1043444-18-3 Usage
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].
IC 50
5.9 μm
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.
Check Digit Verification of cas no
The CAS Registry Mumber 1043444-18-3 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,4,3,4,4 and 4 respectively; the second part has 2 digits, 1 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 1043444-18:
(9*1)+(8*0)+(7*4)+(6*3)+(5*4)+(4*4)+(3*4)+(2*1)+(1*8)=113
113 % 10 = 3
So 1043444-18-3 is a valid CAS Registry Number.
1043444-18-3Relevant articles and documents
SYNTHESIS AND USE OF NOVEL INHIBITORS AND INACTIVATORS OF PROTEIN ARGININE DEIMINASES
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Page/Page column 12, (2008/06/13)
In one embodiment of the present disclosure, an inactivator of protein arginine deiminase 4 is disclosed. The inactivator includes: (I) and x includes F, Cl, and H, y includes OH and NH2, R includes H, an alkyl group, an alkenyl group, an alknyl group, and n is greater than 0.
