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ZM 336372

SKU: orb1307326

Description

ZM 336372 is a highly specific small molecule inhibitor targeting the c-Raf kinase. It is utilized in biochemical and cellular research to investigate the RAF/MEK/ERK signaling pathway and has been applied in both in vitro assays and in vivo animal models of cancer.

Research Area

Cell Biology, Signal Transduction

Images & Validation

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ZM 336372

Key Properties

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CAS Number208260-29-1
MW389.45
Purity97.24%
FormulaC23H23N3O3
SMILESCN(C)c1cccc(c1)C(=O)Nc1ccc(C)c(NC(=O)c2ccc(O)cc2)c1
TargetRaf,Apoptosis
SolubilityDMSO:72 mg/mL (184.88 mM);Ethanol:2 mg/mL (5.14 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.14 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

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Target IC50
C-Raf:70 nM
In Vivo
1 μM ZM 336372 abrogated the up-regulation of eNOS after hydrogen peroxide treatment.ZM 336372 induced inhibition of proliferation, inhibition of hormone secretion and up-regulation of cell cycle inhibitors in a dose-dependent manner in HepG2.ZM 336372 acted selectively on C-Raf 10-fold compared to B-Raf.ZM 336372 inhibited proliferation and suppressed NE vasoactive peptide in pheochromocytoma cells.ZM 336372 inhibited proliferation of pheochromocytoma cells. ZM 336372 weakly inhibited SAPK2a/p38α and SAPK2b/p38β with an IC50 of 2 μM, and was more selective for C-Raf than for 17 other protein kinases, including PKA, PKC, AMPK, p42 MAPK, MKK1, SAPK1/JNK, and CDK1, at a concentration of up to 50 μM. ZM 336372 does not prevent growth factor or fobol ester-induced activation of MKKl or p42 MAPK/ERK2. By inhibiting the MAPK cascade, protein kinase C or phosphatidylinositol 3-kinase did not prevent ZM 336372-induced activation of c-Raf. ZM 336372 treatment induced the activation of c-Raf and B-Raf isoforms > 100, but it did not trigger any activation of MKKI or p42 MAPK/ERKP or induce any increase in GTP loading of Ras. , suggesting that the feedback control loop Raf isoform inhibits its own activation, and thus the inhibition is always counteracted by reactivation.ZM 336372 also induces apoptosis in pancreatic cancer cell lines by inhibiting glycogen synthase kinase-3β via phosphorylation of GSK-3β on Ser 9.
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Cell Research
Cells are exposed to various concentrations of ZM 336372 for 48 and 72 hours. After incubation, the medium is removed and cells are trypsinized. Cells are incubated on ice, and 2.5 μg/mL propidium iodide is added 5 minutes before flow cytometry. Data is acquired using a FACSCalibur benchtop flow cytometer using CellQuest acquisition and analysis software. Cytotoxicity is done using Cell Titer Glo Assay. Cell proliferation is measured using MTT assay.(Only for Reference)
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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inhibit, Inhibitor, Apoptosis, C-Raf, Raf kinases, Raf, ZM 336372, Zinc00581684, ZM336372, ZM-336372

Similar Products

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  • ZM 336372

    ZM 336372 [orb1225710]

    >98% (HPLC)

    208260-29-1

    389.4

    C23H23N3O3

    1 g, 500 mg, 200 mg, 2 mg, 25 mg, 10 mg, 100 mg, 50 mg, 5 mg
Quality Guarantee

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Compound Identifiers

PubChem CID
5730 ↗

Key Properties

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No computed properties available.

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ZM 336372 (orb1307326)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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2 mg
$ 80.00
1 ml x 10 mM (in DMSO)
$ 100.00
5 mg
$ 100.00
10 mg
$ 130.00
25 mg
$ 210.00
50 mg
$ 350.00
100 mg
$ 570.00
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