorylation, upregulates NOXA, and mediates caspase-3-dependent apoptosis and gasdermin E-mediated pyroptosis. Idasanutlin can be used for the research of TP53-mutant non-small cell lung cancer, T-cell acute lymphoblastic leukemia, colorectal carcinoma, melanoma, diffuse large B-cell lymphoma, mantle cell lymphoma, non-Hodgkin lymphoma, severe fever with thrombocytopenia syndrome, neuroblastoma, acute lymphoblastic leukemia, relapsed or refractory acute myeloid leukemia, osteosarcoma, solid tumors, and hematological tumors ^[1] ^[12].

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