Rottlerin
产品名称:Rottlerin
产品描述:
结构类型 | 天然产物 > 其他 |
产品描述 | Rottlerin is a natural product purified from Mallotus Philippinensis and is a specific PKC inhibitor (IC50: PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM). Rottlerin causes apoptosis via caspase 3 activation. |
靶点活性 | PKCγ:40 μM(baculovirus-infected Sf9 insect cells), PKA:78 μM, PKCδ:3 μM(Porcine spleen), PKCζ:100 μM(baculovirus-infected Sf9 insect cells), PKCη:82 μM(baculovirus-infected Sf9 insect cells), PKCε:100 μM(baculovirus-infected Sf9 insect cells), CKII:30 μM(holoenzyme expressed in E.coli), PKCβ:42 μM(baculovirus-infected Sf9 insect cells), PKCα:30 μM(baculovirus-infected Sf9 insect cells) |
体外活性 | Rottlerin (20 μM) shows cell proliferation in HMVEC. Rottlerin (20 μM, 2/6/24 hours) dramatically reduces the cyclin D-1 mRNA levels in a time-dependent manner in primary HMVEC [2]. |
体内活性 | Rottlerin inhibits tumor cell proliferation and causes apoptosis through activation of caspase-3 and cleavage of the poly polymerase. Rottlerin (20 mg/kg, gavage 5 days per week, once daily, for 6 weeks) inhibits AsPC-1 pancreatic tumor growth in Balb C nude mice with no toxicity [3]. |
别名 | NSC 94525, Mallotoxin, 粗糠柴苦素, NSC 56346 |
分子量 | 516.54 |
分子式 | C30H28O8 |
CAS No. | 82-08-6 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 2 mg/mL (3.87 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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