Integrin Inhibitor

PF-06940434 (ADWA-11) is a monoclonal antibody targeting integrin αvβ8. PF-06940434 inhibits αvβ8-mediated TGF-β activation. PF-06940434 increases the accumulation of tumor-infiltrating CD8⁺ T cells and upregulates the expression of granzyme B and TNF-γ. PF-06940434 blocks the inhibitory effect of CD4⁺CD25⁺ T cells on the cytotoxic activity of tumor CD8⁺ T cells. PF-06940434 enhances the anti-tumor efficacy of combination therapies with other immunomodulators or radiotherapy and induces long-term anti-tumor immunity. PF-06940434 can be used in the research of squamous cell carcinoma, breast cancer, colon cancer, and prostate adenocarcinoma.

Fuzapladib calcium, an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib calcium is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib calcium exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site.

MorHap is a heroin hapten. MorHap conjugated to tetanus toxoid (TT), palm-CV2, and to monophosphoryl lipid A (MPLA)-containing liposomes partially blocks heroin-induced analgesia and hyperlocomotion in mice. MorHap designed conjugates also significantly inhibits HIV-1 binding to α4β7 receptors. MorHap can be used in research to develop vaccines related to heroin addiction and HIV-1 infection.

Irigenin (Standard) is the analytical standard of Irigenin. This product is intended for research and analytical applications. Irigenin is a is a lead compound, and mediates its anti-metastatic effect by specifically and selectively blocking α9β1 and α4β1 integrins binding sites on C-C loop of Extra Domain A (EDA). Irigenin shows anti-cancer properties. It sensitizes TRAIL-induced apoptosis via enhancing pro-apoptotic molecules in gastric cancer cells.

ATL 1102 sodium scrambled negative control is the sequence scrambled negative control of ATL 1102 sodium.

Isoxanthohumol (Standard) is the analytical standard of Isoxanthohumol (HY-N2584A). This product is intended for research and analytical applications. Isoxanthohumol is an orally active flavonoid compound. Isoxanthohumol has biological activities such as anti-tumor, anti-inflammatory, antioxidant, antiviral, antifungal, and inhibition of adipogenesis. Isoxanthohumol can induce apoptosis, autophagy, and migration of tumor cells. Isoxanthohumol is active against viruses such as HSV, BVDV, CMV, and Rhino. Isoxanthohumol can be used for the research of tumors, metabolic, and inflammatory diseases.

IPS-05002 is an α5β1 antagonist. IPS-05002 can inhibit VEGF-stimulated human umbilical vein endothelial cell (HUVEC) proliferation, adhesion, and migration, and also suppresses tubular network formation. IPS-05002 can upregulate IKB-β, XRCC4, and downregulate Cdc6 in VEGF-induced HUVECs. IPS-05002 can be used for the study of tumor angiogenesis.

Cyclo(RGDyK) (Standard) is the analytical standard of Cyclo(RGDyK) (HY-100563A). This product is intended for research and analytical applications. Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.

RWJ 50271 (Standard) is the analytical standard of RWJ 50271 (HY-110086). This product is intended for research and analytical applications. RWJ 50271 is an selective and orally active inhibitor of lymphocyte function-associated antigen-1/intercellular adhesion molecule-1(LFA-1/ICAM-1) interaction with an IC₅₀ of 5.0 μM (HL60 cells). RWJ 50271 inhibits LFA-1/ICAM-1-mediated cell adhesion.

BIRT 377 (Standard) is the analytical standard of BIRT 377 (HY-110117). This product is intended for research and analytical applications. BIRT 377 is a potent amd orally bioavailable inhibitor of the interaction between intercellular adhesion molecule-1 (ICAM-1) and lymphocyte function-associated antigen-1 (LFA-1). BIRT 377 also inhibits the production of IL-2 in vivo. BIRT 377 can be used for researching inflammatory and immune disorders.

IMB-10 is an α_Mβ₂ integrin ligand. IMB-10 inhibits α_Mβ₂-dependent migration and inflammation-induced neutrophil emigration.

Cardenolide B-1 is a Steroids product that can be isolated from the herbs of Nerium oleander.

Arg-Gly-Asp-Ser (Standard) is the analytical standard of Arg-Gly-Asp-Ser. This product is intended for research and analytical applications. Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1.

BIO5192 (Standard) is the analytical standard of BIO5192 (HY-107589). This product is intended for research and analytical applications. BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (K_d<10 pM). BIO5192 selectively binds to α4β1 (IC₅₀=1.8 nM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.

Deethyl-emvistegrast TFA is a quinoline derivative and also a α4β7 integrin inhibitor. Deethyl-emvistegrast TFA is the hydrolytic product of Emvistegrast (HY-177080). Deethyl-emvistegrast TFA modulates inflammatory pathways. Deethyl-emvistegrast TFA can be used in research related to inflammatory bowel disease (Crohn's disease and ulcerative colitis).

TC-I 15 (Standard) is the analytical standard of TC-I 15 (HY-107588). This product is intended for research and analytical applications. TC-I 15 (TC-I-15) is a type of allosteric collagen-binding integrin α2β1 inhibitor, and it also inhibits α1β1 and α11β1. TC-I 15 inhibits platelet adhesion to collagen and thrombus deposition. TC-I 15 prevents the formation of a pre-metastatic microenvironment by inhibiting the uptake of cancer-associated fibroblast (CAF) extracellular vesicles (EVs) by lung fibroblasts, which reduces the metastasis of salivary gland adenocystic carcinoma (SACC) to the lungs in mouse models, .

Phellopterin (Standard) is the analytical standard of Phellopterin. Phellopterin, an orally active furocoumarin with multiple biological activities. Phellopterin is a partial agonist of the central benzodiazepine receptors. Phellopterin exerts anti-inflammatory effects by upregulating SIRT1, downregulating ICAM-1 (reducing chronic inflammation, aiding diabetic ulcer healing), inhibiting STAT3 phosphorylation (easing atopic dermatitis inflammation), regulating Akt/PKC pathways (lowering TNF-α-induced VCAM-1 to block monocyte adhesion), and inhibiting TLR4/NF-κB pathway and macrophage M2 polarization (alleviating colitis-related cancers). Phellopterin suppresses ovarian cancer progression via inhibiting the PU.1/CLEC5A/PI3K-AKT loop (inducing cell cycle arrest, apoptosis, DNA damage). Phellopterin alleviates murine diabetes by promoting adipocyte differentiation and increasing PPARγ. Phellopterin also has anti-HSV-1 activity. Phellopterin can be used for studying anti-inflammation, anti-cancer (e.g., ovarian cancer, colitis cancer), blood glucose lowering, anti-diabetes, and anti-virus.

HMR 1031 is a very late antigen-4 (VLA4, i.e., integrin α4β1) inhibitor, with IC₅₀ values of 0.7 nM and 0.3 nM against VLA-4/VCAM-1 and VLA-4/fibronectin, respectively. HMR 1031 blocks allergen-induced airway responses and airway inflammation in mouse and sheep models. HMR 1031 can be used in asthma-related research.

NPC-18915 free base is a neutrophil activation inhibitor. NPC-18915 free base inhibits CD11b/CD18-mediated neutrophil adhesion. NPC-18915 free base induces shedding of L-selectin on the neutrophil surface, thereby reducing endothelial cell adhesion. NPC-18915 free base inhibits calcium ionophore-induced LTB₄ synthesis in neutrophils. NPC-18915 free base reduces the severity of TNBS-induced acute and recurrent colitis in rat experiments. NPC-18915 free base can be used in studies related to colitis.

CLT-28643 is an integrin α5β1 inhibitor. CLT-28643 can inhibit the high expression of integrin α5β1 in the bleb at early time-points after surgery and promote wound healing process.