Ingenol mebutate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ingenol mebutate 是 PKC 亚型（包括 PKC-α、PKC-β、PKC-γ、PKC-δ 和 PKC-ε）的有效激活剂，Kis 为 0.3、0.105、0.162、0.376 和 0.171 nM。

Ingenol mebutate is a potent activator of PKC subtypes including PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM. Ingenol mebutate exhibits antiinflammatory and antitumor activity.(In Vitro):Ingenol mebutate shows EC50s for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-δ, PKC-ε and PKC-μ of 13, 4.37, 10.5, 38.6, 1.08 and 0.9 nM in WEHI-231 cells. The EC50s are 198, 69.1, 4.6, 1 nM in HOP-92 cells for PKC-α, PKC-βI, PKC-ε, PKC-μ and 635, 146, 4.7, 1.1, 30 nM for PKC-α, PKC-βI, PKC-δ, PKC-ε, PKC-μ in Colo-205 cells. Ingenol mebutate sensitizes WEHI-231 cells, HOP-92 and Colo-205 cells with IC50s of 1.41, 3.24, and 11.9 nM, respectively. Ingenol mebutate (20 nM) induces apoptosis in a PKC-δ dependent manner in primary AML marrow blasts but not in normal myeloblasts.

Ingenol Mebutate (Ingenol 3-angelate) is an active ingredient in Euphorbia peplus, acting as a potent PKC activator, with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively. Ingenol Mebutate also EC50s of 13 ± 2.4 nM (PKC-α), 4.37 ± 0.4 nM (PKC-βI), 10.5 ± 2.2 nM (PKC-βII), 38.6 ± 2.9 nM (PKC-δ), 1.08 ± 0.01 nM (PKC-ε), 0.9 ± 0.13 nM (PKC-μ) in WEHI-231 cells, 198 ± 12.5 nM (PKC-α), 69.1 ± 8.2 nM (PKC-βI), 4.6 ± 0.4 nM (PKC-ε) and 1 nM (PKC-μ) in HOP-92 cells, 635 ± 245 nM (PKC-α), 146 ± 35 nM (PKC-βI), 4.7 ± 0.7 nM (PKC-δ), 1.1 ± 0.5 nM (PKC-ε), and 30 nM (PKC-μ) in Colo-205 cells. Ingenol Mebutate sensitizes WEHI-231 cells, HOP-92 and Colo-205 cells, with IC50s of 1.41 ± 0.255 nM, 3.24 ± 2.01 nM, and 11.9 ± 1.307 nM, respectively. Ingenol Mebutate (PEP005; 20 nM) actions are PKC-δ dependent, induces apoptosis in primary AML marrow blasts but not in normal myeloblasts. Ingenol Mebutate (PEP005) activates PKCδ and inhibits PKCα. Colo205-R cells (IC50: >10 μM) are >300-fold more resistant to Ingenol Mebutate than parental Colo205-S cells.

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PEP005 | Ingenol 3-Angelate

Others

Other Targets

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75567-37-2

430.541

C25H34O6

>98% (HPLC)

In Vitro:?DMSO : ≥ 100 mg/mL (232.27 mM)

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(-20℃)

With Ice Pack

≥ 2 years