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cp028

AOB33671

CAS: 347397-83-5

 

Chemical Name: Compound 028; 1-(2-Ethylphenyl)-5-((5-(4-fluorophenyl)furan-2-yl)methylene) pyrimidine-2,4,6 (1H,3H,5H)-trione

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Quantity Discount Table - Order More To Get More Price Discount

QuantitymgUnit Price ($/mg or $/Unit)Final Price
15 $75.65 Total: $378.25
110 $64.08 Total: $640.80
125 $54.29 Total: $1,357.25
150 $46.28 Total: $2,314.00
1100 $40.05 Total: $4,005.00

Data sheet

Molecular FormulaC23H17FN2O4
Molecular Weight404.39
CAS Numbers347397-83-5
Storage Condition0°C (short term), -20°C (long term), desiccated
SolubilityDMSO
Purity98% by HPLC
Synonymcp028; cp-028; cp 028; Compound 028; Compound-028; Compound028;
IUPAC/Chemical Name1-(2-Ethylphenyl)-5-((5-(4-fluorophenyl)furan-2-yl)methylene) pyrimidine-2,4,6 (1H,3H,5H)-trione
InChl KeyKKBJKSJVJPXCRA-QGOAFFKASA-N
InChl CodeInChI=1S/C23H17FN2O4/c1-2-14-5-3-4-6-19(14)26-22(28)18(21(27)25-23(26)29)13-17-11-12-20(30-17)15-7-9-16(24)10-8-15/h3-13H,2H2,1H3,(H,25,27,29)/b18-13+
SMILES CodeO=C1NC(/C(C(N1C2=CC=CC=C2CC)=O)=CC3=CC=C(C4=CC=C(F)C=C4)O3)=O
References1) Sidarovich A, Will CL, Anokhina MM, Ceballos J, Sievers S, Agafonov DE, Samatov T, Bao P, Kastner B, Urlaub H, Waldmann H, Lührmann R. Identification of a small molecule inhibitor that stalls splicing at an early step of spliceosome activation. Elife. 2017 Mar 16;6. pii: e23533. doi: 10.7554/eLife.23533. PubMed PMID: 28300534; PubMed Central PMCID: PMC5354520.

More info

Novel inhibitor of pre-mRNA splicing in vitro

Identity and basic properties

  • CP028 is a small molecule inhibitor, CAS No. 347397-83-5.

  • It is described in the literature as a pre-mRNA splicing inhibitor, specifically interfering with spliceosome activation. MPG.PuRe+1

  • In the “Identification of a small molecule inhibitor that stalls splicing …” paper, the authors name CP028 (R = 4-fluoro in a scaffold) as the compound that blocks conversion of the pre-catalytic spliceosomal B complex into the activated B^act complex. MPG.PuRe+1

Mechanism / functional effect

  • CP028 stalls the spliceosome at an intermediate activation stage: it prevents the transition from the B complex to the B^act complex. MPG.PuRe+1

  • In the stalled spliceosome complex (termed B028), some rearrangements (e.g. release of U4/U6 snRNP proteins) have occurred, but full activation does not proceed (e.g. incorporation of Prp19/CDC5L complex). MPG.PuRe

  • Thus, CP028 acts upstream of full spliceosome catalytic activation, and is useful as a tool for dissecting spliceosome dynamics. MPG.PuRe

Biological / applied relevance

  • Because splicing is essential for mRNA maturation, inhibiting activation of the spliceosome can suppress expression of many genes, particularly those reliant on efficient splicing.

  • In a more specific context, one recent study tied CP028’s splicing inhibition to antiviral effects. In the context of hepatitis B virus (HBV) infection, CP028 (acting upstream of the LSm2-8 complex, which is involved in U6 snRNA and spliceosome machinery) suppressed viral RNA levels, and potentiated the effect of IFN-α. Frontiers

  • That same HBV study notes that knockdown of LSm8 had similar effects, and CP028’s splicing inhibition may disrupt the function of the nuclear LSm2-8 complex (which is involved in U6 snRNA / spliceosome function) in a way that suppresses HBV biosynthesis. Frontiers+1

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