| Identification | Back Directory | [Name]
Cl-Amidine | [CAS]
1043444-18-3 | [Synonyms]
Cl-amidine TFA
Cl-Amidine (trifluoroacetate salt) | [Molecular Formula]
C14H19ClN4O2?CF3CO2H | [MDL Number]
MFCD31536783 | [MOL File]
1043444-18-3.mol | [Molecular Weight]
424.81 |
| Chemical Properties | Back Directory | [storage temp. ]
Keep in dark place,Inert atmosphere,2-8°C | [solubility ]
≤20mg/ml in ethanol;50mg/ml in DMSO;14mg/ml in dimethyl formamide | [form ]
crystalline solid |
| Hazard Information | Back Directory | [Biological Activity]
cl-amidine is a pad4 deimination activity inhibitor.protein arginine deiminase 4 (pad4) can catalyze the post-translational modification of arginine residues on histones to form citrulline, which can change gene expression. thus, dysregulated pad4 activity has been implicated in cancer and rheumatoid arthritis. | [in vitro]
previous study found that cl-amidine antagonized the pad4-mediated enhancement of the the p300gbd-grip1 interaction dose-dependently, and it was noteworthy that cl-amidine treatment had only a minimal reduction in the efficiency of the interaction in cys645s-transfected cells, thereby suggesting that the inhibitory effect of cl-amidine was not a nonspecific one but was targeted at the active pad4 enzyme. these results demonstrated that cl-amidine was significantly more potent than f-amidine, consistent with its improved in vitro potency [1]. | [in vivo]
animal study showed that cl-amidine could improve survival in a mouse model of cecal ligation and puncture (clp)-induced septic shock. cl-amidine was proven to play protective roles by restoring innate immune cells in bm, decreasing bm and thymus atrophy, increasing blood monocytes and blood/liver bacteria clearance, and attenuating pro-inflammatory cytokine production in a murine lethal sepsis model [2]. | [target]
| Target | Value | PAD1
(Cell-free assay) | 0.8 μM | PAD4
(Cell-free assay) | 5.9 μM | < td style="border-bottom: 1px dotted #ccc;padding: 5px;"> PAD3
(Cell-free assay) 6.2 μM |
| [IC 50]
5.9 μm | [storage]
Store at -20°C | [References]
[1] luo, y. ,arita, k.,bhatia, m., et al. inhibitors and inactivators of protein arginine deiminase 4: functional and structural characterization. biochemistry 45(39), 11727-11736 (2006).
[2] zhao t, pan b, alam hb, liu b, bronson rt, deng q, wu e, li y. protective effect of cl-amidine against clp-induced lethal septic shock in mice. sci rep. 2016 nov 7;6:36696. |
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DC Chemicals
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021-58447131 13564518121 |
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