cp028

Name: cp028
Brand: AOBIOUS
SKU: AOB33671
Price: 89 USD
Availability: InStock

Cat No: AOB33671

Condition

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	mg	Unit Price ($/mg or $/Unit)	Final Price
1	5	$75.65	Total: $378.25
1	10	$64.08	Total: $640.80
1	25	$54.29	Total: $1,357.25
1	50	$46.28	Total: $2,314.00
1	100	$40.05	Total: $4,005.00

Overview

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

Chemical Properties

Molecular Formula	C23H17FN2O4
Molecular Weight	404.39
CAS Numbers	347397-83-5
Solubility	DMSO
Purity	98% by HPLC
IUPAC/Chemical Name	1-(2-Ethylphenyl)-5-((5-(4-fluorophenyl)furan-2-yl)methylene) pyrimidine-2,4,6 (1H,3H,5H)-trione
InChl Key	KKBJKSJVJPXCRA-QGOAFFKASA-N
InChl Code	InChI=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 Code	O=C1NC(/C(C(N1C2=CC=CC=C2CC)=O)=CC3=CC=C(C4=CC=C(F)C=C4)O3)=O

Storage and Handling

0°C (short term), -20°C (long term), desiccated

Synonyms

cp028; cp-028; cp 028; Compound 028; Compound-028; Compound028;

References

1) 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.