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Bexotegrast (PLN-74809) is an orally active, potent dual αvβ6/αvβ1 integrin inhibitor with Kd of 5.7 nM and 3.4 nM, respectively. Bexotegrast inhibits αvβ6- and αvβ1-induced TGF-β activation with IC50 values of 29.8 nM and 19.2 nM, respectively. Bexotegrast has antifibrogenic effects and block multiple avenues of TGF-β activation in the fibrotic lung .
MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide pan-integrin antagonist with IC50 values of 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM and 12.2 nM for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1, respectively .
Maleimide-NOTA is a chelate. Maleimide-NOTA can be site-specifically coupled to the hPD-L1 nanobody bearing the Cys-tag. Maleimide-NOTA can specifically conjugate to A20FMDV2 (HY-P1654). The [ 68Ga]Ac-CG6 formed by the conjugation of 68Ga radiolabeled Maleimide-NOTA with A20FMDV2 can be used for PET imaging of αvβ6 integrin-positive pancreatic ductal adenocarcinoma .
EMD527040 is a potent and highly selective αvβ6 antagonist with antifibrotic activities. EMD527040 can be used for carcinoma and liver fibrosis research .
GSK 3008348 is a small molecule antagonist of integrin αvβ6 with IC50 values for αvβ6, αvβ1, αvβ3, αvβ5, and αvβ8 are 1.50, 2.83, 12.53, 4.00, and 2.26 nM, respectively. GSK 3008348 can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 prevents the binding of the foot-and-mouth disease virus (FMDV) to the αvβ6 integrin receptor on the surface of host cells, thereby inhibiting the entry of the virus. GSK 3008348 can be used for research on pulmonary fibrosis and various types of cancer .
MORF-627 is a highly selective, orally active integrin αvβ6 inhibitor. By blocking TGF-β1 activation and pSMAD2 signaling, MORF-627 significantly reduces collagen deposition, epithelial-mesenchymal transition markers, and structural changes in fibrotic cells. MORF-627 exhibits significant antifibrotic efficacy without genotoxicity in idiopathic pulmonary fibrosis models. However, MORF-627 induces bladder epithelial proliferation and early invasive urothelial carcinoma in cynomolgus monkeys and human cells, and this toxic effect can be reversed by exogenous TGF-β. MORF-627 can be used for studying the pathological mechanisms of pulmonary fibrosis and evaluating drug safety .
GSK 3008348 hydrochloride is a small molecule antagonist of integrin αvβ6 with IC50 values for αvβ6, αvβ1, αvβ3, αvβ5, and αvβ8 are 1.50, 2.83, 12.53, 4.00, and 2.26 nM, respectively. GSK 3008348 hydrochloride can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 hydrochloride prevents the binding of the foot-and-mouth disease virus (FMDV) to the αvβ6 integrin receptor on the surface of host cells, thereby inhibiting the entry of the virus. GSK 3008348 hydrochloride can be used for research on pulmonary fibrosis and various types of cancer .
STX-100 (BG00011) is a humanized monoclonal antibody targeting αVβ6 integrin. STX-100 specifically binds αVβ6 integrin, blocks latent TGF-β activation via latency-associated peptide (LAP) interaction prevention, and reduces profibrotic responses. STX-100 can be used for the research of idiopathic pulmonary fibrosis, and cancer .
Integrin-IN-2 (compound 39) is an orally bioavailable pan αv integrin inhibitor. Integrin-IN-2 can increases the αvβ6, αvβ3, αvβ5 and αvβ8 binding affinities with pIC50 values of 7.8, 8.4, 8.4 and 7.4, respectively .
DOTA-ADIBO TFA is a DOTA-derived bifunctional chelator (BFC) that allows drug conjugation via an uncatalyzed, copper-free cycloaddition reaction. DOTA-ADIBO TFA enables the construction of fusion chelator systems that can be further used to synthesize radiotracers after Cu[64] modification. Positron emission tomography imaging of tumors expressing integrin αvβ6 .
A20FMDV2 is a highly selective αvβ6 integrin inhibitor with human IC50 values of 3 nM and binds with at least 1000-fold selectivity over other RGD-binding integrins. A20FMDV2 binds to the integrin’s RGD-binding site, induces rapid integrin internalization, and delays post-internalization integrin recycling to the cell surface. A20FMDV2 can be used for the research of pancreatic cancer, breast cancer, colorectal cancer, ovarian cancer, oral squamous cell carcinoma .
c(avb6)-DOTA TFA is a conjugate of the αvβ6 integrin selective peptide ring modified with DOTA chelator. The Lu(III) complex of c(avb6)-DOTA TFA has a comparable affinity for αvβ6 integrin (IC50=0.8 nM) and can be used as a tumor diagnostic .
Nesvategrast (SF0166) is a potent and selective αvβ3 antagonist with IC50 values of 0.6 nM, 8 nM, and 13 nM for αvβ3, αvβ6, and αvβ8, respectively. Nesvategrast inhibits cellular adhesion to vitronectin across human, rat, rabbit, and dog cell lines with IC50 values of 7.6 pM to 76 nM. Nesvategrast decreases neovascularization in the oxygen-induced retinopathy mouse model .
ATTO 740 NHS ester is a near-infrared fluorescent dye and a multimodal fluorescence/photoacoustic contrast agent with excellent near-infrared emission properties and extremely high photostability. The photoacoustic signal of ATTO 740 NHS ester shows no significant decrease after continuous irradiation with a 750 nm laser for 30 min, making it suitable for in vivo fluorescence imaging and photoacoustic contrast imaging. When conjugated with the cystine knot peptide R01, ATTO 740 NHS ester enables precise detection of integrin αvβ6-positive cells and tumors in nude mouse xenograft models .
Bexotegrast hydrochloride (PLN-74809 hydrochloride) is a small molecule dual selective inhibitor with activity targeting αVβ1 and αVβ6. Bexotegrast hydrochloride is used for idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC). Bexotegrast hydrochloride inhibits the activation of TGF-β1 by blocking the function of these integrins, thereby preventing the growth of fibrous tissue in the lungs and bile ducts .
αvβ6-IN-2 (compound 20) is a potent and orally active αvβ6 integrin inhibitor with a pIC50 value of 7.8. αvβ6-IN-2 has the potential for the research of idiopathic pulmonary fibrosis .
αvβ6-IN-1 (compound 28) is a potent and orally active αvβ6 integrin inhibitor with a pIC50 value of 8.1. αvβ6-IN-1 has the potential for the research of idiopathic pulmonary fibrosis .
EMD527040 (hydrochloride) is a highly potent and selective αvβ6 antagonist with anti-fibrotic activity. EMD527040 (hydrochloride) is used in the research of liver cancer and liver fibrosis .
Arg-Gly-Asp (RGD) is a synthetic peptide corresponding to the cell adhesion sequence for the integrins αVβ1, αVβ3, αVβ5, αVβ6, αVβ8, α8β1, and α5β1. It is a component of radioligands and peptidomimetics that have been used in the study of integrin expression and activity in vivo.
SC-68448 (S 448) is a selective αvβ3 antagonist (IC50 = 1 nM). SC-68448 inhibits αvβ3-mediated endothelial cell proliferation. SC-68448 reduces the total level of αvβ6 in NHBE cells. SC-68448 inhibits angiogenesis in a rat corneal neoplasia model. SC-68448 inhibits tumor growth and completely prevents the development of hypercalcemia in a rat Ledich cell tumor model. SC-68448 can be used in research on cardiovascular and cerebrovascular diseases such as hypercalcemia and cancers such as testicular interstitial cell tumors .
Cyclic αvβ6 (Compound c(FRGDLAFp(NMe)K)) is a αvβ6-integrin-specific cyclic nonapeptide. Cyclic αvβ6 can be coupled with 68Ga-labeled monomeric triazacyclononane-triphosphinate (TRAP). Cyclic αvβ6 can be used in PET imaging studies for cancers including head and neck cancer and pancreatic cancer .
NOTA-Asp2-αvβ6L is an integrin αvβ6 binder with selective accumulation in αvβ6-positive pancreatic cancer cells and tumors. NOTA-Asp2-αvβ6L can be used as a PET/CT tracer for imaging pancreatic ductal adenocarcinoma (PDAC) .
Tri-SM6.1 is a tridentate small-molecule ligand targeting integrin αvβ6. Tri-SM6.1 binds to integrin αvβ6 on epithelial cells to deliver conjugated α-ENaC RNAi agents .
Relitegatide is a cyclic peptide with selectivity for the αvβ6 integrin. Relitegatide can be used for the synthesis of Relitegatide brexetan (HY-P11276) .
EMD527040 (Standard) is the analytical standard of EMD527040 (HY-101473). This product is intended for research and analytical applications. EMD527040 is a potent and highly selective αvβ6 antagonist with antifibrotic activities. EMD527040 can be used for carcinoma and liver fibrosis research .
FSC(PEG4-avb6)3 is a tracer targeting αvβ6 integrin trimer (IC50 = 0.69 nM). FSC(PEG4-avb6)3 can be used for the study of head-and-neck, lung, breast, and pancreatic carcinomas .
SM6.1-azide (Compound 2a) is a ligand for αvβ6 integrin with a azide group. The azide group of SM6.1-azide can undergo a click chemical reaction with small molecules, peptides or siRNA containing DBCO or Alkyne groups, enabling pulmonary-targeted delivery .
A20FMDV2-Cys is a cysteine-containing 20-mer peptide that targets integrin αvβ6 with high affinity. A20FMDV2-Cys can be used for targeted liposome modification to enhance liver and bile duct targeting. A20FMDV2-Cys is applicable for research in drug delivery .
ATTO 740 NHS ester is a near-infrared fluorescent dye and a multimodal fluorescence/photoacoustic contrast agent with excellent near-infrared emission properties and extremely high photostability. The photoacoustic signal of ATTO 740 NHS ester shows no significant decrease after continuous irradiation with a 750 nm laser for 30 min, making it suitable for in vivo fluorescence imaging and photoacoustic contrast imaging. When conjugated with the cystine knot peptide R01, ATTO 740 NHS ester enables precise detection of integrin αvβ6-positive cells and tumors in nude mouse xenograft models .
DOTA-ADIBO TFA is a DOTA-derived bifunctional chelator (BFC) that allows drug conjugation via an uncatalyzed, copper-free cycloaddition reaction. DOTA-ADIBO TFA enables the construction of fusion chelator systems that can be further used to synthesize radiotracers after Cu[64] modification. Positron emission tomography imaging of tumors expressing integrin αvβ6 .
A20FMDV2 is a highly selective αvβ6 integrin inhibitor with human IC50 values of 3 nM and binds with at least 1000-fold selectivity over other RGD-binding integrins. A20FMDV2 binds to the integrin’s RGD-binding site, induces rapid integrin internalization, and delays post-internalization integrin recycling to the cell surface. A20FMDV2 can be used for the research of pancreatic cancer, breast cancer, colorectal cancer, ovarian cancer, oral squamous cell carcinoma .
c(avb6)-DOTA TFA is a conjugate of the αvβ6 integrin selective peptide ring modified with DOTA chelator. The Lu(III) complex of c(avb6)-DOTA TFA has a comparable affinity for αvβ6 integrin (IC50=0.8 nM) and can be used as a tumor diagnostic .
Cyclic αvβ6 (Compound c(FRGDLAFp(NMe)K)) is a αvβ6-integrin-specific cyclic nonapeptide. Cyclic αvβ6 can be coupled with 68Ga-labeled monomeric triazacyclononane-triphosphinate (TRAP). Cyclic αvβ6 can be used in PET imaging studies for cancers including head and neck cancer and pancreatic cancer .
NOTA-Asp2-αvβ6L is an integrin αvβ6 binder with selective accumulation in αvβ6-positive pancreatic cancer cells and tumors. NOTA-Asp2-αvβ6L can be used as a PET/CT tracer for imaging pancreatic ductal adenocarcinoma (PDAC) .
Relitegatide is a cyclic peptide with selectivity for the αvβ6 integrin. Relitegatide can be used for the synthesis of Relitegatide brexetan (HY-P11276) .
FSC(PEG4-avb6)3 is a tracer targeting αvβ6 integrin trimer (IC50 = 0.69 nM). FSC(PEG4-avb6)3 can be used for the study of head-and-neck, lung, breast, and pancreatic carcinomas .
A20FMDV2-Cys is a cysteine-containing 20-mer peptide that targets integrin αvβ6 with high affinity. A20FMDV2-Cys can be used for targeted liposome modification to enhance liver and bile duct targeting. A20FMDV2-Cys is applicable for research in drug delivery .
STX-100 (BG00011) is a humanized monoclonal antibody targeting αVβ6 integrin. STX-100 specifically binds αVβ6 integrin, blocks latent TGF-β activation via latency-associated peptide (LAP) interaction prevention, and reduces profibrotic responses. STX-100 can be used for the research of idiopathic pulmonary fibrosis, and cancer .
Integrin α V beta 5 proteins, specifically the α-V (ITGAV) subunit, are multifunctional receptors for ligands such as vitronectin and fibronectin and recognize RGD sequences. ITGAV: ITGB3 binds fractalkine and acts as a coreceptor in CX3CR1-dependent signaling. Integrin alpha V beta 6 Protein, Human (Biotinylated, HEK293, His-Avi) is a recombinant protein dimer complex containing human-derived Integrin alpha V beta 6 protein, expressed by HEK293 , with C-Avi, C-His labeled tag. Integrin alpha V beta 6 Protein, Human (Biotinylated, HEK293, His-Avi), has molecular weight of 90-150 kDa.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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