SD-208 NEW
| Price | $34 | $47 | $73 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-17 |
Product Details
| Product Name: SD-208 | CAS No.: 627536-09-8 |
| Purity: ≥95% | Supply Ability: 10g |
| Release date: 2024/11/17 |
Product Introduction
Bioactivity
| 名稱(chēng) | SD-208 |
| 描述 | SD-208 (ALK5 Inhibitor V), a selective TGF-βRI (ALK5) inhibitor (IC50: 48 nM), is >100-fold selectivity over TGF-βRII. |
| 細(xì)胞實(shí)驗(yàn) | Glioma cells are cultured in the absence or presence of SD-208 (1 μM) for 48 hours. The cells are pulsed for the last 24 hours with [methyl-3H]thymidine (0.5 μCi) and harvested, and incorporated radioactivity is determined in a liquid scintillation counter.(Only for Reference) |
| 激酶實(shí)驗(yàn) | Kinase assay: Various kinase activities are assayed by measuring the incorporation of radiolabeled ATP into a peptide or protein substrate. The reactions are performed in 96-well plates and included the relevant kinase, substrate, ATP, and appropriate cofactors. The reactions are incubated and then stopped by the addition of phosphoric acid. Substrate is captured onto a phosphocellulose filter, which is washed free of unreacted ATP. The counts incorporated are determined by counting on a microplate scintillation counter. The ability of SD-208 to inhibit the respective kinase is determined by comparing counts incorporated in the presence of compound with those incorporated in the absence of compound. |
| 體外活性 | SD-208 (1 mg/mL, p.o.) significantly prolonged the median survival rate of mice loaded with SMA-560 glioma. In syngeneic 129S1 mice, SD-208 (60 mg/kg, p.o.) inhibited the growth of primary R3T tumors and reduced the number and size of lung metastases. Additionally, in a murine aortic allograft model, SD-208 effectively reduced the formation of intimal hyperplasia associated with transplant arteriosclerosis. |
| 體內(nèi)活性 | In vitro, SD-208 inhibits TGF-β-induced receptor-associated Smads, Smad2/3 phosphorylation, and stimulates differentiation, migration, and invasion from epithelial to mesenchymal cells into the basal membrane. Additionally, SD-208 blocks the protective effects of TGF-β on the migration and proliferation of neointimal smooth muscle-like cells. In both mouse SMA-560 and human SMA-560 glioma cells, SD-208 suppresses cell growth, constitutive and TGF-β-induced migration and infiltration, and enhances immunogenicity. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 7.1 mg/mL (20 mM), Heating is recommended. |
| 關(guān)鍵字 | inhibit | Transforming growth factor beta receptors | TGF-β Receptor | Inhibitor | SD 208 | SD-208 |
| 相關(guān)產(chǎn)品 | Monocrotaline | SB-431542 | DMH-1 | RepSox | Chromenone 1 | LY-364947 | BMP signaling agonist sb4 | Pirfenidone | A 83-01 | Galunisertib | Alantolactone | Pentabromophenol |
| 相關(guān)庫(kù) | 高選擇性抑制劑庫(kù) | 抗結(jié)直腸癌化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 酪氨酸激酶分子庫(kù) | 抗肥胖化合物庫(kù) | 抑制劑庫(kù) | 已知活性化合物庫(kù) | 含氟化合物庫(kù) | TGF-β/Smad靶點(diǎn)化合物庫(kù) | 抗癌活性化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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