5.09583
Diaphanous (mDia)-related Formin Agonist, IMM01
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Synonym(s):
Diaphanous (mDia)-related Formin Agonist, IMM01, Formin Activator
Empirical Formula (Hill Notation):
C12H17N3O2S
Recommended Products
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.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Primary Target
mDia
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.
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
Regulatory Information
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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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