Inflammation/Immunology

Isomangiferin is an orally active xanthone C-glucoside, and its chemical structure is similar to Mangiferin (HY-N0290). Isomangiferin is an effective VEGFR-2 kinase inhibitor, which can induces cell apoptosis, inhibit the growth, metastasis and angiogenesis of breast cancer. Isomangiferin exerts anti-inflammatory effects by inhibiting the HMGB1/NLRP3/NF-κB signaling pathway, thereby improving the renal function indicators of diabetic mice. Isomangiferin exhibits inhibitory effects on various bacteria and herpes simplex virus type 1 (HSV-1). Isomangiferin promotes the migration and osteogenic differentiation of bone marrow mesenchymal stem cells (BMSCs) and reduces cell apoptosis and the production of ROS by activating the AMPK/ACC pathway, thereby facilitating fracture healing.

LR-17 (TLT-1 (94-110)), a 17-aa peptide, is a TREM-1 inhibitor. LR-17 shows anti-inflammatory effects that can reduce the secretion of pro-inflammatory cytokines induced by Lipopolysaccharides (HY-D1056) (LPS). LR-17 can be used for the study of sepsis.

Etrinabdione (EHP-101; VCE-004.8) is an orally active, specific PPARγ and CB₂ receptor dual agonist. Etrinabdione inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. Etrinabdione, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. Etrinabdione attenuates adipogenesis and prevents diet-induced obesity.

RNF5 agonist 1 (analog-1), a structural analog of RNF5 inhibitor inh-02 (HY-123967), is a potent RNF5 agonist. RNF5 agonist 1 increases the ubiquitylation status of ATG4B in F508del-CFTR-expressing CFBE41o- cells.

PAR-4 (1-6) amide human is an N-terminal fragment of protease-activated receptor 4 (PAR4). PAR-4 (1-6) amide human induce platelet aggregation.

PSP-0119 is a highly efficient and effective PROTAC degrader targeting IRAK4 (IC₅₀ = 2.83 nM). PSP-0119 can inhibit IRAK4 kinase activity, NF-κβ activity, and IL-1β-induced IRAK4 phosphorylation. PSP-0119 degrades IRAK4 in FLT3-mutant AML cell lines, sparing FLT3-wild-type AML cells, FLT3-wild-type samples, and normal bone marrow. PSP-0119 downregulates alpha-enolase (eNOS) of MOLM-13 cells. PSP-0119 can be used for the study of Acute Myeloid Leukemia (AML).

3-Oxo-7-hydroxychol-4-enoic acid is an endogenous metabolite. 3-Oxo-7-hydroxychol-4-enoic acid may be an important indicator of a poor prognosis in hepatobiliary disease.

SM-17 is a human monoclonal antibody targeting IL-17RB. SM-17 binds to human IL-17RB, inhibits the dimerization of IL-17RA/IL-17RB, blocks IL-25-induced phosphorylation of ERK1/2 and STAT5, and suppresses Th2-mediated inflammatory responses. SM-17 inhibits the secretion of IL-5, IL-9, IL-13 and IL-4, impairs the proliferation/expansion of ILC2 and Th2 cells, and restores filaggrin expression. SM-17 reduces immune cell infiltration, epidermal hyperplasia, goblet cell hyperplasia, collagen deposition, ear swelling and scratching behavior in animal models. SM-17 can be used in research related to atopic dermatitis and allergic asthma.

VRT-325 is a CFTR modulator. VRT-325 inhibits disulfide cross-linking between cysteines in transmembrane segments 6 and 7 of CFTR and P-gp. VRT-325 promotes maturation of CFTR and P-gp processing mutants, rescues ΔF508-CFTR folding at the endoplasmic reticulum. VRT-325 binds ΔF508-CFTR nucleotide-binding domain 1, and increases mature ΔF508-CFTR cell surface expression and chloride conductance. VRT-325 can be used for the research of cystic fibrosis^[1][3].

Histamine dihydrochloride (Standard) is the analytical standard of Histamine dihydrochloride (HY-B0722). This product is intended for research and analytical applications. Histamine dihydrochloride is the agonist for histamine receptor and a vasodilator. Histamine dihydrochloride is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine dihydrochloride affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine dihydrochloride can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.

Fenobucarb is a carbamate insecticide. Fenobucarb induces zebrafish developmental neurotoxicity through pathways involved in inflammation, oxidative stress, degeneration and apoptosis. Fenobucarb is a possible risk factor to cardiovascular and cerebrovascular systems in animals.

Porustobart (HBM-4003) is a fully human anti-CTLA-4 heavy chain only antibody (HCAb). Porustobart can significantly improve the depletion of regulatory T cells (Treg cells) with high CTLA-4 expression in tumor tissues by enhancing ADCC activity. Porustobart can be used for tumor research.

PF-00356231 hydrochloride is a specific, non-peptidic, non-zinc chelating ligand and inhibitor of matrix metalloproteinase MMP-12 (IC₅₀=1.4 μM). PF-00356231 hydrochloride binds to MMP-12 and forms PF-00356231/MMP-12 complex. PF-00356231 hydrochloride shows potency against MMP-13, MMP-8, MMP-9, MMP-3 with IC₅₀s of 0.00065, 1.7, 0.98, 0.39 μM, respectively.

PROTAC BTK Degrader-6 is an orally active PROTAC-based BTK degrader with a DC₅₀ of 3.18 nM. PROTAC BTK Degrader-6 induces BTK degradation via proteasomal degradation, ubiquitination, and CRBN ligase recruitment pathways. PROTAC BTK Degrader-6 inhibits NF-κB activation, mRNA expression of IL-1β and IL-6, as well as the secretion of pro-inflammatory cytokines. PROTAC BTK Degrader-6 reduces inflammatory responses in a zymosan-induced mouse model of peritonitis. PROTAC BTK Degrader-6 can be used in peritonitis-related research.

(±)-ML 209 (compound 4n), a diphenylpropanamide, is a retinoic acid-related orphan receptor RORγ antagonist with an IC₅₀ of 1.1 μM. (±)-ML 209 inhibits RORγt transcriptional activity with an IC₅₀ of 300 nM in HEK293t cells. (±)-ML 209 inhibits the transcriptional activity of RORγt, but not RORα in cells. (±)-ML 209 selectively inhibits murine Th17 cell differentiation without affecting the differentiation of naïve CD4⁺ T cells into other lineages, including Th1 and regulatory T cells.

Ro 25-1553 TFA is a 31 amino acid vasoactive intestinal peptide (VIP) analog, that acts as an agonist for VIP2 receptor (VPAC2 receptor). Ro 25-1553 TFA exhibits a bronchodilator effect in nerve-induced or Carbachol (HY-B1208)-induced tracheal smooth muscle contraction in guinea pig model.

Benzoin (DL-Benzoin) is a PI3Kα inhibitor with anticancer effects. Benzoin inihits the growth of colon cancer cell line (HCT-116).

SIRT6-IN-3 (compound 8a) is a selective inhibitor of SIRT6 (IC₅₀=7.49 μM). SIRT6-IN-3 inhibits pancreatic ductal adenocarcinoma (PDAC) cells proliferation and induces apoptosis. SIRT6-IN-3 increases the sensitivity of cancer cells to gemcitabine (HY-17026) via blocking the DNA damage repair pathway. SIRT6-IN-3 is used in pancreatic cancer research.

Sodium gualenate (Guaiazulenesulfonate sodium) is a hydrophilic derivative of guaiazulene with excellent anti-inflammatory and wound-healing effects mainly used for the treatment of duodenal ulcer, gastric ulcer and gastritis.

KY-1044 (Alomfilimab; SAR 445256) is a fully human IgG1 antibody targeting inducible costimulatory receptor (ICOS). KY-1044 depletes ICOS^high cells via antibody-dependent cellular cytotoxicity (ADCC) through the engagement of FcgRIIIa. KY-1044 act as a costimulatory molecule on cells expressing lower ICOS levels, such as CD8⁺ T_Eff cells (through FcgR-dependent clustering). KY-1044 exploit the differential expression of ICOS on T-cell subtypes to improve the intratumoral immune contexture and restore an antitumor immune response.