GP-82996 NEW
| Price | $29 | $39 | $68 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-08 |
Product Details
| Product Name: GP-82996 | CAS No.: 359886-84-3 |
| Purity: 99.57% | Supply Ability: 10g |
| Release date: 2024/11/08 |
Product Introduction
Bioactivity
| 名稱 | GP-82996 |
| 描述 | GP-82996 (CINK4) is a pharmacological inhibitor specifically targeting CDK4/6, exhibiting IC50 values of 1.5 μM for CDK4/cyclin D1, 5.6 μM for CDK6/cyclin D1, and 25 μM for Cdk5/p35. It effectively induces apoptosis in U2OS cancer cells, positioning it as a potential investigational tool in cancer research [1] [2]. |
| 體外活性 | GP-82996, at concentrations of 5 and 10 μM applied for 24 hours, causes a G1 phase arrest and an increase in the G0-G1/S ratio in U2OS (p16 negative) and MRC-5 (p16 positive) cells, while reducing the hyperphosphorylation of pRb without affecting CDK4 levels in these cell lines. In U2OS cells, a 48-hour exposure to 10μM of GP-82996 results in apoptosis in 83% of the population. Additionally, GP-82996 inhibits the proliferation of A549, H358, SKLU-1, H23, and PC14 cells, with IC50 values around 4-7 μM after 72 hours of treatment. The compound also induces G1 arrest in A549 and H23 cells at concentrations of 3, 5, and 10 μM over 48 hours and enhances the sensitivity of KRAS mutation-bearing lung cancer cells (A549, SKLU-1, H23) to Paclitaxel with varied concentrations (1, 3, 5, 10 μM) over 72 hours. A combination of GP-82996 (10 μM) and Paclitaxel (3 nM) over 72 hours notably increases apoptosis in A549 and H23 cells. |
| 體內(nèi)活性 | GP-82996 (30 mg/kg, i.p. for 29 days) significantly reduced final tumor volume compared to the vehicle control in mouse xenograft models [1]. In female BALB/c nu/nu mice (19-21 g) with HCT116 tumors (100 mm^3), the compound was administered intraperitoneally at 30 mg/kg every 12 hours for 29 days, leading to smaller tumor volumes than the control group [1]. |
| 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 : 50 mg/mL (109.51 mM), Sonication is recommended. |
| 關(guān)鍵字 | GP82996 | CINK-4 | GP 82996 | CINK 4 | GP-82996 |
| 相關(guān)產(chǎn)品 | Ribociclib | Ro-3306 | GSK 3 Inhibitor IX | Rafoxanide | Palbociclib monohydrochloride | CASIN | Palbociclib | GW 441756 | Sodium Oxamate | Abemaciclib | Dinaciclib | Abemaciclib methanesulfonate |
| 相關(guān)庫(kù) | 抗胰腺癌化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 激酶抑制劑庫(kù) | 抗乳腺癌化合物庫(kù) | 抑制劑庫(kù) | 抗衰老化合物庫(kù) | 已知活性化合物庫(kù) | 抗癌化合物庫(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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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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