Interleukin Related Activator

(R)-Zelebrudomide ((R)-NX-2127) is an isomer of Zelebrudomide (HY-153220). Zelebrudomide is an orally active BTK-targeting PROTAC degrader, with DC₅₀ values of 4.5 nM and 31 nM against wild-type BTK and BTK^C481S mutant, respectively. Zelebrudomide recruits the cereblon E3 ubiquitin ligase complex to mediate the degradation of BTK. Zelebrudomide also acts as a molecular glue to bind the cereblon E3 ubiquitin ligase complex, mediating the degradation of IKZF1 and IKZF3. Zelebrudomide can be used in the research of B-cell malignancies.

Y11 inhibits the autophosphorylation of FAK1 by blocking the phosphorylation of Y397. Y11 increases the expression level of IL-6. Y11 is applicable for cancer research.

13-Methylberberine chloride (13-Methylberberinium chloride), a berberine analogue, has anti-adipogenic and antitumor activities. 13-Methylberberine chloride (13-Methylberberinium chloride) increases production of IL-12 and inhibits the expression of iNOS at posttranscriptional level in macrophages activated with LPS.

Tris(2-chloroethyl)phosphate-d₁₂ is the deuterium labeled Tris(β-chloroethyl) phosphate. Tris(2-chloroethyl) phosphate is a widely used organic phosphorus flame retardant, mainly used as a plasticizer. Tris(2-chloroethyl) phosphate has orally active hepatotoxicity, inducing an increase in reactive oxygen species (ROS) and calcium ions (Ca²⁺) influx, a decrease in mitochondrial membrane potential (△Ψm), and causing DNA damage and cell apoptosis. Tris(2-chloroethyl) phosphate directly binds to FXR, inducing obesity and the formation of fatty liver in mice. Chloroethyl) phosphate activates the TLR4/NF-κB pathway, triggering liver inflammation.

Calotatug ginistinag (XMT-2056) is an antibody-drug conjugate (ADC) targeting HER2, linked to a payload composed of XMT-1519 conjugate-1 (HY-148067) and STING agonist-20 (HY-148068). Calotatug ginistinag activates the STING signaling pathway in tumor cells and tumor-resident immune cells, induces the production of type I interferons and cytokines (CXCL10, IFN-β, IL-6, TNF-α, triggers innate anti-tumor immune responses, and exerts a bystander effect. Calotatug ginistinag exhibits efficacy against HER2-expressing cancer cells in co-culture with PBMCs. Calotatug ginistinag induces tumor regression and reduces systemic inflammation in various tumor models. Combination treatment with Calotatug ginistinag, Trastuzumab (HY-P9907) and T-DXd (HY-138298) yields benefits. Calotatug ginistinag can be used in studies related to HER2-expressing solid tumors such as breast cancer, gastric cancer and ovarian cancer.

Cetrelimab (JNJ 63723283; JNJ 3283) is a human IgG4κ mAb targeting PD-1. Cetrelimab binds PD-1 (K_d=1.72 nM, HEK293) to block the interaction of PD-1 with PD-L1 and PD-L2 (IC₅₀s=111.7 ng/mL and 138.6 ng/mL, respectively). Cetrelimab stimulates peripheral T cells, increases IFN-γ, IL-2, TNF-α level and inhibits tumor growth in vivo.

Glycochenodeoxycholic acid (Standard) is the analytical standard of Glycochenodeoxycholic acid. This product is intended for research and analytical applications. Glycochenodeoxycholic acid (Chenodeoxycholylglycine) is a relatively toxic bile salt generated in the liver from chenodeoxycholic acid and glycine. Glycochenodeoxycholic acid inhibits Autophagosome formation and impairs lysosomal function by inhibiting lysosomal proteolysis and increasing lysosomal pH in human normal liver cells, leading to the Apoptosis of human hepatocyte cells. Glycochenodeoxycholic acid induces stemness and chemoresistance via activating STAT3 signaling pathway in hepatocellular carcinoma cells (HCC). Glycochenodeoxycholic acid is promising for research in the field of cholestasis desease, hepatocellular carcinoma and primary sclerosing cholangitis (PSC)[1][2][3][4].

Emfizatamab (GNC-038) is a monoclonal antibody against CD19/CD3E/TNFRSF9/PD-L1. Emfizatamab exhibits antitumor activity, being capable of activating CD3 and 4-1BB signals on T cells, as well as targeting the high expression of CD19 or PD-L1 on tumor cells. Emfizatamab functions as a CD19-specific T cell engager by mediating direct antitumor activity. Emfizatamab can also overcome the inhibition of T cells by PD-L1. Emfizatamab can be used in the research of tumors such as R/R non-Hodgkin lymphoma or acute lymphoblastic leukemia.

Lauroyl-L-carnitine-d₉ chloride is the deuterium labeled Lauroyl-L-carnitine chloride (HY-130321). Lauroyl-L-carnitine chloride is an orally active metabolite. Lauroyl-L-carnitine chloride significantly reverses the decrease in its target gene IL-10. Lauroyl-L-carnitine chloride alleviates Crohn' s-like colitis.

M199 is a potent TLR3/TLR9 signaling inhibitor. M199 induces secretion of IL-6, IL-8 and TNFα in human PBMCs. M199 is used as a selective inducer of the immune response.

Lauroyl-L-carnitine-d₃ (chloride) is the deuterium labeled Lauroyl-L-carnitine chloride (HY-130321). Lauroyl-L-carnitine chloride is an orally active metabolite. Lauroyl-L-carnitine chloride significantly reverses the decrease in its target gene IL-10. Lauroyl-L-carnitine chloride alleviates Crohn' s-like colitis.

5(S)15(S)-DiHETE is an “activated” intermediate, inhibits platelet aggregation with an IC₅₀ of 1.3 μM. 5(S)15(S)-DiHETE enhances the rate of either LXA4 or LXB4 biosynthesis.

PROTAC HPK1 Degrader-3 is an orally active, PROTAC degrader that selectively targets HPK1, with a DC₅₀ of 21.26 nM. PROTAC HPK1 Degrader-3 induces HPK1 degradation via the ubiquitin-proteasome system and forms a stable ternary complex with HPK1 and CRBN. It inhibits the SLP76 and NF-κB signaling pathways, enhances MAPK signal transduction, reverses the immunosuppressive factor-mediated inhibition of T cell cytokine secretion, and promotes the secretion of T cell immune cytokines. PROTAC HPK1 Degrader-3 suppresses tumor growth and enhances anti-PD-L1-mediated antitumor activity. It can be used in studies related to malignant tumors, such as colorectal cancer.

Pinus pinaster bark extract is extracted from the bark of pine bark with antioxidant, anti-inflammatory and neuroprotective effects. Pinus pinaster bark extract increases toll-like receptor (TLR) activity, inducing production of IL-10.

Flt-3L-Ig (hum/hum) (hFlt3L) is a Flt3 ligand. Flt-3L-Ig (hum/hum) enhances the release of inflammatory cytokines from myeloid cells and dendritic cells in BRGSF-CBC mice induced by OKT3. Flt-3L-Ig (hum/hum) increases the release of IL-2, CCL2 and CXCL10 in an OKT3-dependent manner. Flt-3L-Ig (hum/hum) can be used in studies related to cytokine release syndrome. Flt-3L-Ig (hum/hum) can be used in studies related to psoriasis-like skin inflammation.

Arecaidine hydrobromide is a GABA transport system inhibitor. Arecaidine hydrobromide inhibits the proliferation of oral mucosal fibroblasts, increases the secretion of IL-6, TGF-β and TNF-α in cells, downregulates the expression of PPAR-γ and PCK1 in cells, and upregulates the expression of TGF-β1. Arecaidine hydrobromide inhibits the uptake of γ-aminobutyric acid and β-alanine by the central nervous system of cats. Arecaidine hydrobromide inhibits hPAT1-mediated L-[³H]proline uptake in cells. Arecaidine hydrobromide can be used in research related to neurological diseases.

Propacetamol is an orally active prodrug of Acetaminophen (HY-66005), which exerts antipyretic and analgesic effects after metabolism. Propacetamol reduces Aspirin (ASA) (HY-14654)-induced elevation of malondialdehyde (MDA) in gastric mucosa and plasma, regulates the levels of gastric mucosal glutathione (GSH and GSSG) to maintain cellular antioxidant defense, and increases gastric mucosal uric acid (UA) levels. Propacetamol exerts a dose-dependent protective effect against ASA-induced gastric mucosal damage in rats. Propacetamol can be used for the study of gastric mucosal injury by interfering with oxidative stress.

RIBI-529 (RC-529) is a fully synthetic, low-toxicity TLR4 agonist vaccine adjuvant. RIBI-529 upregulates cell surface co-stimulatory molecules, receptors, cytokines and chemokines, and activates the innate immune system. RIBI-529 enhances short-term CD4⁺ T cell clonal expansion, division, and ex vivo survival under growth factor withdrawal conditions. RIBI-529 enhances humoral and cell-mediated adaptive immune responses, induces non-specific resistance against viral and bacterial pathogens, and skews responses toward a Th1 type, accompanied by Th2 responses.

Cynandione A is an acetophenone that can be isolated from Cynanchum Wilfordii Radix. Cynandione A protects hepatocytes and cortical neurons from toxicity and improves neurological deficits in a rat model of cerebral ischemia. On the other hand, cynandione A has significant anti-inflammatory effects and inhibits inflammation by activating macrophage α7 nAChR and IL-10 expression.

OM-RCA-01 is an anti-FGFR1 monoclonal antibody with a K_d of 1.59 nM for human FGFR1. OM-RCA-01 inhibits the phosphorylation of FGFR1, blocks FGF-mediated signaling pathways, and suppresses the proliferation of downstream tumor cells. OM-RCA-01 delays tumor growth in lung cancer and renal cancer xenograft models expressing FGFR1. When combined with Nivolumab, OM-RCA-01 enhances the release of IFN-γ and IL-2. OM-RCA-01 is applicable for the research of lung cancer and renal cell carcinoma.