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Ingenol mebutate

Catalog No. TN1047   CAS 75567-37-2
Synonyms: Ingenol 3-Angelate, PEP005

Ingenol mebutate (Ingenol 3-Angelate) 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.

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Ingenol mebutate Chemical Structure
Ingenol mebutate, CAS 75567-37-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 64.00
2 mg In stock $ 98.00
5 mg In stock $ 209.00
10 mg In stock $ 349.00
25 mg In stock $ 577.00
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1 mL * 10 mM (in DMSO) In stock $ 196.00
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Purity: 99.04%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ingenol mebutate (Ingenol 3-Angelate) 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.
Targets&IC50 PKC-δ:0.376 nM (Ki), PKC-α:0.3 nM (Ki), PKC-γ:0.162 nM (Ki), PKC-ε:0.171 nM (Ki), PKC-β:0.105 nM (Ki)
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[2]. Ingenol mebutate (20 nM) induces apoptosis in a PKC-δ dependent manner in primary AML marrow blasts but not in normal myeloblasts[3].
Source
Synonyms Ingenol 3-Angelate, PEP005
Molecular Weight 430.53
Formula C25H34O6
CAS No. 75567-37-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90 mg/mL (209 mM)

TargetMolReferences and Literature

1. Ghoul A, et al. Epithelial-to-mesenchymal transition and resistance to ingenol 3-angelate, a novel protein kinase C modulator, in colon cancer cells. Cancer Res. 2009 May 15;69(10):4260-9. 2. Kedei N, et al. Characterization of the interaction of ingenol 3-angelate with protein kinase C. Cancer Res. 2004 May 1;64(9):3243-55. 3. Hampson P, et al. PEP005, a selective small-molecule activator of protein kinase C, has potent antileukemic activity mediated via the delta isoform of PKC. Blood. 2005 Aug 15;106(4):1362-8.

Related compound libraries

This product is contained In the following compound libraries:
Approved Drug Library RO5 Drug-like Natural Product Library Natural Product Library for HTS

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Keywords

Ingenol mebutate 75567-37-2 Chromatin/Epigenetic Cytoskeletal Signaling Immunology/Inflammation Microbiology/Virology Proteases/Proteasome gp120/CD4 HIV Protease PKC Ingenol 3-Angelate PEP 005 PEP005 PEP-005 inhibitor inhibit

 

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