p38 MAPK Activator

(R)-Bromoenol lactone ((R,E)-Bromoenol lactone) is an isomer of Bromoenol lactone (HY-107411). (R)-Bromoenol lactone acts as a selective inhibitor of microsomal calcium-independent phospholipase A2γ (iPLA2γ). (R)-Bromoenol lactone induces mild activation of p38 mitogen-activated protein kinase in prostate cancer cells, resulting in slight increases in the expressions of phosphorylated p53, total p53 and p21. (R)-Bromoenol lactone is applicable to prostate cancer-related research.

Aspirin (Acetylsalicylic Acid) lithium is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC₅₀ values of 5 and 210 μg/mL, respectively. Aspirin lithium induces apoptosis. Aspirin lithium inhibits the activation of NF-κB. Aspirin lithium also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.

Aspirin DL-lysine (ASA DL-lysine) is a lysine-containing aspirin derivative. Aspirin DL-lysine inhibits cyclooxygenase (COX) in platelets, blocks the synthesis of thromboxane A2 (TXA2), and thus inhibits platelet aggregation and activation. Aspirin DL-lysine can be used to study thrombin generation in patients with unstable angina pectoris.

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.

Buforin IIb TFA (BF2-B TFA) is an anticancer peptide, as well as an Antibacterial and Antifungal agent. Buforin IIb TFA is derived from histone H2A. Buforin IIb TFA activates SAPK/JNK and p38 MAPK. Buforin IIb TFA induces mitochondria-dependent Apoptosis. Buforin IIb TFA achieves selective targeting by interacting with gangliosides on the surface of cancer cells, and can penetrate cancer cell membranes without causing damage. Buforin IIb TFA exhibits antibacterial activity against Gram-negative bacteria, Gram-positive bacteria and fungi. Buforin IIb TFA can be used in the research of cervical cancer, as well as cancers including leukemia, central nervous system cancer, ovarian cancer, breast cancer, melanoma, colon cancer, non-small cell lung cancer, renal cancer and prostate cancer.

WMJ-J-09 is an HDAC inhibitor with IC₅₀ values of 7.5 nM (HDAC1), 21.3 nM (HDAC2), 18.4 nM (HDAC3), 90.9 nM (HDAC8), 3.9 nM (HDAC6) and 8715.7 nM (HDAC4). WMJ-J-09 blocks the cell cycle and induces apoptosis in cancer cells. WMJ-J-09 induces cancer cell death through the LKB1-AMPK-p38MAPK-p63-survivin signaling cascade.WMJ-J-09 inhibits HDAC enzyme activity, leading to acetylation of key proteins and thereby regulating cancer cell death. WMJ-J-09 can be used in HCT116 cells and FaDu cells research^[1][2].

LY-2624587 is a humanized IgG4 monoclonal antibody antagonist targeting CXCR4. LY-2624587 blocks SDF-1/CXCR4 interaction and SDF-1-induced GTP binding. LY-2624587 significantly inhibits cell migration and induces apoptosis in human lymphoma and leukemia cells. LY-2624587 also inhibits CXCR4 and SDF-1 mediated cell signaling including activation of MAPK and AKT. LY-2624587 can be used for human hematological malignancies like acute myeloid leukemia (AML) research.

MAPK-IN-3 (Compound 4a) is an anti-proliferative agent that shows particularly strong inhibitory effects on KYSE 30, HCT 116, and HGC 27, with IC₅₀ values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. MAPK-IN-3 blocks the cell cycle via a p53-dependent mechanism and induces cell apoptosis through a p53-independent mechanism. MAPK-IN-3 downregulates the expression of cell cycle-related proteins like Cyclin D1 and cyclin B1, upregulates pro-apoptotic proteins such as cleaved PARP, cleaved caspase-7, and cleaved caspase-9, and reduces the expression of anti-apoptotic proteins like Bcl-2. Additionally, MAPK-IN-3 increases the intracellular level of ROS in KYSE 30 cells and upregulates the expression of members of the MAPK signaling pathway associated with ROS, such as p-ERK, p-p38 and p-JNK.

Iroxanadine (BRX 005) sulfate is a vasculoprotector. Iroxanadine is a p38 kinase and HSP protein dual activator. Iroxanadine sulfate has the potential for atherosclerosis and vascular diseases research.

Apoptosis/necroptosis inducer 1 is an orally active and brain-penetrant apoptosis and necroptosis inducer. Apoptosis/necroptosis inducer 1 induces mitochondria-dependent (intrinsic pathway) apoptosis. Apoptosis/necroptosis inducer 1 induces necroptosis by activating the TNF-α/NF-κB/MAPK signaling pathway. Apoptosis/necroptosis inducer 1 exhibits antiproliferative activity in glioblastoma cell lines and multiple solid tumor types. Apoptosis/necroptosis inducer 1 inhibits growth of orthotopic glioblastoma in animal models and improves survival rate. Apoptosis/necroptosis inducer 1 can be used for the research of glioblastoma.

Nrf2 activator-23 is an orally active Keap1 binder and Nrf2 activator, with K_D values of 28.68 nM and 54.55 nM for Keap1 and its Kelch domain, respectively. Nrf2 activator-23 disrupts the Keap1-Nrf2 interaction, reduces ubiquitination and degradation of Nrf2, and activates the Nrf2 signaling pathway. Nrf2 activator-23 inhibits RANKL-induced osteoclast formation, bone resorptive activity, ROS production, and activation of the MAPK and NF-κB signaling pathways, while downregulating the expression of osteoclast-specific genes and proteins. Nrf2 activator-23 attenuates bone loss and reduces osteoclast formation in vivo without affecting osteoblast differentiation and mineralization. Nrf2 activator-23 can be used for the research of osteoporosis.

NSF-951 (ZINC67299692) is a TLR4 agonist (K_d = 16.01 μM). NSF-951 activates the p38 and JNK kinase pathways. NSF-951 induces IL-6 and TNF-α responses and upregulates CD80 and CD86 expression. In mouse immunization studies, NSF-951 alone or in combination with Alum enhances antigen-specific antibody and T cell responses.

Cyproheptadine-d₃ is the d₃-labeled Cyproheptadine (HY-B1622). Cyproheptadine acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.

Nur77 antagonist 2 (Compound 12b) is an orally active Nur77 antagonist with a K_D value of 0.42 μM. Nur77 antagonist 2 exhibits proliferative activity on liver cancer cells. Nur77 antagonist 2 stabilizes Nur77 by inhibiting its ubiquitin-proteasomal degradation, leading to Nur77-dependent apoptosis via the ASK1-JNK/p38 pathway. Nur77 antagonist 2 inhibits tumor growth in the HCCLM3 xenograft model. Nur77 antagonist 2 can be used for the study of hepatocellular carcinoma (HCC).

SMU-C68 is a highly selective small-molecule TLR1/2 heterodimer agonist (EC₅₀=0.009 μM). SMU-C68 activates NF-κB and MAPK pathways to promote pro-inflammatory cytokine release (e.g., TNF-α, IL-1β). SMU-C68 is promising for research of cancers.

Nitrovin (Difurazon) is an orally active inhibitor of thioredoxin reductase 1 (TrxR1) with both antibacterial and anticancer activities. Nitrovin induces ROS generation and endoplasmic reticulum stress by targeting and inhibiting TrxR1, which in turn induces cytoplasmic vacuolation, activates MAPK, and inhibits Alix. Nitrovin induces paraptosis-like non-apoptotic cell death, thereby exerting significant cytotoxicity against cancer cells. Nitrovin is used for research on glioblastoma, liver cancer, and bacterial infections.

Diphenylcyclopropenone (Standard) is the analytical standard of Diphenylcyclopropenone. This product is intended for research and analytical applications. Diphenylcyclopropenone (Diphencyprone) is a topical immunomodulatory agent that can be used for alopecia areata research.

β-Zearalenol-¹³C₁₈ is the ¹³C-labeled β-Zearalenol (HY-N6741). β-Zearalenol is a zearalenone metabolite and Estrogen receptor binder (K_d = 0.406 nM) that induces apoptosis through activation of p53, JNK, and p38 kinases and the mitochondrial apoptosis pathway, while inhibiting CYP19A1 and inducing autophagy via SIRT1. β-Zearalenol is used in research on cardiotoxicity, mycotoxin-induced reproductive toxicity, and breast cancer.

Pam2CSK4 is a TLR2 agonist. Pam2CSK4 induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis.

Rotundic acid (Standard) is the analytical standard of Rotundic acid (HY-N2217). This product is intended for research and analytical applications. Rotundic acid is an orally effective triterpenoid with a K_d value of 51.3 µM for PTP1B. Rotundic acid downregulates the AKT/mTOR pro-survival pathway and modulates the MAPK pathway. Rotundic acid induces cell cycle S-phase arrest, DNA damage and apoptosis; it inhibits migration, invasion, angiogenesis and proliferation of cancer cells. Rotundic acid improves leptin sensitivity, regulates gut microbiota and reduces cellular senescence. Rotundic acid can be used in research related to hepatocellular carcinoma, obesity, aging, acute lung injury and type 2 diabetes.