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Merck
CN

5.09583

Diaphanous (mDia)-related Formin Agonist, IMM01

别名:

Diaphanous (mDia)-related Formin Agonist, IMM01, Formin Activator

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关于此项目

经验公式(希尔记法):
C12H17N3O2S
化学文摘社编号:
分子量:
267.35
MDL number:
NACRES:
NA.77
UNSPSC Code:
12352200
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assay

≥98% (HPLC)

form

powder

potency

140 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

off-white

solubility

DMSO: 100 mg/mL

Quality Level

General description

A hydrazinecarbothioamide derived intramimic that acts as an agonist of mammalian Diaphanous (mDia)-related formins and disrupts diaphanous inhibitory domain (DID) and diaphanous autoregulatory domain (DAD) interaction (IC50 = 140 nM). Shown to trigger actin assembly and stabilize microtubules in a dose -dependent manner and at levels similar to those induced by Taxol. Induces caspase-3 activation and apoptosis in NIH 3T3 and SW480 cells(~ 100 µM) and slows the growth of SW480 xenograft tumors in mice (~ 25 mg/kg). Shown to induce LacZ expression, producing b-gal activity that is comparable to effects seen with cytochalasin D treatment.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Primary Target
mDia
Reversible: yes

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Lash, L.L., et al. 2013. Cancer Res.73, 6793.
Copeland, S.J. et al. 2007. J Biol. Chem. 282, 30120.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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L Leanne Lash et al.
Cancer research, 73(22), 6793-6803 (2013-11-19)
Although the cancer cell cytoskeleton is a clinically validated target, few new strategies have emerged for selectively targeting cell division by modulating the cytoskeletal structure, particularly ways that could avoid the cardiotoxic and neurotoxic effects of current agents such as
Sarah J Copeland et al.
The Journal of biological chemistry, 282(41), 30120-30130 (2007-08-25)
Formins are multidomain proteins that regulate numerous cytoskeleton-dependent cellular processes. These effects are mediated by the presence of two regions of homology, formin homology 1 and FH2. The diaphanous-related formins (DRFs) are distinguished by the presence of interacting N- and

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