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Heparanase cleaves the linkage between a glucuronic acid unit and an N-sulfo glucosamine unit carrying either a 3-O-sulfo or a 6-O-sulfo group. Heparanase-1 cuts macromolecular heparin into fragments of 5000-20000 Da. The enzyme cleaves the heparan sulfate glycosaminoglycans from proteoglycan core proteins and degrades them to small oligosaccharides. Inside cells, the enzyme is important for the normal catabolism of heparan sulfate proteoglycans, generating glycosaminoglycan fragments that are then transported to lysosomes and completely degraded. When secreted, heparanase degrades basement membrane heparan sulfate glycosaminoglycans at sites of injury or inflammation, allowing extravasion of immune cells into nonvascular spaces and releasing factors that regulate cell proliferation and angiogenesis. Group: Enzymes. Synonyms: Hpa1 heparanase; Hpa1; heparanase 1; heparanase-1; C1A heparanase; HPSE. Enzyme Commission Number: EC 3.2.1.166. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-3848; heparanase; EC 3.2.1.166; Hpa1 heparanase; Hpa1; heparanase 1; heparanase-1; C1A heparanase; HPSE. Cat No: EXWM-3848.
Heparanase 1 from Human, Recombinant
Heparanase is an endo β-D-glucuronidase, which degrades heparan sulfate side chains of heparan sulfate proteoglycans (HSPGs) in the extracellular matrix. Heparanase plays an important role in ECM degradation, facilitating the migration and extravasation of tumor cells and inflammatory leukocytes. Upon degradation, heparanase releases growth factors and cytokines that stimulate cell proliferation and chemotaxis. Heparanase is a heterodimer comprised of a 50 kDa subunit harboring the active site and a 8 kDa subunit. It is produced as a latent 65 kDa precursor and proteolytically processed to its active form. Heparanase is highly expressed in myeloid leukocytes (i.e. neutrophils) in platelets and in human placenta. Human heparanase was found to be upregulated in various types of primary tumors, correlating in some cases with increased tumor invasiveness and vascularity and with poor prospective survival. Recombinant heparanase protein hpa1 is produced in cho cells. the protein is purified by several orthogonal chromatography steps. Applications: Positive control for western blot analysis. Group: Enzymes. Synonyms: Heparanase; Hpa1 heparan. HPA1. Storage: Store at -20°C, avoid repeated freeze-thaw cycles. Source: CHO. Species: Human. Heparanase; Hpa1 heparanase; Hpa1; heparanase 1; heparanase-1; C1A heparanase; HPSE; HPA1. Cat No: NATE-0843.
A-72363 A1
A-72363 A1 is a Heparanase inhibitor produced by Streptomyces nobilis SANK 60192. Synonyms: A-72363 A-1; 4alpha,5beta-Dihydroxy-6beta-(acetylamino)piperidine-3alpha-carboxylic acid. Molecular formula: C8H14N2O5. Mole weight: 218.21.
A-72363 A2
A-72363 A2 is a Heparanase inhibitor produced by Streptomyces nobilis SANK 60192. Synonyms: A-72363 A-2; 4beta,5beta-Dihydroxy-6beta-(acetylamino)piperidine-3alpha-carboxylic acid. Molecular formula: C8H14N2O5. Mole weight: 218.21.
A-72363 C
A-72363 C is a Heparanase inhibitor produced by Streptomyces nobilis SANK 60192. Synonyms: A-72363; 4alpha,5alpha-Dihydroxy-6alpha-(acetylamino)piperidine-3alpha-carboxylic acid. Molecular formula: C8H14N2O5. Mole weight: 218.21.
Acetobromo-alpha-D-glucuronic Acid Methyl Ester
Acetobromo-alpha-D-glucuronic Acid Methyl Ester (CAS# 21085-72-3) is a useful compound for preparing a fluorogenic probe for human heparanase. Uses: It is a useful compound for preparing a fluorogenic probe for human heparanase. Synonyms: Methyl(tri-O-acetyl-α-D-glucopyranosyl bromide)uronate; (2S,3S,4S,5R,6R)-3,4,5-triacetyloxy-6-bromo-2-oxanecarboxylic acid methyl ester; 1-Bromo-1-deoxy-2,3,4-triacetate α-D-Glucopyranuronic Acid Methyl Ester; Methyl 2,3,4-Tri-O-acetyl-1-bromo-1-deoxy-α-D-glucopyranuranate; Methyl α-Acetobromoglucuronate. Grades: ≥95%. CAS No. 21085-72-3. Molecular formula: C13H17BrO9. Mole weight: 397.17.
Antibiotic RK-682 (Antibiotic TAN 1364B, Antibiotic CI 010)
Antibiotic RK-682 is the calcium salt of one of a complex family of tetronic acids isolated from Streptomyces species. The formation of the salt is almost certainly an artefact of silica chromatography. RK-682 is the most extensively studied of the analogues, having been shown to inhibit protein tyrosine phosphatases and heparanase. Pharmacological studies with RK-682 demonstrated enhanced ATP-induced long-term potentiation using guinea-pig hippocampal slices. Investigation of the complex has also shown potent activity against HIV-1 protease. Group: Biochemicals. Alternative Names: Antibiotic TAN 1364B, Antibiotic CI 010. Grades: Highly Purified. CAS No. 154639-24-4(TAN1364B). Pack Sizes: 500ug. US Biological Life Sciences.
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DMBO (CCDC-272761)
An oxazine that appears to mimic the pyranosidic moiety of heparin sulfate, and is shown to interact directly with several growth factors and cytokines including VEGF, TNF-a and heparin-binding-EGF in a surface plasmon resonance assay. At concentrations of 10-80uM, this compound dose-dependently inhibits the proliferation of VEGF-expressing LM8G7 cells (IC50=13uM), and TNF-a-expressing OVSAHO cells (IC50=19uM). At 195uM, a 99% reduction in cell growth is observed in HB-EGF-expressing SKOV-3 cultures. This compound inhibits heparanase-mediated degradation of heparin sulfate in LM8G7 cells (IC50=65uM and 104-206uM, in an enzymatic and a cell based assay, respectively). At 0.5-5uM, it markedly prevents the migration and invasion of the same culture, in a dose-dependent manner. In addition, it completely suppresses liver metastatic nodules of osteosarcoma mice injected with LM8G7 cells at 0.5mg/kg without any signs of toxicity in vivo, and demonstrates a synergistic anti-tumor effect when Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
Worldwide
OGT 2115
OGT 2115 is a heparanase inhibitor with IC50 value of 0.4 μM. It shows antiangiogenic properties in vitro. Synonyms: OGT -115; OGT2115; OGT2115. 2-[4-[[3-(4-Bromophenyl)-1-oxo-2-propenyl]amino]-3-fluorophenyl]-5-benzoxazoleacetic acid. Grades: ≥98% by HPLC. CAS No. 853929-59-6. Molecular formula: C24H16BrFN2O4. Mole weight: 495.3.
PG545
PG545 is an angiogenesis and heparanase inhibitor, which inhibited the proliferation, migration, and colony formation of pancreatic cancer cells in vitro at pharmacologically relevant concentrations. PG545 significantly prolonged animal survival in intraperitoneal and genetic models (mPDAC: LSL-Kras(G12D); Cdkn2a(lox/lox); p48(Cre)) of PDAC. PG545 also inhibited primary tumor growth and metastasis in orthotopic and genetic endpoint studies. PG545 significantly decreased cell proliferation, increased apoptosis, reduced microvessel density, disrupted vascular function, and elevated intratumoral hypoxia. Synonyms: PG 545; PG-545. CAS No. 1144492-69-2. Molecular formula: C51H75Na13O60S13. Mole weight: 2363.75.
RK-682
RK-682 is the inhibitor for protein tyrosine phosphatase ( PTPase ), heparanase , phospholipase A2 and HIV-1 protease. RK-682 inhibits the dephosphorylation of CD45 ( IC 50 is 54 μM) and VHR ( IC 50 is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC 50 s of 78.2, 43.2 and 145 nM, respectively, arrests the cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24 [1] [2] [3]. Uses: Scientific research. Group: Signaling pathways. CAS No. 150627-37-5. Pack Sizes: 200 μg. Product ID: HY-135564A.
Siastatin B
A-72363 B is a Heparanase inhibitor produced by Streptomyces nobilis SANK 60192. Synonyms: A-72363 B; 3-Piperidinecarboxylic acid, 6-(acetylamino)-4,5-dihydroxy-, (3S-(3-alpha,4-alpha,5-alpha,6-beta))-; Siastatin B microbial; (2s,3r,4s,5s)-2-(Acetylamino)-5-Carboxy-3,4-Dihydroxypiperidinium. Grades: 95%. CAS No. 54795-58-3. Molecular formula: C8H14N2O5. Mole weight: 218.21.
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