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5.09583

Sigma-Aldrich

Diaphanous (mDia)-related Formin Agonist, IMM01

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C12H17N3O2S
CAS Number:
Molecular Weight:
267.35
UNSPSC Code:
12352200
NACRES:
NA.77

Pricing and availability is not currently available.

Assay

≥98% (HPLC)

Quality Level

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

storage temp.

2-8°C

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.
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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


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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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