CDDO-Im (RTA-403)

Synonyms: CDDO-Imidazolide, TP-235

CDDO-Im (RTA-403) is an activator of nuclear factor erythroid 2–related factor 2 (Nrf2) and peroxisome proliferator-activated receptor (PPAR). CDDO-Im binds to PPARα and PPARγ with Ki of 232 nM and 344 nM, respectively. CDDO-Im inhibits inflammatory response and tumor growth in vivo.

CDDO-Im (RTA-403) Chemical Structure

CDDO-Im (RTA-403) Chemical Structure

CAS No. 443104-02-7

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CDDO-Im (RTA-403) Related Products

Biological Activity

Description CDDO-Im (RTA-403) is an activator of nuclear factor erythroid 2–related factor 2 (Nrf2) and peroxisome proliferator-activated receptor (PPAR). CDDO-Im binds to PPARα and PPARγ with Ki of 232 nM and 344 nM, respectively. CDDO-Im inhibits inflammatory response and tumor growth in vivo.
Targets
Nrf2 [1] PPARα [1]
(Cell-free assay)
PPARγ [1]
(Cell-free assay)
232 nM(Ki) 344 nM(Ki)
In vitro
In vitro

CDDO-Im is highly active in suppressing cellular proliferation of human leukemia and breast cancer cell lines (IC50, 10–30 nM). In U937 leukemia cells, CDDO-Im also induces monocytic differentiation as measured by increased cell surface expression of CD11b and CD36. CDDO-Im has significant actions independent of PPAR transactivation.[2]

Cell Research Cell lines U937, THP-1, and HL-60 leukemia cells
Concentrations 100 pM to 1 μM
Incubation Time 5 days
Method

U937, THP-1, and HL-60 leukemia cells are treated with either control vehicle, CDDO, or CDDO-Im at concentrations ranging from 100 pM to 1 μM, and after 5 days, proliferation is measured by cell counting.

In Vivo
In vivo

CDDO-Im is a novel synthetic triterpenoid more potent than its parent compound (CDDO). In vivo, CDDO-Im is a potent inhibitor of de novo inducible nitric oxide synthase expression in primary mouse macrophages. Moreover, CDDO-Im inhibits growth of B16 murine melanoma and L1210 murine leukemia cells in vivo.[2]

Animal Research Animal Models female CD-1 mice, male and female BDF-1 mice
Dosages 1 nmole, 10 nmole
Administration IP

Chemical Information & Solubility

Molecular Weight 541.72 Formula
C34H43N3O3
CAS No. 443104-02-7 SDF --
Smiles CC1(C)CCC2(CCC3(C)C(C2C1)C(=O)C=C4C5(C)C=C(C#N)C(=O)C(C)(C)C5CCC34C)C(=O)[N]6C=CN=C6
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 56 mg/mL ( (103.37 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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