2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. RG3039 hydrochloride

RG3039 hydrochloride is an orally active, blood-brain barrier-permeable DcpS inhibitor with an IC50 of 4.2 nM against hDcpS. RG3039 hydrochloride inhibits the decapping activity of DcpS and maintains DcpS in a catalytically inactive conformation in the central nervous system and other tissues. RG3039 hydrochloride extends survival and improves function in spinal muscular atrophy mice. RG3039 hydrochloride is applicable to research related to spinal muscular atrophy.

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RG3039 hydrochloride

RG3039 hydrochloride Chemical Structure

CAS No. : 1466525-84-7

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Description

RG3039 hydrochloride is an orally active, blood-brain barrier-permeable DcpS inhibitor with an IC50 of 4.2 nM against hDcpS. RG3039 hydrochloride inhibits the decapping activity of DcpS and maintains DcpS in a catalytically inactive conformation in the central nervous system and other tissues. RG3039 hydrochloride extends survival and improves function in spinal muscular atrophy mice. RG3039 hydrochloride is applicable to research related to spinal muscular atrophy[1][2].

In Vitro

RG3039 (1-100 nM) potently hydrochloride inhibits the decapping enzyme activity of purified hDcpS, with an IC50 of 4.2 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RG3039 hydrochloride Related Antibodies
Parmacokinetics
Species Dose Route Cmax AUClast AUC0-inf CL/F Tmax (Plasma) AUCinf Tmax (Brain)
Mice[1] 10 mg/kg p.o. 25.6 (Plasma) ng/mL 156.8 (Plasma) ng·h/mL 285.8 (Plasma) ng·h/mL 35153 (Plasma) mL/h/kg 0.5 (Plasma) h 7049 (Brain) ng·h/mL 6.0 (Brain) h
In Vivo

RG3039 (20 mg/kg; p.o.; once daily; from P4 to P20) hydrochloride extends the median survival of 2B/2 SMA mice by over 600% to 112 days, and improves their cardiac, motor and neuromuscular functions[1].
RG3039 (20 mg/kg; p.o.; once daily; postnatal day 11 to postnatal day 20) hydrochloride confers only a very weak survival benefit in 2B/2 SMA mice (median survival time: 23 days)[1].
RG3039 hydrochloride (3-40 mg/kg; daily; starting from postnatal day 1) hydrochloride potently inhibits DcpS in vivo, and improves survival rate, motor function, synaptic connectivity, neuromuscular junction function and muscle size in severe SMA mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: FVB/N (neonatal pups; hemizygous SMA, generated by crossing FVB.Cg-Tg(SMN2)2HungSmn1tm1Hung/J 5058 mice)[1]
Dosage: 20 mg/kg
Administration: p.o.; once daily; P4 to P11
Result: Increased median survival by 38% compared with vehicle-treated mice.
Maintained righting reflex times of 10-14 s until P11, whereas vehicle-treated mice showed progressive slowing of righting reflex from ~13 s at P6 to 41 s at P10.
Animal Model: SMAD7 (severe spinal muscular atrophy delta 7) on FVB background (postnatal day 1, SMA model: null for endogenous mouse Smn gene, expressing human SMN2 gene and delta 7 transgene)[2]
Dosage: 10 mg/kg (survival, motor function, molecular/histological/electrophysiological endpoints); 3 mg/kg (DcpS inhibition); 20 mg/kg; 40 mg/kg (toxicity)
Administration: daily; from postnatal day 1 (until death for 10,20,40 mg/kg; to P10 for 3 mg/kg)
Result: Increased median survival by 26% compared with vehicle-treated mice.
Increased maximal weight achieved by 16%.
Improved righting time latencies after P11.
Improved ambulatory index scores between P13 and P17.
Increased full-length SMN transcript levels by 30-40% in neural tissues (spinal cord, brain) at P10, 6 hours after the last dose.
Increased VGLUT1 synapses on L3-L5 motor neurons by 50% at P13.
Increased percentage of fully innervated neuromuscular junctions (NMJs) to 57.4% in SPI muscle and 40.6% in longissimus capitis muscle at P12-P13.
Increased endplate potential (EPP) amplitude and quantal content by 30% in EDL muscle at P12-P13.
Decreased percentage of silent NMJs in splenius muscle to 20% at P12-P13.
Increased longissimus capitis muscle cross-sectional area by 80% and individual myofiber size by 95% at P12.
Inhibited DcpS enzyme activity by 90% within 2 hours and remained 80% inhibited 72 hours after the last dose in brain tissue (3 and 10 mg/kg doses dosed to P10).
Caused impaired weight gain and shortened survival (40 mg/kg dose).
Molecular Weight

505.27

Formula

C21H25Cl4N5O
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

NC1=NC(N)=C2C(OCC3CCN(CC4=C(Cl)C=CC=C4Cl)CC3)=CC=CC2=N1.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Purity & Documentation
References
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RG3039 hydrochloride Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RG30391466525-84-7RG 3039RG-3039DNA/RNA SynthesisSMN gemRNA metabolismspinal motor neuronneuromuscular junctionspinal muscular atrophycentral nervous systemSMN2SMA mouse modelsDcpSsmall nuclear ribonucleoproteinInhibitorinhibitorinhibit

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