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Advancing the Application of Immunotherapy Targeting MAPK/ERK Signaling

Cancer Immunotherapy Tumor Microenvironment Cellular Stress Cell Programmed Death

The RAS–RAF–MEK–ERK pathway drives proliferation, survival, differentiation, and adaptation in many cancers. Targeted inhibitors can produce rapid tumor regression, but pathway reactivation and bypass signaling commonly limit durability. MAPK signaling also shapes tumor antigen expression, cytokines, stromal interactions, and immune-cell function, creating a rationale for combination with checkpoint blockade. The interaction is bidirectional: suppressing oncogenic MAPK can make tumor cells more visible or less suppressive, yet T cells also require MAPK signaling for activation. The therapeutic objective is therefore not maximal continuous pathway inhibition, but a schedule and target depth that restrain cancer while preserving or enhancing antitumor immunity Clinical interest intensified after targeted therapy was observed to change immune infiltration rapidly, creating a window before resistant clones restored pathway output[1][2][3].

Oncogenic MAPK activity can reduce antigen presentation, alter chemokines, increase immunosuppressive mediators, and support an immune-excluded microenvironment. BRAF or MEK inhibition may reverse some of these effects and increase T-cell infiltration in selected tumors. At the same time, MEK–ERK transduces signals downstream of the T-cell receptor and costimulatory receptors, so systemic inhibition can impair proliferation and cytokine production. Feedback relief activates receptor tyrosine kinases or alternative pathways, while SHP2 links several receptors to RAS and contributes to adaptive resistance and immune regulation. Drug class, tumor genotype, dose, and sequence determine which effect dominates MAPK output in myeloid and stromal cells can also regulate cytokines and antigen presentation, so immune effects cannot be assigned only to lymphocytes[1][2][3].

Applications are most developed in MAPK-driven melanoma and are being explored in triple-negative breast cancer and other solid tumors. Combinations may pair BRAF and MEK inhibitors with PD-1 or PD-L1 blockade, or use SHP2 inhibition to suppress RAS reactivation and remodel myeloid signaling. Overlapping hepatic, cutaneous, gastrointestinal, and inflammatory toxicities can narrow the therapeutic window. Intermittent or lead-in dosing may reduce tumor burden and improve antigen presentation before checkpoint therapy, whereas prolonged simultaneous inhibition may suppress lymphocytes. Molecular confirmation of pathway dependence is essential because a combination cannot overcome resistance driven by an unrelated oncogenic program Triple combinations may improve pathway coverage but increase discontinuation, making exposure actually delivered as important as the nominal regimen[1][2].

Future trials should integrate tumor phosphoproteomics, antigen presentation, circulating drug exposure, and immune-cell signaling. Paired biopsies can determine whether treatment increases intratumoral T cells or merely reduces tumor size. Adaptive designs may use early pathway and immune biomarkers to adjust schedule. Resistance studies should distinguish MAPK reactivation, alternate signaling, antigen loss, and checkpoint-independent immune exclusion. Cell-restricted delivery or degraders could separate tumor inhibition from T-cell effects. Targeting MAPK/ERK can advance immunotherapy when oncogenic signaling is a measurable cause of immune resistance, but durable benefit requires temporal control and mechanistic evidence that the combination improves immunity rather than simply adding two active drugs The strongest biomarker may combine oncogenic genotype with an on-treatment immune change, demonstrating both tumor dependence and successful microenvironmental remodeling. Dose optimization should consider pathway rebound between treatments, because intermittent release can restore T-cell function while also permitting malignant signaling to recover[1][2][3].

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Cat. No. Product Name Information Application Publication
HY-10071 Y-27632
Y-27632 is a ROCK inhibitor with Ki values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade.
ROCK   Reactive Oxygen Species (ROS)   Akt   Ras   mTOR   Apoptosis   PAK   NADPH Oxidase   NF-κB   Autophagy  
Cancer   Digestive System Disease   Digestive System Inflammation   Lung Fibrosis  
603
HY-12031 U0126-EtOH
U0126 (U0126-EtOH) is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor.
MEK   Autophagy   Mitophagy   Influenza Virus  
Colorectal Cancer   Liver Cancer   Pancreatic Cancer   Viral Infection   Pain   Digestive System Inflammation   Obesity   Rheumatoid Arthritis  
491
HY-12031A U0126
U0126 is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor.
MEK   Autophagy   Mitophagy   Influenza Virus  
Colorectal Cancer   Liver Cancer   Pancreatic Cancer   Viral Infection   Pain   Digestive System Inflammation   Obesity   Rheumatoid Arthritis  
491
HY-12028 PD98059
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.
MEK   ERK   Aryl Hydrocarbon Receptor   Autophagy  
Colorectal Cancer   Prostate Cancer   Liver Cancer   Pancreatic Cancer   Pain   Obesity   Lung Fibrosis   Rheumatoid Arthritis  
427
HY-10201 Sorafenib
Sorafenib (Bay 43-9006) is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.
Raf   VEGFR   FLT3   Autophagy   Apoptosis   STAT   Akt   MMP   Cadherin   p38 MAPK   ERK   MEK   PI3K   PARP   Bcl-2 Family   Ephrin Receptor   PDGFR  
Gastric Cancer   Liver Cancer   Ovarian Cancer   Digestive System Inflammation   Small Cell Lung Cancer   Non-Small Cell Lung Cancer   Metastatic Breast Cancer   Metastatic Colorectal Cancer   Metastatic Prostate Cancer   Multiple Myeloma   Metastatic Pancreatic Cancer   SARS-CoV-2 Infection   Alzheimer's Disease   Parkinson's Disease   Obesity   Lung Fibrosis  
316
HY-10999 Trametinib
Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis, cross the blood-brain barrier (BBB), used in research related to subarachnoid hemorrhage (SAH).
MEK   Autophagy   Apoptosis  
Breast Cancer   Colorectal Cancer   Prostate Cancer   Liver Cancer   Pancreatic Cancer   Pain   Digestive System Inflammation   Non-Small Cell Lung Cancer   Lung Adenocarcinoma   SARS-CoV-2 Infection   Obesity   Rheumatoid Arthritis  
307
HY-50846 SCH772984
SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naive and MAPK inhibitor-resistant cells containing BRAF or RAS mutations.
ERK  
Colorectal Cancer   Prostate Cancer   Liver Cancer   Pancreatic Cancer   Pain  
202
HY-10254 Mirdametinib
Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. Mirdametinib exhibits a Kiapp 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.
MEK   Autophagy   Apoptosis  
Colorectal Cancer   Liver Cancer   Pancreatic Cancer   Pain   Digestive System Inflammation   Obesity   Rheumatoid Arthritis  
161
HY-50896 Erlotinib
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.
EGFR   OAT   ERK   GSK-3   β-catenin  
Gastric Cancer   Pancreatic Cancer   Renal Disease   Non-Small Cell Lung Cancer   Lung Adenocarcinoma  
147
HY-114277 Sotorasib
Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC).
Ras  
Lung Cancer   Colorectal Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer  
125
HY-18723 Yoda 1
Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca2+ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation.
Piezo Channel   Akt   ERK   Potassium Channel  
Pancreatic Cancer   Depression   Pain   Digestive System Inflammation   Cardiovascular Disease   Lung Fibrosis  
120
HY-19696 Tauroursodeoxycholate
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.
ERK   Caspase   Endogenous Metabolite   Apoptosis  
Colorectal Cancer   Prostate Cancer   Liver Cancer   Viral Infection   Neurodegenerative Disease   Pain   Digestive System Inflammation   Glucose Metabolism   Obesity  
111
HY-12057 Vemurafenib
Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively. Vemurafenib induces cell autophagy.
Raf   Autophagy  
Colorectal Cancer   Prostate Cancer   Liver Cancer   Pancreatic Cancer   Obesity  
105
HY-50706 Selumetinib
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).
MEK   Apoptosis  
Colorectal Cancer   Liver Cancer   Pancreatic Cancer   Pain   Digestive System Inflammation   Non-Small Cell Lung Cancer   Triple-Negative Breast Cancer   Metastatic Breast Cancer   Obesity   Rheumatoid Arthritis  
101
HY-10331 Regorafenib
Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity.
VEGFR   Autophagy   PDGFR   Raf   RET   c-Kit   FGFR   Tie  
Lung Cancer   Breast Cancer   Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   SARS-CoV-2 Infection   Obesity   Lung Fibrosis  
96
HY-L010 MAPK Compound Library
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 1,154 MAPK signaling pathway inhibitors that act as a useful tool for MAPK-related drug screening and disease research.

Signaling Pathway Targeting Libraries

88
HY-14590 Kaempferol
Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK. Kaempferol can be uesd for the research of breast cancer.
Estrogen Receptor/ERR   Autophagy   Mitophagy   Apoptosis   HIV   Parasite   Endogenous Metabolite  
Digestive System Disease   Lung Cancer   Breast Cancer   Ovarian Cancer   Viral Infection   Parasitic Infection   Digestive System Inflammation   Glucose Metabolism  
85
HY-L077 Anti-Pancreatic Cancer Compound Library
Pancreatic cancer is a devastating disease with a low overall survival rate. Chemotherapy is the most common treatment for patients presenting with advanced pancreatic cancer. More recently, the era of targeted therapies has generated a lot of interest in discovering better approaches for patients with pancreatic cancer. Commonly mutated genes in pancreatic cancer include K-ras (in 74-100% of cases), p16INK4a (up to 98%), p53 (43 to 76%), DPC4 (about 50%), HER-2/neu (in about 65%) and FHIT (found in 70% of cases). Other genes involved are notch1, Akt-2, BRCA2 and COX-2. These proteins are important targets of target therapies for pancreatic cancer. MCE offers a unique collection of 4,336 compounds with identified and potential anti- pancreatic cancer activity. These compounds target K-Ras, p53, HER2, Notch, AKT, etc. MCE anti-pancreatic cancer compound library is a useful tool for anti-pancreatic cancer drugs screening and other related research.

Disease Focused Libraries

85
HY-14660 Dabrafenib
Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively.
Raf   CDK  
Colorectal Cancer   Prostate Cancer   Liver Cancer   Pancreatic Cancer   Non-Small Cell Lung Cancer  
84
HY-L075 Anti-Lung Cancer Compound Library
Lung cancer is a major global health problem, as it is the leading cause of cancer-related deaths worldwide. Lung cancer is divided into two categories: small cell lung cancer and non-small cell lung cancer (NSCLC). Non-small cell lung cancer accounts for about 85 percent of lung cancers. As with all cancers, lung cancer may be treated with surgery, chemotherapy, radiation therapy, targeted therapy, immunotherapy or a combination thereof. Targeted therapy is one of the most exciting developments in lung cancer medicine, especially for NSCLC. Extensive genomic characterization of NSCLC has led to the identification of molecular subtypes of NSCLC that are oncogene addicted and exquisitely sensitive to targeted therapies. These include activating mutations in epidermal growth factor receptor (EGFR) and BRAF or echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase (ALK) fusions and ROS1 receptor tyrosine kinase fusions. These are important targets for target therapy. MCE offers a unique collection of 3,061 compounds with identified and potential anti-lung cancer activity. These compounds target lung cancer’s major targets and signaling pathways. MCE anti-lung cancer compound library is a useful tool for anti-lung cancer drugs screening and other related research.

Disease Focused Libraries

84
HY-L045 Oxygen Sensing Compound Library
Oxygen homeostasis regulation is the most fundamental cellular process for adjusting physiological oxygen variations, and its irregularity leads to various human diseases, including cancer. Hypoxia is closely associated with cancer development, and hypoxia/oxygen-sensing signaling plays critical roles in the modulation of cancer progression. Hypoxia-inducible factor 1 (HIF-1) is a transcription factor that functions as a master regulator of oxygen homeostasis. A variety of HF-1 target genes have been identified thus far which encode proteins that play key roles in critical developmental and physiological processes including angiogenesis/vascular remodeling, erythropoiesis, glucose transport, glycolysis, iron transport, and cell proliferation/survival. HIF-1 is a heterodimeric transcription factor consisting of a constitutively expressed β-subunit and an oxygen-regulated α-subunit. The unique feature of HIF-1 is the regulation of HIF-1α expression and activity based upon the cellular O2 concentration. Under normoxic conditions, hydroxylation of HIF-1α on these different proline residues is essential for HIF proteolytic degradation by promoting interaction with the von Hippel-Lindau tumor-suppressor protein (pVHL) through hydrogen bonding to the hydroxyproline-binding pocket in the pVHL β-domain. As oxygen levels decrease, hydroxylation of HIF decreases; HIF-1α then no longer binds pVHL, and becomes stabilized, allowing more of the protein to translocate to the cell’s nucleus, where it acts as a transcription factor, upregulating (often within minutes) the production of proteins that stimulate blood perfusion in tissues and thus tissue oxygenation. MCE offers a unique collection of 4,317 oxygen sensing related compounds targeting HIF/HIF Prolyl-Hydroxylase, MAPK/ERK, PI3K/AKT signaling pathways, etc. MCE Oxygen Sensing Compound Library is a useful tool to study hypoxia, oxidative stress and discover new anti-cancer drugs.

Signaling Pathway Targeting Libraries

83
HY-L079 Anti-Blood Cancer Compound Library
Blood cancers, also called hematologic cancers, occur when abnormal blood cells start growing out of control, interrupting the function of normal blood cells, which fight off infection and produce new blood cells. Most blood cancers start in the bone marrow, which is where blood is produced. There are three main types of blood cancers: leukemia, lymphoma and myeloma, which afflict millions of children and adults every year, and are often deadly. Some common blood cancer treatments include stem cell transplantation, chemotherapy, radiation therapy, targeted therapy, immunotherapy or a combination thereof. As we begin to understand the key signaling pathways and molecular drivers of malignant transformation in haematological disorders, new treatment strategies will continue to be developed. MCE offers a unique collection of 4,333 compounds with identified and potential anti-blood cancer activity. These compounds target blood cancer’s major targets and signaling pathways. MCE anti-blood cancer compound library is a useful tool for anti-blood cancer drugs screening and other related research.

Disease Focused Libraries

83
HY-L145 Antihypertensive Compound Library
The majority of hypertensive patients have primary (or essential) hypertension, that is, hypertension in which secondary causes are not present. Management aims to control arterial pressure, prevent end-organ damage (cerebrovascular, cardiovascular, and renal), and reduce the risk of premature death. Antihypertensive drugs may be divided into two broad groups, the first group being those which directly or indirectly block the renin–angiotensin system (RAS), for example, ACEIs, angiotensin receptor antagonists (ARAs), direct renin inhibitors (DRIs), and to a lesser extent β-blockers. The second group of drugs works by increasing water and sodium excretion, thereby reducing intravascular volume, or by causing vasodilatation through non-RAS pathways, for example, diuretics and calcium channel blockers (CCBs). MCE offers a unique collection of 930 compounds with identified and potential antihypertensive activity. MCE Antihypertensive Compound Library is critical for antihypertensive drug discovery and development.

Disease Focused Libraries

83
HY-L164 Serine/Threonine Kinase Inhibitor Library
Protein serine/threonine kinases (PSKs) are protein kinases that use ATP as a high-energy donor molecule to transfer phosphate groups to serine/threonine residues of target protein. As an important signal transduction regulator, serine/threonine kinases can affect the function of target proteins by disrupting enzyme activity or binding of target proteins to other proteins. Serine/threonine kinases are involved in the regulation of immune response, cell proliferation, differentiation, apoptosis and other physiological processes. Serine/threonine kinase inhibitors are an important class of compounds that have been widely studied in cancer, chronic inflammation, autoimmune diseases, aging and other diseases. MCE designs a unique collection of 2,276 serine/threonine kinase inhibitors, mainly targeting the receptor PKA, Akt, PKC, MAPK/ERK, etc, which is an effective tool for development and research of anti-cancer, anti-chronic inflammatory diseases, anti-autoimmune diseases and anti-aging compounds.

Signaling Pathway Targeting Libraries

83
HY-L213 Anti-Cancer Approved Drug Library
The anti-cancer drug library meticulously collects all drugs approved by FDA and other major national drug regulatory authorities for cancer treatment. These drugs cover a variety of cancer types, including but not limited to lung cancer, breast cancer, colorectal cancer, leukemia, and other common cancers. The library includes a wide range of drugs, from classic chemotherapeutic agents to cutting-edge targeted therapies and immunotherapies. It contains various types of drug compounds with different mechanisms of action. There are cytotoxic drugs that directly kill cancer cells, as well as drugs that work by modulating the tumor microenvironment, inhibiting tumor angiogenesis, and activating the immune system. This diversity provides researchers with a broad range of perspectives and options for intervention strategies. This library can be used for basic research on cancer treatment, exploring new targets and new mechanisms of drug action; Conducting drug reuse research to look for potential therapeutic effects of existing drugs on other cancer types or diseases; Or conducting research into combination drugs to optimize cancer treatment. MCE has collected 265 small-molecule compounds with cancer indications, which are good tools for drug repurposing.
83
HY-L260 KRAS Targeted Compound Library
KRAS (Kirsten Rat Sarcoma Viral Oncogene Homolog) is one of the most important oncogenic driver genes in oncology, with high mutation frequencies in pancreatic cancer, non‑small cell lung cancer, and colorectal cancer. For a long time, KRAS was considered "undruggable" due to the lack of suitable small‑molecule binding pockets on its protein surface. In recent years, with the discovery of the switch‑II pocket and the successful approval of KRAS G12C inhibitors, KRAS‑targeted research has achieved groundbreaking progress, which has also spurred a wave of development targeting non‑G12C mutants such as G12D and G12V, as well as upstream and downstream regulatory factors including SOS1 and SHP2. MCE KRAS Targeted Compound Library contains 82 small‑molecule compounds targeting the KRAS, serving as high‑quality research tools for mechanistic studies of KRAS‑mutant tumors, combination therapy development, resistance mechanism exploration, and high‑throughput drug screening, thereby providing robust support for KRAS‑targeted drug discovery.

Signaling Pathway Targeting Libraries

83
HY-100388A SHP099 monohydrochloride
SHP099 hydrochloride is a potent, selective and orally available SHP2 inhibitor with an IC50 of 70 nM.
SHP2   Phosphatase  
Cancer  
76
HY-100388 SHP099
SHP099 is an allosteric SHP2 inhibitor, with IC50s of 0.690, 1.241, 0.416, 1.968, 2.896 μM for SHP2, SHP2D61Y, SHP2E69K, SHP2A72V, SHP2E76K. SHP099 inhibits cancer cell growth, such as MV4-11 and TF-1 cell (IC50: 0.32 and 1.73 μM). SHP099 inhibits RAS-ERK signaling and inhibits tumor growth.
SHP2   Phosphatase  
Cancer  
76
HY-18234A Leupeptin hemisulfate
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.

Source: Streptomyces roseus MB-26-AI

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)  
Inflammation or Immune System Disease   Respiratory Disease   Coronavirus Infection   Skin Disease  
68
HY-50876 Daporinad
Daporinad (FK866) is a non-competitive inhibitor of nicotinamide phosphoribosyltransferase (Nampt), with a Ki value of 0.3 nM. Daporinad depletes NAD+ and ATP levels, inhibits mTORC1 and MAPK/ERK pathways, and activates TFEB to induce autophagy. Daporinad causes the depletion of the endoplasmic reticulum Ca²⁺ pool, ultimately weakening the mitogen-induced Ca²⁺ signal and the activation and function of T cells. Daporinad induces cell cycle arrest and apoptosis, and inhibits cell proliferation. Daporinad can be used for the study of myeloma, liver cancer, and immunosuppression.
NAMPT   Autophagy   Apoptosis   mTOR   p38 MAPK   ERK  
Cancer  
67
HY-130149 Adagrasib
Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction.
Ras  
Lung Cancer   Colorectal Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer  
64
HY-13064 Cobimetinib
Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
MEK   Apoptosis  
Lung Cancer   Colorectal Cancer   Prostate Cancer   Liver Cancer   Pancreatic Cancer   Pain   Digestive System Inflammation   Obesity   Rheumatoid Arthritis  
63
HY-134813 MRTX1133
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations.
Ras  
62
HY-15723A NSC 23766 trihydrochloride
NSC 23766 trihydrochloride is an inhibitor of Rac1 activation.
Ras   Apoptosis  
Colorectal Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Digestive System Inflammation   Glucose Metabolism  
56
HY-15202 Binimetinib
Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
MEK   Autophagy  
Colorectal Cancer   Prostate Cancer   Pancreatic Cancer   Non-Small Cell Lung Cancer   Lung Adenocarcinoma   Triple-Negative Breast Cancer   Rheumatoid Arthritis  
53
HY-10320 Doramapimod
Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM.
p38 MAPK   Raf   Autophagy  
Lung Cancer   Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Pancreatic Cancer   Ovarian Cancer   Neurodegenerative Disease   Depression   Pain   SARS-CoV-2 Infection   Obesity   Lung Fibrosis   Rheumatoid Arthritis  
53
HY-15605 Encorafenib
Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
Raf  
Colorectal Cancer   Liver Cancer   Pancreatic Cancer   SARS-CoV-2 Infection   Obesity  
47
HY-108635 C16-PAF
C16-PAF (PAF (C16)), a phospholipid mediator, is a platelet-activating factor and ligand for PAF G-protein-coupled receptor (PAFR). C16-PAF exhibits anti-apoptotic effect and inhibits caspase-dependent death by activating the PAFR. C16-PAF is a potent MAPK and MEK/ERK activator. C16-PAF induces increased vascular permeability.
p38 MAPK   MEK   ERK   Endogenous Metabolite  
Inflammation or Immune System Disease   Lung Cancer   Neurodegenerative Disease   Depression   Pain   Cardiovascular Disease  
43
HY-N0431 Astragaloside IV
Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
MMP   ERK   JNK  
Lung Cancer   Breast Cancer   Colorectal Cancer   Prostate Cancer   Liver Cancer   Pancreatic Cancer   Depression   Pain   Parkinson's Disease   Obesity   Lung Fibrosis   Rheumatoid Arthritis  
43
HY-D0886 β-Glycerophosphate disodium salt pentahydrate
β-Glycerophosphate disodium salt pentahydrate is a bioactive endogenous metabolite and a phosphatase inhibitor. β-Glycerophosphate disodium salt pentahydrate plays an important role in inducing and maintaining osteoblast differentiation, mineral metabolism and signal transduction, and can be used as a drug carrier to form heat-sensitive hydrogels. β-Glycerophosphate disodium salt hydrate accelerates the calcification of vascular smooth muscle cells.
Phosphatase   Endogenous Metabolite   ERK  
Cancer   Metabolic or Endocrine Disease  
35
HY-W011269 Eicosapentaenoic Acid sodium
Eicosapentaenoic Acid (EPA)sodium is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid sodium exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid sodium activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid sodium can promote relaxation of vascular smooth muscle cells and vasodilation.
Endogenous Metabolite   Histone Demethylase  
Blood or Cardio-cerebrovascular Disease   Metabolic or Endocrine Disease  
33
HY-B0660 Eicosapentaenoic Acid
Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation.
Endogenous Metabolite   Histone Demethylase  
Neurological, Eye or Ear Disease   Prostate Cancer   Leukemia/Lymphoma/Myeloma  
33
HY-B0105 Ketoconazole
Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.
Fungal   Cytochrome P450   Ras   Bacterial  
Colorectal Cancer   Prostate Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Viral Infection   Bacterial Infection   Fungal Infection   Metastatic Breast Cancer  
32
HY-B0183 Ellagic acid
Ellagic acid is a natural antioxidant, and acts as a potent and ATP-competitive inhibitor of CK2 and SHP2, with an IC50 of 40 nM and a Ki of 20 nM.
Casein Kinase   Reactive Oxygen Species (ROS)   Endogenous Metabolite   SHP2  
Cancer   Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
22
HY-156498 RMC-7977
RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRASG12C cancer models, and demonstrates good tolerability across various RAS cancer models.
Ras   ERK   Raf   Ribosomal S6 Kinase (RSK)   AMPK   Apoptosis   PARP  
18
HY-148439 Daraxonrasib
Daraxonrasib (RMC-6236) is an orally active, non-covalent RAS (ON) inhibitor. Daraxonrasib disrupts the interaction of wild-type or mutant RAS proteins with the RAS binding domain of BRAF, with EC50 values ranging from 28-220 nM for wild-type KRAS, NRAS, HRAS, and multiple oncogenic RAS variants. Daraxonrasib inhibits pERK. Daraxonrasib has anti-tumor activity against KRAS mutant tumors.
Ras   PERK  
Respiratory Disease   Colorectal Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Non-Small Cell Lung Cancer  
18
HY-N0103 Sophocarpine
Sophocarpine is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage.
Autophagy   Apoptosis   NF-κB   PI3K   Akt   MEK   ERK   PTEN  
Lung Cancer   Breast Cancer   Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Depression   Pain   Digestive System Inflammation   Cardiovascular Disease   Parkinson's Disease   Obesity   Lung Fibrosis   Rheumatoid Arthritis  
12
HY-153724 BI-2865
BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively. BI-2865 inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells (mean IC50: roughly 140 nM).
Ras  
Cancer  
12
HY-116009 RMC-4550
RMC-4550 is a potent, selective and allosteric inhibitor of SHP2, with an IC50 of 0.583 nM.
SHP2   Phosphatase  
Cancer  
11
HY-N0678 Icaritin
Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium brevicornuMaxim. and potently inhibits proliferation of K562 cells (IC50 of 8 µM) and primary CML cells (IC50 of 13.4 µM for CML-CP and 18 µM for CML-BC). Icaritin can regulate MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis.
JAK   Autophagy   Apoptosis  
Lung Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Autoimmune Disease   Digestive System Inflammation   SARS-CoV-2 Infection  
11
HY-N0104 Curcumol
Curcumol ((-)-Curcumol), a bioactive sesquiterpenoid, possesses numerous pharmacological activities like anticancer, antimicrobial, antifungal, antiviral, and antiinflammatory. Curcumol is a potent inducer of apoptosis in numerous cancer cells via targeting key signaling pathways as MAPK/ERK, PI3K/Akt and NF-κB which are generally deregulated in several cancers.
Apoptosis  
Digestive System Disease   Breast Cancer   Digestive System Inflammation  
9
HY-10966 SB-590885
SB-590885 is a BRAF/c-Raf kinase inhibitor that selectively targets B-Raf, and it amplifies the ERK/MAPK signaling pathway in RAS-activated cells. SB-590885 effectively inhibits the malignant proliferation, transformation and tumorigenicity of oncogenic B-Raf cells; it also induces the proliferation of erythroid progenitor cells, delays their differentiation and promotes hemoglobin synthesis, thereby improving ineffective erythropoiesis and reducing apoptosis. SB-590885 exerts a synergistic effect with TGF-β inhibitors and glucocorticoids, significantly promoting the formation of erythroid colonies in cells from patients with Diamond-Blackfan anemia (DBA). SB-590885 is mainly used in relevant studies on DBA, cisplatin-induced myelosuppression-related anemia, and pan-cancers such as melanoma and colorectal cancer.
Raf   Apoptosis  
Neurological, Eye or Ear Disease   Colorectal Cancer   Liver Cancer   Pancreatic Cancer   Obesity  
9
HY-15246 Tovorafenib
Tovorafenib (TAK-580, MLN 2480) is an orally active and selective inhibitor of pan-Raf kinase. Tovorafenib can be used for the study of glioma.
Raf  
Colorectal Cancer   Liver Cancer   Pancreatic Cancer   Obesity  
8
HY-112368 PHPS1
PHPS1 is a potent and selective Shp2 inhibitor with Kis of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively.
SHP1   SHP2   Phosphatase  
Cancer   Cardiovascular Disease   Obesity  
7
HY-136173 Batoprotafib
Batoprotafib (TNO155) is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). Batoprotafib has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors.
SHP2   Phosphatase  
Lung Cancer   Prostate Cancer   Pancreatic Cancer  
7
HY-156819 Zoldonrasib
Zoldonrasib (RMC-9805) is a potent and orally active KRAS G12D inhibitor.Zoldonrasib induces apoptosis in KRAS G12D mutant cancer cells. Zoldonrasib has the potential for the research of KRAS G12D mutant cancer.
Ras   Apoptosis  
Colorectal Cancer   Pancreatic Cancer   Non-Small Cell Lung Cancer  
6
HY-P0119A Lixisenatide acetate
Lixisenatide acetate is a glucagon-like peptide-1 (GLP-1) receptor agonist. Lixisenatide acetate inhibits the inflammatory response through down regulation of pro-inflammatory cytokines, and suppresses of the Akt-MEK1/2 signaling pathway. Lixisenatide acetate can inhibit oxidative stress, mitochondrial dysfunction and apoptosis. Lixisenatide acetate can be used for the researches of inflammation, metabolic disease, neurological disease and cardiovascular disease, such as rheumatoid arthritis, diabetes, Alzheimer's disease and atherosclerosis.
GLP Receptor   Akt   MEK   Reactive Oxygen Species (ROS)   Apoptosis   MMP  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease   Metabolic or Endocrine Disease  
4
HY-N0498 Nitidine chloride
Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway, also has anti-inflammatory activity. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway.
Parasite   Apoptosis   STAT   Topoisomerase   ERK   FAK   p38 MAPK   NF-κB  
Lung Cancer   Breast Cancer   Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Parasitic Infection   Neurodegenerative Disease   Depression   Pain   Digestive System Inflammation   Obesity   Lung Fibrosis   Rheumatoid Arthritis  
4
HY-N2963 Broussonin E
Broussonin E is a phenolic compound and shows anti-inflammatory activity. Broussonin E can suppress inflammation by modulating macrophages activation statevia inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway. Broussonin E can be used for the research of inflammation-related diseases such as atherosclerosis.
ERK   p38 MAPK   JAK   STAT   TNF Receptor   Interleukin Related   COX   Arginase  
Lung Cancer   Colorectal Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Pancreatic Cancer   Ovarian Cancer   Neurodegenerative Disease   Depression   Pain   Digestive System Inflammation   Obesity   Lung Fibrosis   Rheumatoid Arthritis  
3
HY-18756 NSC-87877
NSC-87877 is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively. NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26).
SHP1   SHP2   Phosphatase   Apoptosis  
Digestive System Disease   Digestive System Inflammation  
3
HY-19700 trans-Zeatin
trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
Environmental Pollutants   ERK   MEK   Endogenous Metabolite  
Colorectal Cancer   Prostate Cancer   Liver Cancer   Pain   Obesity   Rheumatoid Arthritis  
3
HY-N0363 (+)-Columbianetin
(+)-Columbianetin ((S)-Columbianetin) acts as an inhibitor of JNK/ERK. (+)-Columbianetin inhibits UVA-induced phosphorylation of JNK and ERK, reduces the production of MMP-1, reverses UVA-induced Collagen (HY-NP003) degradation, and alleviates UVA-mediated inhibition of Smad2/3 phosphorylation and translocation. (+)-Columbianetin regulates the AP-1 and ASK1-MAPK signaling pathways, inhibits the production of ROS and blocks sub-G1 cell cycle arrest. (+)-Columbianetin is applicable to research related to skin aging.
ERK   JNK   Collagen   TGF-beta/Smad   p38 MAPK   Reactive Oxygen Species (ROS)  
2
HY-P4322 H-Ile-Lys-Val-Ala-Val-OH
H-Ile-Lys-Val-Ala-Val-OH is one of the most potent active sites of laminin-1. H-Ile-Lys-Val-Ala-Val-OH promotes cell adhesion, neurite outgrowth, and tumor growth. H-Ile-Lys-Val-Ala-Val-OH stimulates BMMSC population growth and proliferation by activating MAPK/ERK1/2 and PI3K/Akt signalling pathways.
ERK   Akt  
Pancreatic Cancer   Depression   Pain   Digestive System Inflammation  
2
HY-N0526 2"-O-Galloylhyperin
2''-O-Galloylhyperin is an active natural compound with anti‑inflammatory, antioxidant, anti‑adipogenic, antifibrotic, and cytostatic activities. 2''-O-Galloylhyperin upregulates SIRT1/Nrf2 signaling, inhibits NF-κB and MAPK (ERK1/2, p38, JNK) phosphorylation, suppresses TSHR activation, reduces ROS accumulation, and enhances SOD and GSH-Px activities. 2''-O-Galloylhyperin protects against LPS-induced tissue injury, enhances survival, and inhibits adipogenesis and fibrosis. 2"-O-Galloylhyperin can be used for the research of sepsis, acute lung injury, and thyroid eye disease.
Sirtuin   Keap1-Nrf2   NF-κB   ERK   p38 MAPK   JNK   TSH Receptor   Reactive Oxygen Species (ROS)   SOD  
Inflammation or Immune System Disease   Parkinson's Disease  
2
HY-N1419 Vaccarin
Vaccarin is an orally active flavonoid glycoside with multiple biological functions. Vaccarin promotes neovascularization by activating AKT and ERK. Vaccarin activates the AMPK signaling pathway to improve insulin resistance and steatosis. Vaccarin is a MAPK, NF-κB, and NFAT inhibitor, effectively blocking RANKL-induced osteoclastogenesis.
AMPK   Akt   ERK   p38 MAPK   NF-κB   Nuclear Factor of activated T Cells (NFAT)   JNK  
Lung Cancer   Breast Cancer   Prostate Cancer   Gastric Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Ovarian Cancer   Depression   Pain   Digestive System Inflammation   Cardiovascular Disease   Glucose Metabolism   Parkinson's Disease   Obesity   Lung Fibrosis   Rheumatoid Arthritis  
2
HY-P5522 TriDAP
TriDAP (L-Ala-γ-D-Glu-meso-diaminopimelic acid) is a NOD1 agonist with a Kd value of 34.5 μM. TriDAP enhances the binding of NOD1-RICK, promotes RICK phosphorylation, and activates the NF-κB, TAK1, MEK/ERK, p38 and interferon response pathways. TriDAP downregulates Runx2 via increasing ubiquitination and reduces trabecular bone parameters. TriDAP decreases IκBα levels and increases p65 levels. TriDAP induces the secretion of proinflammatory mediators IL-8 and prostaglandins, triggers tissue inflammation and innate immune activation, and inhibits SARS-CoV-2 replication in lung epithelial cells. TriDAP increases the RANKL/OPG ratio in mice, reduces bone mass and enhances osteoclast activity, and inhibits new bone formation by decreasing the mineralization deposition rate in mice. TriDAP can be used in research related to pulpitis, chronic ulcerative colitis, Crohn's disease and SARS-CoV-2 infection.
NOD-like Receptor (NLR)   NF-κB   MAP3K   MEK   ERK   p38 MAPK   Interleukin Related   SARS-CoV  
Digestive System Inflammation   SARS-CoV-2 Infection   Crohn's Disease   Ulcerative Colitis  
1
HY-N7694 Isotoosendanin
Isotoosendanin is an orally active TGFβR1 inhibitor and abrogating its kinase activity (IC50 = 6732 nM). Isotoosendanin inhibits the JAK/STAT3 signaling pathway by directly targeting SHP-2, enhancing its stability, and reducing its ubiquitination. Isotoosendanin inhibits TGF-β-induced reduces the migration, invasion, and metastasis in triple-negative breast cancer (TNBC) cells. Isotoosendanin exhibits anti-tumor efficacy in TNBC xenograft models and A549 xenograft tumors. Isotoosendanin exhibits significant anti-inflammatory effects in acetic acid-induced vascular permeability and λ-carrageenan-induced hind paw edema tests. Isotoosendanin can be used for the study of non-small cell lung cancer (NSCLC), TNBC and inflammation.
TGF-β Receptor   JAK   STAT   Apoptosis  
Lung Cancer   Breast Cancer   Colorectal Cancer   Prostate Cancer   Liver Cancer   Leukemia/Lymphoma/Myeloma   Pancreatic Cancer   Digestive System Inflammation   Obesity   Lung Fibrosis   Rheumatoid Arthritis  
1
HY-N4322 Decursinol angelate
Decursinol angelate acts as a PKC activator and GDH inhibitor, with an IC50 of 1.432 μM against human GDH. Decursinol angelate activates PKC, downregulates PKCα and PKCβII isoforms, and exerts cytotoxic activity against cancer cells. Decursinol angelate binds to GDH and inhibits its enzymatic activity. Decursinol angelate inhibits VEGF-induced autophosphorylation of VEGFR2, downstream p42/44 ERK and JNK-MAPK signaling pathways, as well as the angiogenesis process. Decursinol angelate is applicable to research related to cancer and leukemia.
PKC  
Cancer   Digestive System Disease   Digestive System Inflammation  
1
HY-10254G Mirdametinib (GMP)
Mirdametinib (PD0325901) (GMP) is Mirdametinib (HY-10254) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Mirdametinib is an orally active, selective and non-ATP-competitive MEK inhibitor.
MEK  
1
HY-P5522A TriDAP dihydrochloride
TriDAP dihydrochloride (L-Ala-γ-D-Glu-meso-diaminopimelic acid dihydrochloride) is a NOD1 agonist with a Kd value of 34.5 μM. TriDAP dihydrochloride enhances the binding of NOD1-RICK, promotes RICK phosphorylation, and activates the NF-κB, TAK1, MEK/ERK, p38 and interferon response pathways. TriDAP dihydrochloride downregulates Runx2 via increasing ubiquitination and reduces trabecular bone parameters. TriDAP dihydrochloride decreases IκBα levels and increases p65 levels. TriDAP dihydrochloride induces the secretion of proinflammatory mediators IL-8 and prostaglandins, triggers tissue inflammation and innate immune activation, and inhibits SARS-CoV-2 replication in lung epithelial cells. TriDAP dihydrochloride increases the RANKL/OPG ratio in mice, reduces bone mass and enhances osteoclast activity, and inhibits new bone formation by decreasing the mineralization deposition rate in mice. TriDAP dihydrochloride can be used in research related to pulpitis, chronic ulcerative colitis, Crohn's disease and SARS-CoV-2 infection.
NOD-like Receptor (NLR)   NF-κB   MAP3K   MEK   ERK   p38 MAPK   Interleukin Related   SARS-CoV  
Digestive System Inflammation   SARS-CoV-2 Infection   Crohn's Disease   Ulcerative Colitis  
1
HY-161952 Sitneprotafib
Sitneprotafib (JAB-3312) is an orally effective anticancer phosphatase SHP2 inhibitor (IC50: 1.9 nM) with anti-cancer activity. Sitneprotafib has good tolerability and significantly induced tumor regression in a KYSE-520 mouse xenograft model.
SHP2  
Cancer  
1
HY-P700618 SHP-2 Protein, Human (T253M, Q257L, His)
The SHP-2 protein is a key player downstream of the receptor and cytoplasmic protein tyrosine kinases, facilitating signal transduction from the cell surface to the nucleus. It actively regulates the MAPK pathway and dephosphorylates key substrates, including GAB1, ARHGAP35, EGFR, ROCK2 ("Tyr-722"), and CDC73. SHP-2 Protein, Human (T253M, Q257L, His) is the recombinant human-derived SHP-2 protein, expressed by E. coli , with N-6*His labeled tag and T253M, Q257L mutation.

Species: Human; Source: E. coli

1
HY-P80298 Ras Antibody (YA106)
Ras Antibody (YA106) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Ras.

Host: Rabbit; Reactivity: Human, Mouse, Rat, Zebrafish

Monoclonal Antibodies Recombinant Antibodies Flow Cytometry Antibodies Primary Antibodies

1
HY-N12740 Napyradiomycin B4
Napyradiomycin B4 is a Napyradiomycin derivative, which inhibits the RANKL-induced MEK-ERK signaling pathway. Napyradiomycin B4 attenuates osteoclastogenesis and prevents alveolar bone destruction in experimental periodontitis.

Source: marine-derived Streptomyces species

MEK   ERK  
/
HY-B1272AS1 Desipramine-d3
Desipramine-d3 is the deuterium labeled Desipramine (HY-B1272A). Desipramine is a first-generation tricyclic antidepressant. Desipramine selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine can be used for the research of hepatocellular cancer, inflammation, and neurological diseases.
Isotope-Labeled Compounds   Adrenergic Receptor   ERK   JNK   p38 MAPK   NF-κB   AP-1   Apoptosis   Reactive Oxygen Species (ROS)   Mitochondrial Metabolism   TNF Receptor  
Cancer   Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
/
HY-B1014S1 Acenocoumarol-d4
Acenocoumarol-d4 is deuterium labeled Acenocoumarol (HY-B1014). Acenocoumarol is an anticoagulant that functions as a Vitamin K antagonist. Acenocoumarol inhibits MAPK/ERK/JNK signaling pathway, reduces the nuclear translocation of NF-κB p65, activates Akt/GSK3β signaling pathway. Acenocoumarol induces apoptosis in cell A549, arrests cell cycle at S phase.
Isotope-Labeled Compounds   ERK   Akt   JNK   Apoptosis   PKA   p38 MAPK   VD/VDR   GSK-3   NF-κB  
Cancer   Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease  
/
HY-P11242 Cm-CATH2
Cm-CATH2 is an antimicrobial peptide discovered from Chelonia mydas. Cm-CATH2 has a potent, broad-spectrum and rapid bactericidal ability by rapidly destroying the integrity of bacterial cell membranes. It shows strong activity against Gram-positive bacteria (such as VREF, Staphylococcus aureus), Gram-negative bacteria (such as Escherichia coli, Klebsiella pneumoniae), and fungi (such as Candida albicans) with MICs ranges from 1.17 to 18.75 μg/mL. Cm-CATH2 is also effective against various aquatic pathogenic bacteria. Cm-CATH2 not only inhibits biofilm formation but can also remove the formed biofilms. Cm-CATH2 has immunomodulatory functions and chemotactic effects on immune cells, and can inhibit the production of pro-inflammatory cytokines by macrophages stimulated by LPS (HY-D1056). Cm-CATH2 prevents the activation of NF-κB by inhibiting the degradation of IκBα, and also inhibits the phosphorylation of MAPK signaling pathways (p38, JNK, ERK). Cm-CATH2 demonstrates strong anti-infective ability in mouse peritonitis models and pneumonia models.
Bacterial   NF-κB   p38 MAPK   JNK   ERK   TNF Receptor   Interleukin Related  
Infection  
/
HY-P2157 Ras Inhibitory Peptide
Ras Inhibitory Peptide (VPPPVPPRRR) is a Ras inhibitor with antitumor activity.
Ras  
Cancer  
/
HY-122465 Aspafilioside B
Aspafilioside B is a steroidal saponin. Aspafilioside B is extractable from Asparagus filicinus. Aspafilioside B activates the ERK, c-Raf and p38 MAPK signaling pathways, and upregulates H-Ras and N-Ras. Aspafilioside B mediates G2/M cell cycle arrest by altering the expression of cell cycle regulatory proteins. Aspafilioside B induces Apoptosis. Aspafilioside B increases intracellular ROS levels. Aspafilioside B is applicable to research related to hepatocellular carcinoma.
ERK   Raf   p38 MAPK   Ras   Apoptosis   Reactive Oxygen Species (ROS)  
Liver Cancer  
/
HY-128393S2 Trilinolein-d5
Trilinolein-d5 is the deuterium labeled Trilinolein (HY-128393). Trilinolein is an orally active triglyceride that inhibits the PI3K/Akt, Ras/MEK/ERK signaling pathways, and MMP-2. Trilinolein can reduce oxidative stress, induce apoptosis, and inhibit cell migration. Trilinolein can be used in the research fields of cardiovascular disease, cerebrovascular disease (such as cerebral ischemia), and non-small cell lung cancer.
Isotope-Labeled Compounds   ERK   MEK   Apoptosis   Akt   PI3K   MMP   E-Selectin  
/
HY-113313S2 Aldosterone-d4
Aldosterone-d4 is the deuterium labeled Aldosterone. Aldosterone is the primary mineralocorticoid. Aldosterone is a steroid hormone, and it is synthesized and secreted in response to renin-angiotensin system activation (RAS) or high dietary potassium by t
Isotope-Labeled Compounds   Endogenous Metabolite  
Blood or Cardio-cerebrovascular Disease  
/
HY-W065835 2-Bromoaldisine
2-Bromoaldisine is a pyrrole alkaloid that can be isolated from the Red Sea: marine sponge Stylissa carter. 2-Bromoaldisine inhibits HIV-1 vector infection. 2-Bromoaldisine inhibits Raf/MEK/MAPK pathway.

Source: marine sponge Stylissa carteri

HIV  
Viral Infection  
/
HY-B0185AS1 Lidocaine-d6 hydrochloride
Lidocaine-d6 (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor.
Sodium Channel   MEK   ERK   NF-κB   Apoptosis  
Blood or Cardio-cerebrovascular Disease  
/
HY-15947G Ravoxertinib (GMP)
Ravoxertinib GMP is Ravoxertinib (HY-15947) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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.
ERK   c-Myc   Hexokinase   Lactate Dehydrogenase  
Breast Cancer   Ovarian Cancer   Squamous Cell Carcinoma  
/
HY-P990146 Anti-Mouse/Rat/Human v-H-Ras Antibody (Y13-238)
Anti-Mouse/Rat/Human v-H-Ras Antibody (Y13-238) is an anti-mouse/rat/human v-H-Ras IgG2a monoclonal antibody. Anti-Mouse/Rat/Human v-H-Ras Antibody (Y13-238) can be used as a control antibody. Anti-Mouse/Rat/Human v-H-Ras Antibody (Y13-238) is often used for immunofluorescence and immunoprecipitation.

Species: Human/Mouse/Rat

Ras  
Inflammation or Immune System Disease  
/
HY-P10074 TAT-MEK1
TAT-MEK1 is an inhibitor ofERK2, consisting of TAT and MEK1 (N-terminal), TAT (YGRKKRRQRRR) derived from human immunodeficiency (HIV-1) transcriptional trans activator (TAT), is a cell-penetrating peptide. TAT-MEK1 IC50 in vitro for ERK2 is 29 μM.
ERK  
Inflammation or Immune System Disease  
/
HY-P2360A G12 TFA
G12 (Ras 5-17) TFA is a wild-type Ras peptide consisted of amino acids 5-17 (KLVVVGAGGVGKS). G12 TFA can be used as a control of mutant Ras peptides studies (such V12).
Ras  
/
HY-B0660S2 Eicosapentaenoic acid-d10
Eicosapentaenoic acid-d10 (EPA-d10) is the deuterium labeled Eicosapentaenoic acid (HY-B0660). Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation.
Isotope-Labeled Compounds   Histone Demethylase   Endogenous Metabolite  
Cancer   Neurological, Eye or Ear Disease  
/
HY-P4133 MEK1 Derived Peptide Inhibitor 1
MEK1 Derived Peptide Inhibitor 1 is a ERK2 inhibitor that inhibits the activation of ERK2 by MEK1 in vitro, with an IC50 of 30 μM, and exhibits selectivity for ERK over JNK and p38 kinases. MEK1 Derived Peptide Inhibitor 1 can be used to study ERK activation and ERK-mediated responses.
ERK   MEK  
/
HY-N9980 Antcin K
Antcin K is a selective inhibitor targeting the PI3K/Akt, NF-κB, MEK1/2-ERK, p38 and AP-1 pathways. Antcin K upregulates IL-10 expression, thereby inhibiting the production of pro-inflammatory factors, blocking monocyte adhesion, reducing tissue damage, and promoting myogenesis. Antcin K has significant anti-inflammatory, anti-damage and tissue protective activities. Antcin K is mainly used in the research of inflammation-related diseases such as periodontitis, rheumatoid arthritis, and skeletal muscle injury.

Source: Antrodia cinnamomea

PI3K   p38 MAPK   NF-κB   Akt   AP-1  
Rheumatoid Arthritis  
/
HY-P11250 HVF18-a3-d
HVF18-a3-d is an antimicrobial peptide. HVF18-a3-d reduces NO production. HVF18-a3-d inhibits the production of TNF-α and IL-6, reduces ROS production, and suppresses the TLR4 signaling pathway, as well as LPS-induced phosphorylation of ERK, JNK, and p38 MAPK. HVF18-a3-d exhibits antimicrobial activity against a variety of bacteria by disrupting their outer and inner membranes. HVF18-a3-d protects mice from fatal septic shock induced by Acinetobacter baumannii resistant to Carbapenem. HVF18-a3-d shows anti-inflammatory and antioxidant effects.
Bacterial   NO Synthase   Interleukin Related   Reactive Oxygen Species (ROS)   Toll-like Receptor (TLR)   ERK   JNK   p38 MAPK  
Infection   Inflammation or Immune System Disease  
/
HY-P5977 STE-MEK1(13)
STE-MEK1(13) (Ste-MPKKKPTPIQLNP-NH ) is a cell permeable ERK1/2 inhibitor (IC50: 13-30 μM). STE-MEK1(13) inhibits ERK1/2 phosphorylation.
ERK  
Cancer  
/
HY-10999S1 Trametinib-13C6
Trametinib-13C6 is the 13C-labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.
MEK   Autophagy   Apoptosis  
Cancer  
/
HY-121532 (-)-Rasfonin
(-)-Rasfonin is a fungal secondary metabolite and inhibits small G proteins Ras. (-)-Rasfonin induces apoptosis, necrosis and autophagy in ACHN cells (a renal carcinoma cell line).

Source: Talaromyces sp. 3656-A1

Ras   Apoptosis   Autophagy  
/
HY-G0007S Omeprazole sulfone-d3
Omeprazole sulfone-d3 is the deuterium labeled Omeprazole sulfone. Omeprazole sulfone (Omeprazole sulphone) is one of the major circulating metabolites of Omeprazole (HY-B0113) in vivo, and belongs to class 4 non-mutagenic impurities. Omeprazole sulfone does not bind to the aryl hydrocarbon receptor (AhR), nor does it induce the expression of CYP1A1 or CYP1A2. However, Omeprazole sulfone promotes the migration of gastric epithelial cells under basal conditions and reverses the inhibitory effect of Indomethacin (HY-14397) on cell migration. Omeprazole sulfone does not promote cell proliferation, nor does it upregulate COX-2 expression or activate signaling pathways such as ERK, P38 MAPK and PI3K. Omeprazole sulfone maintains basal ulcer healing under non-acid-dependent conditions and can be used in studies related to gastric ulcer repair.
Isotope-Labeled Compounds   Drug Metabolite   Cytochrome P450   Aryl Hydrocarbon Receptor  
Cancer   Infection  
/
HY-10966G SB-590885 (GMP)
SB-590885 GMP is SB-590885 (HY-10966) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SB-590885 is a BRAF/c-Raf kinase inhibitor that selectively targets B-Raf, and it amplifies the ERK/MAPK signaling pathway in RAS-activated cells. SB-590885 effectively inhibits the malignant proliferation, transformation and tumorigenicity of oncogenic B-Raf cells; it also induces the proliferation of erythroid progenitor cells, delays their differentiation and promotes hemoglobin synthesis, thereby improving ineffective erythropoiesis and reducing apoptosis. SB-590885 exerts a synergistic effect with TGF-β inhibitors and glucocorticoids, significantly promoting the formation of erythroid colonies in cells from patients with Diamond-Blackfan anemia (DBA). SB-590885 is mainly used in relevant studies on DBA, cisplatin-induced myelosuppression-related anemia, and pan-cancers such as melanoma and colorectal cancer.
Raf   Apoptosis  
Colorectal Cancer   Blood Disease  
/
HY-P11467 Gy-CATH
Gy-CATH is an anionic antimicrobial peptide. Gy-CATH activates MAPK and NF-κB signaling pathways (elevated levels of phospho-ERK, -p38, -JNK, -p65, and -IκBα). Gy-CATH upregulates the expression levels of three physiological anticoagulant pathways. Gy-CATH inhibits ADP-, Collagen-, and PMA-induced platelet aggregation. Gy-CATH has no direct antimicrobial activity, but shows significant preventive abilities against mice infected with Staphylococcus aureus, Escherichia coli, and Methicillin (HY-121544)-resistant Staphylococcus aureus. Gy-CATH exhibits potent immunomodulatory activity, enhancing macrophage-and neutrophil-mediated bactericidal functions. Gy-CATH significantly reduces the extent of pulmonary fibrin deposition and prevents thrombosis in mice.
Bacterial   p38 MAPK   NF-κB   PERK   JNK  
Staphylococcus Aureus Infection   Escherichia Coli Infection   Platelet Disease  
/
HY-13078S Cobimetinib-13C6 racemate
Cobimetinib-13C6 (GDC-0973-13C6; XL518-13C6) racemate is the deuterium labeled Cobimetinib (racemate) (HY-13078). Cobimetinib racemate (GDC-0973 racemate; XL518 racemate) is the racemate of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.
Isotope-Labeled Compounds   MEK  
/
HY-W010201S1 Citronellol-d3
Citronellol-d3 ( (±)-Citronelloll-d3) is the deuterium labeled Citronellol (HY-W010201). Citronellol ((±)-Citronellol) is an orally active inducer of apoptosis. Citronellol can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis.
p62   Isotope-Labeled Compounds   Apoptosis   TNF Receptor   Necroptosis   PI3K   Autophagy   Atg8/LC3   Fungal   ERK   Reactive Oxygen Species (ROS)  
Cancer   Neurological, Eye or Ear Disease   Blood or Cardio-cerebrovascular Disease  
/
HY-P991744 Anti-Mouse CXCR4 Antibody (Cx4Mab-1)
Anti-Mouse CXCR4 Antibody is a monoclonal antibody that specifically recognizes murine CXCR4 (C-X-C chemokine receptor 4), also known as fusin or CD184. CXCR4 is a seven-transmembrane G protein–coupled receptor whose principal endogenous ligand is CXCL12 (stromal cell–derived factor-1α, SDF-1α) and is widely expressed in hematopoietic cells, endothelial cells, neurons, as well as embryonic and adult stem cells. The CXCR4–CXCL12 signaling axis activates multiple downstream pathways, including ERK1/2, Ras, p38 MAPK, PLC/MAPK, and SAPK/JNK, thereby regulating cell survival, proliferation, migration, and stemness maintenance. Aberrant overexpression of CXCR4 is closely associated with poor prognosis and metastasis in various cancers, with CXCR4-positive tumor cells preferentially home to CXCL12-rich tissues such as the liver, bone marrow, lung, and lymph nodes. Accordingly, CXCR4 and its CXCL12-related antagonists emerge as attractive targets for experimental anticancer therapy. Anti-Mouse CXCR4 Antibody is generated using a cell-based immunization and screening strategy and exhibits high affinity for both endogenous and exogenous murine CXCR4. Anti-Mouse CXCR4 Antibody can be used for thestudy of chronic lymphocytic leukemia and multiple myeloma.
CXCR  
Chronic Lymphocytic Leukemia   Multiple Myeloma  
/
HY-N12177 Cryptosporioptide A
Cryptosporioptide A (Compound 3) is a pigment protein tyrosine phosphatase inhibitor derived from the insect-parasitic fungus Cordyceps gracilioides. Cryptosporioptide A inhibits PTP1B, SHP2, CDC25B, LAR and SHP1 enzymes with IC50 of 7.3, 5.7, 7.6, >50, 4.9 μg/mL, respectively.

Source: Cordyceps gracilioides

Phosphatase   SHP1  
Metabolic or Endocrine Disease  
/
HY-N10079 Suchilactone
Suchilactone (Jatrophan) is a lignan extracted from Monsonia angustifolia E.Mey. Suchilactone binds to SHP2 and inhibits SHP2 activation, thereby inhibiting ERK-mediated cell proliferation. Suchilactone can be ued in acute myeloid leukaemia (AML).
SHP2  
Cancer  
/
HY-119481 Swerchirin
Swerchirin is an orally active, plant-derived xanthone that acts as an inhibitor of the Raf/MEK/ERK signaling pathway. Swerchirin downregulates the expression of phosphorylated MEK and phosphorylated ERK, induces mitochondrial apoptosis and cell cycle arrest, regulates Bcl-2 family proteins, triggers cytochrome c release, activates caspases, and drives PARP cleavage. Swerchirin reduces blood glucose levels in rat models under fasting, fed, glucose-loaded conditions, and following treatment with Tolbutamide (HY-B0401). Swerchirin can be used in research related to ovarian cancer, liver injury, and diabetes.
PERK   MEK   Raf   Caspase   PARP   Bcl-2 Family  
Ovarian Cancer   Type 1 Diabetes   Type 2 Diabetes   Liver Injury  
/
HY-P4136 Myristoyl-MEK1 Derived Peptide Inhibitor 1
Myristoyl-MEK1 Derived Peptide Inhibitor 1 is the myristoylated form of the MEK1 Derived Peptide Inhibitor 1 (HY-P4133). Myristoyl-MEK1 Derived Peptide Inhibitor 1 inhibits ERK activation with an IC50 of 10 μM.
ERK  
Cancer  
/
HY-P3444A CD31 TFA
CD31 (PECAM-1) TFA is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 TFA is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 TFA peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cell activation-.
SHP2   Bacterial  
Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
/
HY-134505 Avicin G
Avicin G is a sphingomyelinase inhibitor and plasma membrane disruptor. Avicin G inhibits the enzymatic activities of neutral sphingomyelinases (SMPD2/3) and acid sphingomyelinase (SMPD1), elevates intracellular sphingomyelin levels, and alters the distribution of sphingomyelin. Avicin G interferes with the lateral segregation of GTP- and GDP-bound H-Ras, inhibits the signal output of oncogenic K-Ras and H-Ras, reduces the phosphorylation of ERK and Akt, increases lysosomal pH, and inhibits the endocytic recycling of epidermal growth factor receptor. Avicin G can be used in research related to pancreatic ductal adenocarcinoma and non-small cell lung cancer.
Ras   Phospholipase   ERK   Akt  
Non-Small Cell Lung Cancer   Pancreatic Ductal Adenocarcinoma  
/
HY-10999S2 Trametinib-13C,d3
Trametinib-13C,d3 is the 13C- and deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.
Isotope-Labeled Compounds   MEK   Autophagy   Apoptosis  
Cancer  
/
HY-P11617 CLP-d2
CLP-d2 is a multi-target anti-inflammatory agent, osteoclastogenesis inhibitor and immunomodulator with superior pharmacokinetic properties to Daptomycin (HY-B0108) and good safety profiles. CLP-d2 inhibits the NF-κB and MAPK signaling pathways by reducing the expression levels of c-Fos and NFATc1, and decreasing the phosphorylation levels of IκBα, p65, ERK and JNK, thereby reducing the secretion of pro-inflammatory cytokines such as IL-6, TNF-α and IL-1β to exert anti-inflammatory activity. CLP-d2 inhibits intra-articular osteoclastogenesis in mice, alleviates bone erosion and joint swelling, reduces synovial hyperplasia and inflammatory cell infiltration, and decreases serum rheumatoid factor (RF) levels. CLP-d2 is applicable to related research on rheumatoid arthritis.
NF-κB   ERK   JNK   p38 MAPK   Interleukin Related  
Rheumatoid Arthritis  
/
HY-137971 (±)-Spiro-oxanthromicin A
(±)-Spiro-oxanthromicin A (Compound 4), a polyketide, is a K-Ras inhibitor with an IC50 of 26.7  μM. (±)-Spiro-oxanthromicin A can be isolated from soil-derived Streptomyces sp. (±)-Spiro-oxanthromicin A can mislocalize oncogenic mutant K-Ras from the plasma membrane of intact MDCK cells. (±)-Spiro-oxanthromicin A can be used for cancers research.

Source: Streptomyces sp.

Ras  
Cancer  
/
HY-P10847 KS-58
KS-58 is a KRpep-2d (HY-P3277) derivative. KS-58 is a K-Ras (G12D) inhibitory peptide that selectively binds K-Ras. KS-58 can enter cells and block intracellular Ras interaction with effector proteins. KS-58 inhibits the proliferation of tumor cells and has antitumor activity.
Ras  
/
HY-15244G Alpelisib (GMP)
Alpelisib GMP is Alpelisib (HY-15244) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Alpelisib (BYL-719) is an orally active PI3Kα-selective inhibitor that blocks the conversion of PIP2 to PIP3, thereby inhibiting pathways including PI3K/AKT/mTOR, MAPK/ERK, Notch and JAK-STAT. Alpelisib also induces apoptosis, G0/G1 phase arrest and senescence; it significantly inhibits the proliferation, self-renewal, stemness and epithelial-mesenchymal transition (EMT) of tumor cells, reduces cancer stem cell populations and decreases the expression of stem cell markers. Alpelisib not only enhances the sensitivity to Eribulin (HY-13442) and exerts a synergistic effect with Paclitaxel (HY-B0015), but may also induce drug resistance by upregulating the SGK3/GSK3β/β-catenin signaling pathway. Alpelisib can be applied to research related to breast cancer, gastric cancer and lipomas associated with PTEN hamartoma tumor syndrome.
PI3K   Apoptosis  
/
HY-169232 PCC16 chloride
PCC16 chloride is a dual PROTAC degrader targeting DHHC3 and PD-L1, with a DC50 of 0.103 μM for PD-L1 degradation. PCC16 chloride induces DHHC3 degradation via the ubiquitin-proteasome pathway by recruiting the CRBN E3 ubiquitin ligase (E3 ubiquitin ligase). By targeting DHHC3-which is essential for PD-L1 palmitoylation and membrane stability-PCC16 chloride reduces PD-L1 levels, decreases PD-L1 membrane retention time, and impairs its immunosuppressive function. PCC16 chloride enhances anti-tumor immunity by disrupting PD-L1-mediated immunosuppression. PCC16 chloride can be used in the research of immune checkpoint blockade-resistant cancers.
PROTACs   PD-1/PD-L1  
Cancer  
/
HY-P0119S Lixisenatide (Leu-13C6,15N) TFA
Lixisenatide (Leu-13C6,15N) TFA is the 13C- and 15N-labeled Lixisenatide (HY-P0119). Lixisenatide is a glucagon-like peptide-1 (GLP-1) receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of pro-inflammatory cytokines, and suppresses of the Akt-MEK1/2 signaling pathway. Lixisenatide can inhibit oxidative stress, mitochondrial dysfunction and apoptosis. Lixisenatide can be used for the researches of inflammation, metabolic disease, neurological disease and cardiovascular disease, such as rheumatoid arthritis, diabetes, Alzheimer's disease and atherosclerosis.
Isotope-Labeled Compounds   GLP Receptor   Akt   MEK   Apoptosis   Reactive Oxygen Species (ROS)   MMP  
Neurological, Eye or Ear Disease   Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease   Metabolic or Endocrine Disease  
/
HY-15202S3 Binimetinib-d4
Binimetinib-d4 (MEK162-d4) is deuterium labeled Binimetinib. Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
Isotope-Labeled Compounds   MEK   Autophagy  
Cancer  
/
HY-120885 (+)-Oxanthromicin
(+)-Oxanthromicin (Compound 1) mislocalizes the oncogenic mutant K-Ras from the plasma membrane of intact Madin-Darby canine kidney (MDCK) cells, and exhibits thereby antitumor efficacy.

Source: Streptomyces sp.

Ras  
Cancer  
/
HY-32718S Pelitinib-d6
Pelitinib-d6 (EKB-569-d6) is the deuterium labeled Pelitinib. Pelitinib (EKB-569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively.
Isotope-Labeled Compounds   EGFR   Src  
Cancer  
/
HY-N15438 Herbacitrin
Herbacitrin is a HIV-1 reverse transcriptase and integrase inhibitor with IC50 values of 21.5 μM and 2.15 μM, respectively. Herbacitrin inhibits the growth of normal mouse embryonic cells, hybridoma HF cells, and ras/myc-transformed SFME cells, regulates the growth of ras-transformed SFME cells, and exhibits cytotoxic activity against hybridoma HF cells. Herbacitrin can be used in studies related to HIV-1 infection.
HIV   HIV Integrase  
HIV Infection  
/
HY-112541 21-Hydroxyoligomycin A
21-Hydroxyoligomycin A is a potent inhibitor of K-Ras PM localization with an IC50 value of 4.82 nM. 21-Hydroxyoligomycin A has cytotoxicity and can be isolated from Streptomyces.

Source: Streptomyces cyaneogriseus

Ras   Antibiotic  
Cancer  
/
HY-N12915 SHP2-IN-29
SHP2-IN-29 (Compound 3) is a potent SHP2 inhibitor with an IC50 value of 0.18 μM. SHP2-IN-29 also has inhibitory activity against PTP1B and TCPTP, with IC50 values of 4.27 and 4.74 μM, respectively.

Source: fungal strain F10Z1082

SHP2   Phosphatase  
Cancer   Metabolic or Endocrine Disease  
/
HY-W010201S Citronellol-d6
Citronellol-d6 is deuterated labeled Citronellol (HY-W010201). Citronellol ((±)-Citronellol) is an orally active inducer of apoptosis. Citronellol can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis.
Reactive Oxygen Species (ROS)   Isotope-Labeled Compounds  
Lung Cancer  
/
HY-B1014S Acenocoumarol-d5
Acenocoumarol-d5 is the deuterium labeled Acenocoumarol (HY-B1014). Acenocoumarol is an anticoagulant that functions as a Vitamin K antagonist. Acenocoumarol inhibits MAPK/ERK/JNK signaling pathway, reduces the nuclear translocation of NF-κB p65, activates Akt/GSK3β signaling pathway. Acenocoumarol induces apoptosis in cell A549, arrests cell cycle at S phase.
Isotope-Labeled Compounds   ERK   Akt   JNK   Apoptosis   PKA   p38 MAPK   VD/VDR   GSK-3   NF-κB  
Cancer   Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease  
/
HY-126871 Zaragozic acid D2
Zaragozic acid D2 is the inhibitor for squalene synthase and Ras farnesyl-protein transferase (Ras FPTase), with IC50 of 2 nM and 100 nM, respectively. Zaragozic acid D2 is potentially ameliorating hypercholesterolemia and Ras-induced cancer.

Source: Amauroascus niger

Farnesyl Transferase  
Cancer   Metabolic or Endocrine Disease  
/
HY-152003S Ganglioside GM2-d3 ammonium
Ganglioside GM2-d3 (ammonium) is the deuterium labeled Ganglioside GM2 (HY-148385). Ganglioside GM2 is a human tumor antigen predominantly found in human tumor cells and fetal brain tissue. As a sialylated glycosphingolipid, Ganglioside GM2 is involved in processes such as cell signaling, adhesion, and motility. Ganglioside GM2 abnormal expression and accumulation are associated with tumors and neurodegenerative disorders. Ganglioside GM2 promotes tumor cell migration and invasion by directly binding to the integrin β1 receptor, activating the FAK/Src/Erk-MAPK signaling pathway, and inducing actin cytoskeleton remodeling.
Isotope-Labeled Compounds  
/
HY-B0627S1 Metformin-13C2 hydrochloride
Metformin-13C2 (1,1-Dimethylbiguanide-13C2) hydrochloride is the 13C-labeled Metformin hydrochloride (HY-17471A). Metformin (1,1-Dimethylbiguanide) hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride exerts central glucose-lowering effects by inhibiting Ras-related protein 1 (Rap1) in SF1 hypothalamic neurons. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, Metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo.
Isotope-Labeled Compounds   Mitophagy   Autophagy   mTOR   AMPK   Apoptosis  
Cancer   Blood or Cardio-cerebrovascular Disease   Metabolic or Endocrine Disease  
/
HY-159846S Luvometinib-d
Luvometinib-d (FCN-159-d) is the deuterated-labeled Luvometinib (HY-159846). Luvometinib is an orally potent MEK1/2 inhibitor. Luvometinib selectively blocks the MAPK signaling pathway by forming a ternary complex with MEKase and ATP, thereby reducing the phosphorylation level of ERK. Luvometinib induces cell cycle arrest and apoptosis, and inhibits cancer cell proliferation. Luvometinib can be used in relevant research on various solid tumors including melanoma, non-small cell lung cancer, colon cancer, and acute myeloid leukemia.
Isotope-Labeled Compounds   MEK   p38 MAPK   Apoptosis  
Cancer  
/
HY-B0627S Metformin-d6
Metformin-d6 (1,1-Dimethylbiguanide-d6) is a deuterated labeled Metformin (HY-B0627). Metformin (1,1-Dimethylbiguanide) inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin exerts central glucose-lowering effects by inhibiting Ras-related protein 1 (Rap1) in SF1 hypothalamic neurons. Metformin also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, Metformin regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo.
Isotope-Labeled Compounds   Mitophagy   Autophagy   mTOR   AMPK   Apoptosis  
Cancer   Blood or Cardio-cerebrovascular Disease  
/
HY-14188S Amiodarone-d4 hydrochloride
Amiodarone-d4 (hydrochloride) is the deuterium labeled Amiodarone hydrochloride. Amiodarone hydrochloride, a benzofuran-based Class III antiarrhythmic agent, inhibits WT outwardIhERG tails with an IC50 of ～45 nM. Amiodarone hydrochloride induces cell proliferation and myofibroblast differentiation via ERK1/2 and p38 MAPK signaling in fibroblasts. Amiodarone hydrochloride can be used in the research of both supraventricular and ventricular arrhythmias.
Potassium Channel   Autophagy  
Cancer   Blood or Cardio-cerebrovascular Disease  
/
HY-P10051A Cyclorasin 9A5 TFA
Cyclorasin 9A5 TFA is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC50 of 120 nM.
Ras   Raf  
Cancer  
/
HY-153939S Idasanutlin-d3-1
Idasanutlin-d3-1 (RG7388-d3-1) is the deuterated-labeled Idasanutlin (HY-15676). 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.
Isotope-Labeled Compounds   MDM-2/p53   E1/E2/E3 Enzyme   Apoptosis   Pyroptosis   Reactive Oxygen Species (ROS)   Caspase  
Musculoskeletal and Skin Disease   Colorectal Cancer   Melanoma   Neuroblastoma   Osteosarcoma   Non-Small Cell Lung Cancer   Acute Myeloid Leukemia   Non-Hodgkin Lymphoma  
/
HY-P991507 SCT200
SCT200 is a fully humanized IgG1 anti-EGFR monoclonal antibody with a Kd of 0.08 nM. SCT200 can kill tumor cells by complement-dependent cytotoxicity (CDC) and antibody-dependent cellular cytotoxicity (ADCC) through the Fc. SCT200 can be used for the study of refractory RAS and BRAF wild-type metastatic colorectal cancer.

Species: Human

EGFR  
Cancer  
/
HY-P2360 G12
G12 (Ras 5-17) is a wild-type Ras peptide consisted of amino acids 5-17 (KLVVVGAGGVGKS). G12 can be used as a control of mutant Ras peptides studies (such V12).
Ras  
/
HY-B0183S Ellagic acid-13C12
Ellagic acid-13C12 is 13 C-labeled Ellagic acid (HY-B0183). Ellagic acid is a natural antioxidant and acts as a potent and ATP-competitive inhibitor of CK2 and SHP2, with an IC50 of 40 nM and a Ki of 20 nM.
Isotope-Labeled Compounds  
/
HY-P10051 Cyclorasin 9A5
Cyclorasin 9A5 is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC50 of 120 nM.
Ras   Raf  
Cancer  
/
HY-19700R trans-Zeatin (Standard)
trans-Zeatin (Standard) is the analytical standard of trans-Zeatin. This product is intended for research and analytical applications. trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
Reference Standards   MEK   ERK   Endogenous Metabolite  
/
HY-P3277A KRpep-2d TFA
KRpep-2d (TFA) is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research.
Ras  
/
HY-P2361 S12
S12 is a mutant RAS peptide containing the Gly (G) to Ser (S12) substitution. The sequence of the peptide is KLVVVGASGVGKS.
Ras  
/
HY-B0185G Lidocaine (GMP)
Lidocaine (GMP) is Lidocaine (HY-B0185) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Lidocaine inhibits sodium channels involving complex voltage and using dependence. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia.
Apoptosis   ERK   MEK   Sodium Channel   NF-κB  
/
HY-146127 Grb2 SH2 domain inhibitor 1
Grb2 SH2 domain inhibitor 1 is an inhibitor of the Grb2 SH2 domain with an IC50 of 0.40 μM. Grb2 SH2 domain inhibitor 1 is also a cell-permeable cyclic peptide that can enter the cytosol of mammalian cells. Grb2 SH2 domain inhibitor 1 downregulates the expression level of p-MEK. Grb2 SH2 domain inhibitor 1 can be used in the research of breast cancer.
MEK  
Breast Cancer  
/
HY-P3444 CD31
CD31 (PECAM-1) is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cell activation-.
SHP2   Bacterial  
Inflammation or Immune System Disease   Metabolic or Endocrine Disease  
/
HY-P991413 ZEB85
ZEB85 is a human monoclonal antibody (mAb) targeting TrkB. ZEB85 activates TrkB and its downstream cascades, including the ERK, PLCγ, AKT, MAPK signaling pathways and cFOS expression, and enhances neuronal activity. ZEB85 prevents β-amyloid toxicity in cultured hippocampal neurons. ZEB85 is applicable to the research of Alzheimer's disease (AD).

Species: Human

Trk Receptor   ERK   Akt   p38 MAPK  
Neurological, Eye or Ear Disease   Vaccine and Immunization  
/
HY-10999S Trametinib-d4
Trametinib-d4 is the deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.
MEK   Autophagy   Apoptosis  
Cancer  
/
HY-118563 Farnesylthioacetic acid
Farnesylthioacetic acid is a competitive, non-substrate inhibitor of Prenylcysteine α-carboxyl methyltransferase. It acts as a non-substrate competitive inhibitor of Arabidopsis thaliana Prenylcysteine α-carboxyl methyltransferase and blocks methyltransferase activity. Farnesylthioacetic acid does not inhibit protein farnesyltransferase activity in Arabidopsis. It induces Apoptosis. Farnesylthioacetic acid regulates the subcellular localization of Ras protein, reducing the proportion of cytoplasmic Ras protein without disrupting membrane binding. It enhances ABA-induced seed dormancy, delays seed germination, and promotes maximum stomatal closure at lower exogenous ABA concentrations. Farnesylthioacetic acid can be used in studies related to promyelocytic leukemia.
ICMT   Apoptosis   Ras  
Leukemia/Lymphoma/Myeloma  
/
HY-13064S1 Cobimetinib-d4 hydrochloride
Cobimetinib-d4 hydrochloride is deuterated labeled Cobimetinib (HY-13064). Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
MEK   Apoptosis   Isotope-Labeled Compounds  
/
HY-B1272AS Desipramine-d4
Desipramine-d4 is the deuterium labeled Desipramine (HY-B1272A). Desipramine is a first-generation tricyclic antidepressant. Desipramine selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine can be used for the research of hepatocellular cancer, inflammation, and neurological diseases.
Adrenergic Receptor   ERK   JNK   p38 MAPK   NF-κB   AP-1   Apoptosis   Reactive Oxygen Species (ROS)   Mitochondrial Metabolism   TNF Receptor  
Cancer   Neurological, Eye or Ear Disease   Inflammation or Immune System Disease  
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HY-B0183R Ellagic acid (Standard)
Ellagic acid (Standard) is the analytical standard of Ellagic acid. This product is intended for research and analytical applications. Ellagic acid is a natural antioxidant, and acts as a potent and ATP-competitive inhibitor of CK2 and SHP2, with an IC50 of 40 nM and a Ki of 20 nM.
Reference Standards   Casein Kinase   Reactive Oxygen Species (ROS)   Endogenous Metabolite   SHP2  
Cancer   Neurological, Eye or Ear Disease  
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HY-107417 Hypothemycin
Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively.

Source: Hypomyces trichothecoides

VEGFR   MEK   FLT3   PDGFR   ERK  
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HY-P3277 KRpep-2d
KRpep-2d is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research.
Ras  
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HY-19700S trans-Zeatin-d5
trans-Zeatin-d5 is deuterium labeled trans-Zeatin. trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
MEK   ERK   Endogenous Metabolite  
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HY-15001G Stemregenin 1 (GMP)
Stemregenin 1 (SR1) (GMP) is a GMP-grade Stemregenin 1 (HY-15001). GMP-grade small molecules can be used as adjuvants in cell therapy. Stemregenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with an IC50 of 127 nM. Stemregenin 1 (GMP) can competitively bind to AhR and inhibit its nuclear translocation, inhibiting osteoclastogenesis and promoting hematopoietic progenitor cell expansion by blocking the AhR-c-src-NF-κB/p-ERK MAPK-NFATc1 signaling pathway. Stemregenin 1 (GMP) can be used for the study of osteoporosis, in vitro expansion of hematopoietic stem cells, and the study of the mechanism of bone metabolic diseases.
Aryl Hydrocarbon Receptor  
Cancer  
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HY-N9330 Broussoflavonol F
Broussoflavonol F is a potent dual inhibitor of the HER2-RAS-MEK-ERK signaling pathway and mushroom tyrosinase with an IC50 value of 82.3 μM. Broussoflavonol F downregulates the expression of RAS, HER2, phosphorylated BRAF, phosphorylated MEK and phosphorylated Erk proteins. Broussoflavonol F induces cell cycle arrest and apoptosis, and exhibits cytotoxicity in colon cancer cells. Broussoflavonol F inhibits endothelial proliferation, migration and tube formation, suppresses subintestinal vascular development, and reduces the mRNA levels of angiogenesis-associated genes.Broussoflavonol F can be used for colon cancer research.
Xanthine Oxidase   Ras   EGFR   MEK   PERK   Apoptosis  
Colorectal Cancer  
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HY-113313S1 Aldosterone-d7
Aldosterone-d7 is the deuterium labeled Aldosterone. Aldosterone is the primary mineralocorticoid. Aldosterone is a steroid hormone, and it is synthesized and secreted in response to renin-angiotensin system activation (RAS) or high dietary potassium by the zona glomerulosa (ZG) of the adrenal cortex. Aldosterone activity is dependent by the binding and activation of the cytoplasmic/nuclear mineralocorticoid receptor (MR) at cellular level.
Endogenous Metabolite  
Blood or Cardio-cerebrovascular Disease  
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HY-N2375 L-Quebrachitol
L-Quebrachitol is a methoxy analog of inositol that can be isolated from plants. L-Quebrachitol has free-radical scavenging, gastroprotection, anti-platelet aggregation and anti-diabetic activity. L-Quebrachitol promotes osteoblastogenesis by uppregulation of BMP-2, runt-related transcription factor-2 (Runx2), MAPK (ERK, JNK, p38α), and Wnt/β-catenin signaling pathway.
Wnt   β-catenin   p38 MAPK  
Inflammation or Immune System Disease   Lung Cancer   Neurodegenerative Disease   Depression   Pain   Glucose Metabolism   Obesity   Lung Fibrosis  
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HY-141867 Z-FF-FMK
Z-FF-FMK (Z-Phe-Phe-FMK) is a cell-permeable, irreversible, and cysteine protease inhibitor targeting cathepsin-L. Z-FF-FMK inhibits angiotensin II-induced MEK activation in vascular walls, aortic medial remodeling, blood pressure elevation, and upregulation of cystatin C in aortic walls. Z-FF-FMK prevents β-amyloid-mediated caspase-3 activation, poly (ADP-ribose) polymerase cleavage, DNA fragmentation, and apoptosis of cortical neurons (apoptosis). Z-FF-FMK can be used in research related to hypertension and Alzheimer's disease.
Cathepsin   MEK   Caspase   DNA/RNA Synthesis   Apoptosis  
Alzheimer's Disease   Hypertension  
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HY-P1615 Cenupatide
Cenupatide (UPARANT) is a uPAR and FPR antagonist with anti-angiogenic, anti-inflammatory, and vascular barrier regulatory activities, as well as high stability and resistance to enzymatic degradation in blood/plasma. Cenupatide blocks the uPAR-FPR interaction, reduces VEGF-induced phosphorylation levels of AKT, VEGFR-2, STAT3, JNK, p38 MAPK, ERK1/2, and NF-κB p65, and inhibits αvβ3 integrin activation. Cenupatide suppresses endothelial cell migration, invasion, tube formation, and angiogenic signaling pathways, restores tight junctions and blood-retinal barrier integrity, reduces pro-inflammatory marker levels, and inhibits apoptosis. Cenupatide reduces retinal neovascularization, renal fibrosis, and vascular leakage, and restores visual function in preclinical models. Cenupatide is applicable to research related to retinopathy, diabetic complications, ocular diseases, cancer, and inflammatory diseases.
Transmembrane Glycoprotein   Formyl Peptide Receptor (FPR)   VEGFR   Akt   STAT   JNK   p38 MAPK   ERK   NF-κB   Apoptosis   Integrin  
Cancer   Inflammation or Immune System Disease   Blood or Cardio-cerebrovascular Disease   Glucose Metabolism   Retinopathy  
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HY-153740 PF-07284892
PF-07284892 (ARRY-558) is a potent and orally active SHP2 inhibitor with an IC50 value of 21 nM. PF-07284892 decreases the expression of pERK.
SHP2  
Cancer  
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HY-D0168 Orcinol
Orcinol (3,5-Dihydroxytoluene) is an organic compound used in biological dyeing and proteomics research. Orcinol inhibits melanogenesis in B16F10 cells by upregulating the MAPK/ERK signaling pathway, and suppresses the expression of MITF, tyrosinase (TYR), TRP1, and DCT. Orcinol exhibits certain DPPH radical scavenging activity. In addition, Orcinol can alter nitrogen balance in animals. Orcinol holds promise for research in cancer and metabolic diseases.

Source: Aspergillus niger

Fluorescent Dye   Free Radical Scavengers   Tyrosinase   p38 MAPK   ERK  
Cancer   Metabolic or Endocrine Disease  
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HY-P99175 KWAR 23
KWAR23 is an anti-human SIRPα antibody. KWAR23 binds human SIRPα with high affinity and disrupts its binding to CD47. KWAR23 shows antitumor activity in combination with tumor-opsonizing antibodies and can be used in cancer immunotherapy research.

Species: Human

CD47  
Cancer  
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HY-141523 Vociprotafib
Vociprotafib (RMC-4630) is an orally active, selective and potent phosphatase SHP2 inhibitor, which blocks activation of the RAS-RAF-MEK-ERK signaling pathway with antitumor activity. Vociprotafib accelerates the time to, and increases the magnitude of, tumor regressions in Osimertinib (HY-15772)-sensitive EGFR-mutant tumors of mice.
SHP2   Phosphatase  
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HY-156002 LUNA18
LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with KRAS genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer.
Ras   ERK  
Respiratory Disease   Non-Small Cell Lung Cancer  
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HY-P99278 Adecatumumab
Adecatumumab (Anti-Human EPCAM Recombinant Antibody; MT201) is a full human monoclonal antibody of the IgG1 isotype, targeting human EpCAM. Adecatumumab is expressed in almost all adenocarcinomas, and its activity is not dependent of K-Ras status.

Species: Human

Others  
Cancer  
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HY-P10408 Candidalysin
Candidalysin is a cytolytic peptide toxin secreted by the fungus Candida albicans. Candidalysin drives epithelial immune responses by activating the EGFR-MAPK signaling pathway, inducing MMP expression and calcium influx, and regulating the c-Fos transcription factor and MKP1 via p38 MAPK and ERK1/2 respectively. Candidalysin is essential for mucosal and systemic infections, activating NLRP3 to promote inflammatory responses, neutrophil recruitment, and Th17 immunity. Candidalysin activates LDH causing membrane damage and exhibiting cytotoxicity
EGFR   MMP   Calcium Channel   NOD-like Receptor (NLR)   ERK   p38 MAPK  
Infection   Inflammation or Immune System Disease  
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HY-158115 NST-628
NST-628 is a brain-permeable MAPK pathway molecule glue that inhibits RAF phosphorylation and MEK activation. NST-628 also binds RAF and prevents the formation of BRAF-CRAF and BRAF-ARAF heterodimers, effectively inhibiting the RAS-MAPK pathway. NST-628 inhibits RAS- and RAF-driven cancers and demonstrated potent inhibition in mutant KRAS, NRAS, BRAF class II/III, and NF1-mutant tumors.
Molecular Glues   Raf   MEK  
Colorectal Cancer   Liver Cancer   Pancreatic Cancer   Pain   Non-Small Cell Lung Cancer   Lung Adenocarcinoma   Obesity   Rheumatoid Arthritis  
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HY-P74549 SHP-2 Protein, Mouse (HEK293, His)
SHP-2 Protein functions downstream of diverse receptor and cytoplasmic tyrosine kinases, participating in signal transduction from the cell surface to the nucleus.It positively regulates the MAPK pathway and dephosphorylates key proteins like GAB1, ARHGAP35, EGFR, ROCK2, CDC73, and SOX9.Additionally, SHP-2 dephosphorylates NEDD9/CAS-L to modulate cellular processes.SHP-2 Protein, Mouse (HEK293, His) is the recombinant mouse-derived SHP-2 protein, expressed by HEK293 , with C-His labeled tag.

Species: Mouse; Source: HEK293

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HY-P7805 Kras4B Protein, Human (184a.a, G12V, His)
KRAS protein is a key Ras family member that binds GDP/GTP and has intrinsic GTPase activity. Its critical role in regulating cell proliferation emphasizes its importance in cellular processes. Kras4B Protein, Human (184a.a, G12V, His) is the recombinant human-derived KRAS protein, expressed by E. coli , with N-6*His labeled tag and G12V mutation.

Species: Human; Source: E. coli

Enzymes & Regulators Hydrolases (EC 3)

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HY-P74684 Non-structural protein 1/NS1 Protein, H1N1 (His)
Nonstructural protein 1/NS1 plays multiple roles in viral infection.It inhibits cellular pre-mRNA processing by binding to CPSF4 and PABPN1, disrupting normal 3' end processing and halting host protein synthesis.Non-structural protein 1/NS1 Protein, H1N1 (His) is the recombinant Virus-derived Non-structural protein 1/NS1 protein, expressed by E.coli , with N-His labeled tag.

Species: Virus; Source: E. coli

Viral Proteins Influenza Viruses Proteins Influenza Non-structural Protein 1

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HY-P701974 RRAS2 Protein, Human
RRAS2 protein, a GTP-binding with GTPase activity, crucially regulates the MAPK signaling pathway, impacting diverse cellular processes and playing a pivotal role in orchestrating cellular responses. Its influence extends to regulating craniofacial development, emphasizing its multifaceted role in biological pathways essential for proper cellular and developmental outcomes. RRAS2 Protein, Human is the recombinant human-derived RRAS2 protein, expressed by E. coli , with tag free.

Species: Human; Source: E. coli

Enzymes & Regulators Hydrolases (EC 3)

/
HY-P77781 HLA-A*0301 KRAS G12V Complex Protein, Human (HEK293, His-Avi)
HLA-A*0301 collaborates with B2M to present viral and tumor peptides that direct CD8-positive T cells to respond against infected or transformed cells. It can also present self-peptides to avoid self-reaction. HLA-A*0301 KRAS G12V Complex Protein, Human (HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-A*0301 and B2M/Beta-2-microglobulin Protein, expressed by HEK293, with C-Avi, C-His labeled tag and VVGAVGVGK peptide. HLA-A*0301 KRAS G12V Complex Protein, Human (HEK293, His-Avi), has molecular weight of 55-60 kDa.

Species: Human; Source: HEK293

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HY-P77783 HLA-A*11:01&B2M&KRAS G12D(VVVGADGVGK) Protein, Human (HEK293, His-Avi)

Species: Human; Source: HEK293

/
HY-P77789 HLA-A*03:01&B2M&KRAS WT(VVVGAGGVGK) Protein, Human (HEK293, His-Avi)

Species: Human; Source: HEK293

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HY-P77790 HLA-A*03:01&B2M&KRAS WT(VVVGAGGVGK) Protein, Human (Biotinylated, HEK293, His-Avi)

Species: Human; Source: HEK293

Biotinylated Proteins

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HY-P700929 HLA-A*11:01&B2M&KRAS WT(VVVGAGGVGK) Monomer Protein, Human (Biotinylated, HEK293, His-Avi)

Species: Human; Source: HEK293

Biotinylated Proteins

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HY-P700930 HLA-A*11:01&B2M&KRAS WT(VVVGAGGVGK) Monomer Protein, Human (HEK293, His-Avi)

Species: Human; Source: HEK293

/
HY-P700931 HLA-A*11:01&B2M&KRAS WT(VVVGAGGVGK) Tetramer Protein, Human (HEK293, His-Avi)

Species: Human; Source: HEK293

/
HY-P701975 RRAS2 Protein, Human (His, StrepⅡ)
RRAS2 protein, a GTP-binding with GTPase activity, crucially regulates the MAPK signaling pathway, impacting diverse cellular processes and playing a pivotal role in orchestrating cellular responses. Its influence extends to regulating craniofacial development, emphasizing its multifaceted role in biological pathways essential for proper cellular and developmental outcomes. RRAS2 Protein, Human (His, Strep) is the recombinant human-derived RRAS2 protein, expressed by E. coli , with N-Strep, N-6*His labeled tag.

Species: Human; Source: E. coli

Enzymes & Regulators Hydrolases (EC 3)

/
HY-P704877 SHP-2 Protein, Human (N-His)
The SHP-2 protein is a key player downstream of the receptor and cytoplasmic protein tyrosine kinases, facilitating signal transduction from the cell surface to the nucleus. It actively regulates the MAPK pathway and dephosphorylates key substrates, including GAB1, ARHGAP35, EGFR, ROCK2 ("Tyr-722"), and CDC73. SHP-2, Human (N-His) is the recombinant human-derived SHP-2 protein, expressed by E. coli, with C-mFc labeled tag.

Species: Human; Source: E. coli

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HY-P87170 KRAS Antibody (YA6861)
KRAS Antibody (YA6861) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to KRAS.

Host: Mouse; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Flow Cytometry Antibodies Primary Antibodies

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HY-P86935 KRAS Antibody (YA6628)
KRAS Antibody (YA6628) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to KRAS.

Host: Mouse; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

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HY-P80513 Phospho-SHP2 (Tyr542) Antibody (YA154)
Phospho-SHP2 (Tyr542) Antibody (YA154) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Phospho-SHP2 (Tyr542).

Host: Rabbit; Reactivity: Mouse

Monoclonal Antibodies Recombinant Antibodies Modification Specific Antibodies Primary Antibodies

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HY-P81898 SHP2 Antibody (YA1643)
SHP2 Antibody (YA1643) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to SHP2.

Host: Rabbit; Reactivity: Human

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

/
HY-P81898A SHP2 Antibody (YA1643)(PBS only)
SHP2 Antibody (YA1643) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to SHP2.

Host: Rabbit; Reactivity: Human

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

/
HY-P84492 SHP2 Antibody (YA4189)
SHP2 Antibody (YA4189) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to SHP2.

Host: Mouse; Reactivity: Human

Monoclonal Antibodies Flow Cytometry Antibodies Primary Antibodies

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HY-P84492A SHP2 Antibody (YA4189)(PBS only)
SHP2 Antibody (YA4189) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to SHP2.

Host: Mouse; Reactivity: Human

Monoclonal Antibodies Primary Antibodies

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HY-P810818 RRAS2 Antibody (YA10061)
RRAS2 Antibody (YA10061) is a Mouse-derived and non-conjugated IgG1 Monoclonal antibody, targeting to RRAS2.

Host: Mouse; Reactivity: Human, Mouse

Monoclonal Antibodies Primary Antibodies

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HY-P83335 MRAS Antibody (YA3080)
MRAS Antibody (YA3080) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to MRAS.

Host: Rabbit; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

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HY-P85464 RASSF1 Antibody (YA5156)
RASSF1 Antibody (YA5156) is a Mouse-derived and non-conjugated monoclonal antibody, targeting to RASSF1.

Host: Mouse; Reactivity: Human

Monoclonal Antibodies Primary Antibodies

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HY-P86320 SH-PTP2 Antibody (YA6012)
SH-PTP2 Antibody (YA6012) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to SH-PTP2.

Host: Rabbit; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

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HY-P87281 Rab3A Antibody (YA6964)
Rab3A Antibody (YA6964) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Rab3A.

Host: Rabbit; Reactivity: Human, Mouse, Rat

Monoclonal Antibodies Recombinant Antibodies Flow Cytometry Antibodies Primary Antibodies

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HY-P87380 ERAS Antibody (YA7063)
ERAS Antibody (YA7063) is a Mouse-derived and non-conjugated IgG1 monoclonal antibody, targeting to ERAS.

Host: Mouse; Reactivity: Human, Mouse

Monoclonal Antibodies Primary Antibodies

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HY-P87534 RASA1 Antibody (YA7218)
RASA1 Antibody (YA7218) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to RASA1.

Host: Rabbit; Reactivity: Human, Rat, Mouse

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

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HY-P87571 RASSF1A Antibody (YA7255)
RASSF1A Antibody (YA7255) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to RASSF1A.

Host: Rabbit; Reactivity: Human

Monoclonal Antibodies Recombinant Antibodies Primary Antibodies

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Keywords

MAPK/ERK signaling | MEK inhibitors | immune checkpoint blockade | RAS | SHP2 | combination immunotherapy