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Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC50 of 250 nM . Tie2 kinase inhibitor 1 has anti-cancer activity [2].
TIE-2/VEGFR-2kinase-IN-2 is a potent dual VEGFR2 and Tie-2 inhibitor with pIC50 values of 8.61 and 8.56, respectively . TIE-2/VEGFR-2kinase-IN-2 is an anti-angiogenic agent and can be used for cancer research [2].
TIE-2/VEGFR-2 kinase-IN-1 is used for the synthesis of TIE-2 and/or VEGFR-2 inhibitors, extracted from patent WO2003022852, example 14. TIE-2/VEGFR-2 kinase-IN-1 is used for the study of diseases associated with inappropriate angiogenesis .
AMG-Tie2-1 is an inhibitor of tunica interna endothelial cell kinase 2(Tie2) with an IC50 of 1 nM. AMG-Tie2-1 is a VEGFR2 inhibitor with an IC50 of 3 nM .
Tie2 kinase inhibitor 2 (compound 7) is a selective Tie2 kinase inhibitor with an IC50 value of 1 μM. Tie2 kinase inhibitor 2 inhibits endothelial cell tube formation, and can be used for Tie2-mediated angiogenic disorders research .
Tie2 kinase inhibitor 3 (compound 63) is a potent Tie-2 kinase inhibitor with good oral activity (IC50=30 nM). Tie2 kinase inhibitor 3 inhibits phosphorylation and signaling of Tie-2 by competing with the ATP binding site of Tie-2 kinase. This inhibition affects the stability and maturity of blood vessels, which has an impact on tumor angiogenesis. Tie2 kinase inhibitor 3 can be used to restrict tumor growth and regulate angiogenesis .
TIE-2/VEGFR-2 kinase-IN-3, benzimidazole, is a potent TIE-2 and VEGFR-2 tyrosine kinase receptors inhibitors with IC50 values of 6.9 nM and 3.5 nM, respectively. TIE-2/VEGFR-2 kinase-IN-3 can be used for the research of angiogenesis .
TIE-2/VEGFR-2 kinase-IN-4, benzimidazole, is a potent TIE-2 and VEGFR-2 tyrosine kinase receptors inhibitors with IC50 values of 5.2 nM and 5.1 nM, respectively. TIE-2/VEGFR-2 kinase-IN-4 can be used for the research of angiogenesis .
TIE-2/VEGFR-2 kinase-IN-5 is an anti-angiogenic agent. TIE-2/VEGFR-2 kinase-IN-5 also is a potent TIE-2 and VEGFR-2 tyrosine kinase inhibitor with pIC50 values of 7.78 nM and 8.11 nM, respectively. TIE-2/VEGFR-2 kinase-IN-5 can be used for the research of angiogenesis .
Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.
Nesvacumab is a fully human immunoglobulin G1 (IgG1) monoclonal antibody that specifically binds and inactivates the Tie2 receptor ligand Angiopoietin-2(Ang2) with high affinity, but shows no binding to Ang1 .
CEP-11981 (tosylate) (ESK981 (tosylate), BOL 303213X (tosylate)) is an orally active tyrosine kinase inhibitor (TKI), which can target TIE2, VEGFR1-3 and FGFR1, and has potential anti-tumor and anti-angiogenic effects .
5α-Hydroxycostic acid, a eudesmane-type sesquiterpene, is isolated from the herb Laggera alata. 5α-Hydroxycostic acid inhibits angiogenesis and suppresses breast cancer cell migration through regulating VEGF/VEGFR2 and Ang2/Tie2 pathways .
CEP-11981(ESK981; BOL 303213X) is an orally active tyrosine kinase inhibitor (TKI), which can target TIE2, VEGFR1-3 and FGFR1, and has potential anti-tumor and anti-angiogenic effects .
Vasculotide, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock [2] .
SB-633825 is a potent and ATP-competitive inhibitor of TIE2, LOK (STK10) and BRK with IC50s of 3.5 nM, 66 nM, 150 nM, respectively. SB-633825 can inhibit cancer cell growth and angiogenesis .
Vasculotide TFA, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide TFA ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide TFA promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide TFA protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide TFA decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock [2] .
Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM) .
GW768505A free base is a potent dual inhibitor of VEGFR2 (KDR) and Tie-2, with a pIC50 of 7.81 for VEGFR2. GW768505A free base has anti-angiogenic activity .
PP2 Analog (compound 3) is a ATP-competitive Src family kinases inhibitor with the IC50 values of 0.22, 0.15, 2.68, and 7 aganist of lck (64-509), src , kdr, and tie-2 .
Trebananib (2xCon4C; AMG 386) is an Fc fusion peptibody that prevents Tie2 receptor activation through binding of both angiopoietin 1 (Ang1) and Ang2. Trebananib has anti-angiogenesis activity [2].
Rebastinib (DCC-2036) is an orally active, non-ATP-competitive Bcr-Abl inhibitor for Abl1 WT and Abl1 T315I with IC50s of 0.8 nM and 4 nM, respectively. Rebastinib also inhibits SRC, KDR, FLT3, and Tie-2, and has low activity to seen towards c-Kit.
CEP-14083 is a ATP-competitive ALK kinase inhibitor with an IC50 value in enzymatic assays of 2 nM. CEP-14083 also inhibits other kinases, such as insulin receptor (IR), vascular endothelial growth factor receptor 2(VEGFR2), angiopoietin-1 receptor (TIE2) and dual leucine zipper kinase (DLK). CEP-14083 suppresses CD274 mRNA expression and the NPM/ALK function in the NPM/ALK-carrying T cell lymphoma (ALK+TCL) cells. CEP-14083 is promising for research of lymphoma [2].
Altiratinib (DCC-2701) is a multi-targeted kinase inhibitor with IC50s of 2.7, 8, 9.2, 9.3, 0.85, 4.6, 0.83 nM for MET, TIE2, VEGFR2, FLT3, Trk1, Trk2, and Trk3 respectively.
RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR/VEGF2R and Tie-2 with IC50 values of 0.24, 1.19, 10.74 and 5.85 µM, respectively. RK-20448 also inhibits BLK, Csk, Fyn and Lyn with IC50 values of 0.37, 4.27, 2.03 and 0.43 µM, respectively. RK-20448 is the cis isomer of A-419259 (HY-15764) [2].
Gersizangitide (AXT107) is an anti-angiogenic peptide consisting of 20 amino acids, derived from collagen IV. Gersizangitide is an inhibitor of VEGF-A and VEGF-C and an activator of Tie2. Gersizangitide can block VEGF receptor signaling, inhibit vascular leakage, neovascularization and inflammation. Gersizangitide can be used in the research of diseases related to ocular neovascularization and angiogenesis [2].
SYN1143 is a potent, selective and orally active dual inhibitor of c-Met/RON, with IC50s of 4 and 9 nM, respectively. SYN1143 has weak inhibitory activity on Lck, Tie2, Src, and BTK with IC50s ranging from 160 to 710 nM. SYN1143 can be used for the research of cancers that RON and c-Met are activated .
Srctide is a biological active peptide. (This is a peptide substrate for many protein kinases, such as Blk, BTK, cKit, EPHA1, EPHB2, EPHB3, ERBB4, FAK, Flt3, IGF-1R, ITK, Lck, MET, MUSK, Ret, Src, TIE2, TrkB, VEGF-R1 (Flt-1) and VEGF-R2 (KDR).)
Corylifol C is a potent protein kinase inhibitor with IC50 valueS of 8.7, 3.0, 2.1, 6.4, 4.5, 6.2, 2.3, 1.2, 5.1 μg/ml for ARK5, Aurora-A, Aurora-B, AXL, B-RAF-VE, CDK4/CycD1, TIE2, EGF-R, EPHB4, respectively .
Cabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib hydrochloride shows antiangiogenic activity. Cabozantinib hydrochloride disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis .
Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis[2].
Cabozantinib (Standard) is the analytical standard of Cabozantinib. This product is intended for research and analytical applications. Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis[2].
SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC50 values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer .
S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies [2] . S116836 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Vasculotide TFA, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide TFA ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide TFA promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide TFA protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide TFA decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock [2] .
Gersizangitide (AXT107) is an anti-angiogenic peptide consisting of 20 amino acids, derived from collagen IV. Gersizangitide is an inhibitor of VEGF-A and VEGF-C and an activator of Tie2. Gersizangitide can block VEGF receptor signaling, inhibit vascular leakage, neovascularization and inflammation. Gersizangitide can be used in the research of diseases related to ocular neovascularization and angiogenesis [2].
Srctide is a biological active peptide. (This is a peptide substrate for many protein kinases, such as Blk, BTK, cKit, EPHA1, EPHB2, EPHB3, ERBB4, FAK, Flt3, IGF-1R, ITK, Lck, MET, MUSK, Ret, Src, TIE2, TrkB, VEGF-R1 (Flt-1) and VEGF-R2 (KDR).)
Vasculotide, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock [2] .
FAM-CSKtide is a biological active peptide. (This is a FAM labeled peptide substrate (Abs/Em = 494/521 nm) for C-terminal Src kinase (Csk) and many other kinases such as Axl, cKit, ERBB4, Fes, Flt3, IGF-1 R, MET, MUSK, PYK2, Ret, TIE2, TrkA, VEGF-R1 and VEGF-R2.)
Nesvacumab is a fully human immunoglobulin G1 (IgG1) monoclonal antibody that specifically binds and inactivates the Tie2 receptor ligand Angiopoietin-2(Ang2) with high affinity, but shows no binding to Ang1 .
Trebananib (2xCon4C; AMG 386) is an Fc fusion peptibody that prevents Tie2 receptor activation through binding of both angiopoietin 1 (Ang1) and Ang2. Trebananib has anti-angiogenesis activity [2].
5α-Hydroxycostic acid, a eudesmane-type sesquiterpene, is isolated from the herb Laggera alata. 5α-Hydroxycostic acid inhibits angiogenesis and suppresses breast cancer cell migration through regulating VEGF/VEGFR2 and Ang2/Tie2 pathways .
Corylifol C is a potent protein kinase inhibitor with IC50 valueS of 8.7, 3.0, 2.1, 6.4, 4.5, 6.2, 2.3, 1.2, 5.1 μg/ml for ARK5, Aurora-A, Aurora-B, AXL, B-RAF-VE, CDK4/CycD1, TIE2, EGF-R, EPHB4, respectively .
TIE-2 is a tyrosine protein kinase that serves as a cell surface receptor for ANGPT1, ANGPT2, and ANGPT4 and is critical for angiogenesis, endothelial cell processes, and vascular stability. In addition to embryonic vasculogenesis, TIE-2 also affects postnatal hematopoiesis, regulating angiogenesis depending on the situation. TIE-2 Protein, Human (HEK293, His) is the recombinant human-derived TIE-2 protein, expressed by HEK293 , with C-6*His labeled tag.
TIE-2 protein has growth factor binding activity and is involved in ossification, cAMP response, and estrogen response. It is predicted to be present in a variety of cellular components, as a component of the plasma membrane, and as part of receptor complexes. TIE-2 Protein, Rat (HEK293, Fc) is the recombinant rat-derived TIE-2 protein, expressed by HEK293 , with C-hFc labeled tag.
TIE-2 Protein, Mouse (HEK293, His) belongs to the receptor tyrosine kinase family and functions as a receptor for Angiopoietin-1 (Ang1). Ang1 bridges TIE-2 at cell-cell contacts, resulting in trans-association of TIE-2 in the presence of cell-cell contacts. TIE-2 activation promotes vessel assembly and maturation by mediating survival signals for EC and regulating the recruitment of pericytes. TIE-2 maintains the vascular integrity of mature vessels by enhancing endothelial barrier function and inhibiting apoptosis of endothelial cells. TIE-2 Protein, Mouse (HEK293, His) is the recombinant mouse-derived TIE-2 protein, expressed by HEK293 , with C-His labeled tag.
TIE-2 is a tyrosine protein kinase that serves as a cell surface receptor for ANGPT1, ANGPT2, and ANGPT4 and is critical for angiogenesis, endothelial cell processes, and vascular stability. In addition to embryonic vasculogenesis, TIE-2 also affects postnatal hematopoiesis, regulating angiogenesis depending on the situation. TIE-2 Protein, Cynomolgus (HEK293, His) is the recombinant cynomolgus-derived TIE-2 protein, expressed by HEK293 , with C-His labeled tag.
TIE-2 is a tyrosine protein kinase that serves as a cell surface receptor for ANGPT1, ANGPT2, and ANGPT4 and is critical for angiogenesis, endothelial cell processes, and vascular stability. In addition to embryonic vasculogenesis, TIE-2 also affects postnatal hematopoiesis, regulating angiogenesis depending on the situation. TIE-2 Protein, Mouse (HEK293, Fc) is the recombinant mouse-derived TIE-2 protein, expressed by HEK293 , with C-hFc labeled tag.
TIE2 Protein is a cell surface receptor for ANGPT1, ANGPT2, and ANGPT4, belonging to the protein tyrosine kinase Tie2 family. TIE2 Protein is an angiogenic factor that regulates angiogenesis, endothelial cell survival, proliferation, migration, adhesion, cell spreading, and actin cytoskeleton reorganization, and has anti-inflammatory effects. TIE2 Protein consists of 1124 amino acids (M1-A1124), with two immunoglobulin-like domains, three N-terminal fibronectin type III domains (447-541 a.a, 545-636 a.a, 641-735 a.a), and three epidermal growth factor (EGF)-like domains (210-252 a.a, 254-299 a.a, 301-341 a.a). TIE-2 Protein, Human (HEK293, His-Fc) is the recombinant human-derived TIE-2 protein, expressed by HEK293 , with C-hFc, C-His labeled tag.
TIE-2 is a tyrosine protein kinase that serves as a cell surface receptor for ANGPT1, ANGPT2, and ANGPT4 and exerts a global control over angiogenesis and vascular stability. It regulates endothelial cell survival, proliferation, migration, adhesion, and actin cytoskeletal reorganization. TIE-2 Protein, Human (sf9, His-GST) is the recombinant human-derived TIE-2 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.
TIE-2 is a tyrosine protein kinase that serves as a cell surface receptor for ANGPT1, ANGPT2, and ANGPT4 and is critical for angiogenesis, endothelial cell processes, and vascular stability.In addition to embryonic vasculogenesis, TIE-2 also affects postnatal hematopoiesis, regulating angiogenesis depending on the situation.TIE-2 Protein, Mouse (sf9, His-GST) is the recombinant mouse-derived TIE-2 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.
TIE-2 is a tyrosine protein kinase that serves as a cell surface receptor for ANGPT1, ANGPT2, and ANGPT4 and exerts a global control over angiogenesis and vascular stability. It regulates endothelial cell survival, proliferation, migration, adhesion, and actin cytoskeletal reorganization. TIE-2 Protein, Human (Biotinylated, HEK293, His) is the recombinant human-derived TIE-2 protein, expressed by HEK293 , with C-His labeled tag.
TIE-2 is a tyrosine protein kinase that serves as a cell surface receptor for ANGPT1, ANGPT2, and ANGPT4 and exerts a global control over angiogenesis and vascular stability. It regulates endothelial cell survival, proliferation, migration, adhesion, and actin cytoskeletal reorganization. TIE-2 Protein, Human (Biotinylated, sf9, Avi) is the recombinant human-derived TIE-2, expressed by Sf9 insect cells , with Avi labeled tag.
TIE-2 belongs to the RTPK family of proteins and is a type I transmembrane protein. TIE-2 can serve as a receptor for growth factors, differentiation factors, and metabolic response stimulators. TIE-2 Protein, Cynomolgus (HEK293, Fc) is the recombinant cynomolgus-derived TIE-2 protein, expressed by HEK293 , with C-hFc labeled tag.
TIE-2 Protein, a tyrosine-protein kinase, acts as a cell-surface receptor for ANGPT1, ANGPT2, and ANGPT4, exerting comprehensive control over angiogenesis, endothelial cell behavior, and vascular stability. It regulates diverse processes, including endothelial cell survival, proliferation, migration, adhesion, and actin cytoskeleton reorganization, while also playing a crucial role in maintaining vascular quiescence and preventing the leakage of pro-inflammatory plasma proteins and leukocytes from blood vessels. TIE-2 Protein, Rhesus Macaque (HEK293, His) is the recombinant Rhesus Macaque-derived TIE-2 protein, expressed by HEK293 , with C-His labeled tag.
ANGPT2/Angiopoietin-2 (dog) complexly regulates angiogenesis by binding to TEK/TIE2, competitively affecting ANGPT1 signaling. It independently induces TEK/TIE2 phosphorylation and, in the absence of VEGF, may cause endothelial cell apoptosis, thereby promoting vascular regression. ANGPT2/Angiopoietin-2, Dog (HEK293, His) is the recombinant dog-derived ANGPT2/Angiopoietin-2, Dog, expressed by HEK293 , with C-6*His labeled tag.
Angiopoietin-2 (ANGPT2) protein competes with ANGPT1 for TEK/TIE2 binding, modulates ANGPT1 signaling and induces TEK/TIE2 phosphorylation even in the absence of ANGPT1. In the absence of angiogenic stimulation, ANGPT2 disrupts cell-matrix contacts, potentially triggering endothelial cell apoptosis and vessel regression. Angiopoietin-2 Protein, Human (HEK293, His-Avi) is the recombinant human-derived Angiopoietin-2 protein, expressed by HEK293 , with N-His, N-Avi labeled tag.
Angiopoietin-2 (ANGPT2) protein competes with ANGPT1 for TEK/TIE2 binding, modulates ANGPT1 signaling and induces TEK/TIE2 phosphorylation even in the absence of ANGPT1. In the absence of angiogenic stimulation, ANGPT2 disrupts cell-matrix contacts, potentially triggering endothelial cell apoptosis and vessel regression. Angiopoietin-2 Protein, Human (Biotinylated, HEK293, His-Avi) is the recombinant human-derived Angiopoietin-2 protein, expressed by HEK293 , with N-His, N-Avi labeled tag.
ANGPT2 is a secreted factor on the angiopoietin/Tie (tyrosine kinase with Ig and EGF homology domains) signaling pathway and is involved in tumor angiogenesis. In the presence of ANGPT1, ANGPT2 antagonizes ANGPT1-mediated Tie2 phosphorylation, leading to vessel sprouting or degeneration depending on the level of VEGF-A. Overexpression or inhibition of ANGPT2 increases or decreases angiogenic capacity, respectively. Angiopoietin-2 Protein, Rhesus macaque (HEK293, Fc) is the recombinant Rhesus Macaque-derived Angiopoietin-2 protein, expressed by HEK293 , with C-hFc labeled tag.
Angiopoietin 2 protein (ANGPT2) binds to TEK/TIE2, competes with ANGPT1, and modulates its signaling. Even in the absence of ANGPT1, ANGPT2 induces TEK/TIE2 phosphorylation. Angiopoietin-2 Protein, Mouse (HEK293, Fc) is the recombinant mouse-derived Angiopoietin-2 protein, expressed by HEK293 , with C-hFc labeled tag.
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