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IRE1α kinase-IN-2 is a potent IRE1α kinase inhibitor, with an EC50 of 0.82 μM. IRE1α kinase-IN-2 inhibits IRE1α kinase autophosphorylation (IC50=3.12 μM). IRE1α kinase-IN-2 inhibits XBP1 mRNAsplicing in the WT cell lines .
Madrasin (DDD00107587) is a splicing inhibitor that prevents formation of both splicing intermediates and products in vitro and interferes with one or more early steps in the pathway of spliceosome assembly. Madrasin also can inhibit pre-mRNAsplicing in vitro and modify splicing of endogenous pre-mRNA in cells .
Hinokiflavone is a novel modulator of pre-mRNAsplicing activity in vitro and in cellulo. Hinokiflavone blocks splicing of pre-mRNA substrates by inhibiting spliceosome assembly, specifically preventing B complex formation. Hinokiflavone is a SUMO protease inhibitor, inhibiting sentrin-specific protease 1 (SENP1) activity .
PRMT5-IN-28 (compound 36) is an inhibitor of protein arginine methyltransferase 5 (PRMT5) enzyme. Protein arginine methylation is a common post-translational modification involved in gene transcription, mRNAsplicing, DNA repair, protein cellular localization, cell fate determination and signal transduction, etc. Abnormal PRMT5 can promote cancer cell proliferation, resist apoptosis, enhance invasion and metastasis, and affect immune escape .
CD33 splicing modulator 1 (Compound 1) is a CD33 splicing modulator. CD33/Siglec 3 is a myeloid lineage cell surface receptor that is known to regulate microglia activity. CD33 splicing modulator 1 increases exon 2 skipping in cellular mRNA pools. CD33 splicing modulator 1 has the potential for the research of neurodegenerative disease including Alzheimer's disease .
CD33 splicing modulator 1 (Compound 1) hydrochloride is a CD33 splicing modulator. CD33/Siglec 3 is a myeloid lineage cell surface receptor that is known to regulate microglia activity. CD33 splicing modulator 1 hydrochloride increases exon 2 skipping in cellular mRNA pools. CD33 splicing modulator 1 hydrochloride has the potential for the research of neurodegenerative disease including Alzheimer's disease .
m7GpppGpG, an oligonucleotide, is an M 7GpppNpG trinucleotide cap analogue. m7GpppGpG prevents premature degradation by 5′-exonucleases and recruits proteins required for pre-mRNAsplicing, mRNA transport and initiation of protein biosynthesis .
SMN-C2, an analog of RG-7916, is a selective modulator of SMN2 gene splicing that acts by binding SMN2 pre-mRNA, thereby increasing far upstream element binding protein 1 (FUBP1) and KH-spliced RNA binding Protein affinity regulator protein (KHSRP) to the SMN2 pre-mRNA complex. SMN-C2 can be used in spinal muscular atrophy (SMA) research .
Risdiplam (RG7916) is an orally administered, centrally and peripherally distributed SMN2 pre-mRNAsplicing modifier that increases survival motor neuron (SMN) protein levels .
Drisapersen, a antisense oligonucleotide, induces exon 51 skipping during dystrophin pre-mRNAsplicing and allows synthesis of partially functional dystrophin in Duchenne muscular dystrophy (DMD) patients with amenable mutations.
NSC 194308, a U2AF2-RNA complexes enhancer, increases association of the U2AF1-U2AF2-SF1-splice site RNA complex by binding a site between the U2AF2 RNA recognition motifs (RRM1 and RRM2). NSC 194308 inhibits pre-mRNAsplicing by stalling spliceosome assembly at the point where U2AF helps recruit U2 snRNP to the branchpoint. NSC 194308 enhances the binding of pre-mRNA to U2AF2, selectively triggering cell death in leukemia cell lines containing spliceosome mutations .
Isoginkgetin is a pre-mRNAsplicing inhibitor inhibitor. Isoginkgetin also inhibits activities of both Akt, NF-κB and MMP-9. Isoginkgetin inhibits the activity of the 20S proteasome, induces apoptosis and activates autophagy .
Risdiplam-d4 is deuterium labeled Risdiplam. Risdiplam (RG7916) is an orally administered, centrally and peripherally distributed SMN2 pre-mRNAsplicing modifier that increases survival motor neuron (SMN) protein levels[1].
FITC-labeled Drisapersen (sodium) is Drisapersen labeled with FITC. Drisapersen, a antisense oligonucleotide, induces exon 51 skipping during dystrophin pre-mRNAsplicing and allows synthesis of partially functional dystrophin in Duchenne muscular dystrophy (DMD) patients with amenable mutations.
Risdiplam-hydroxylate-d3 is a Risdiplam-hydroxylate tritium substitute. Risdiplam (RG7916) is an orally administered, centrally and peripherally distributed SMN2 pre-mRNAsplicing modifier that increases survival motor neuron (SMN) protein levels .
Risdiplam-hydroxylate-d6 is a Risdiplam-hydroxylate tritium substitute. Risdiplam (RG7916) is an orally administered, centrally and peripherally distributed SMN2 pre-mRNAsplicing modifier that increases survival motor neuron (SMN) protein levels .
Pladienolide B is a potent cancer cell growth inhibitor that targets the SF3B1 subunit of the spliceosome. Pladienolide B exerts antitumor activities mediated through the inhibition of pre-mRNAsplicing. Pladienolide B induces apoptosis .
Herboxidiene (GEX1A) is a potent phytotoxic polyketide from Streptomyces sp. A7847 with a diverse range of activities, including herbicidal, anti-cholesterol, anti-tumor effects. Herboxidiene inhibits the pre-mRNAsplicing process by binding to spliceosome-associated protein (SAP) 155, a subunit of SF3b, in the splicesome .
SPHINX31 is a potent and selective SRPK1 inhibitor, with an IC50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 also decreases the mRNA expression of pro-angiogenic VEGF-A165a isoform. SPHINX31 can be used to research neovascular eye disease .
Spliceostatin A, the FR901464 (HY-16212) methylated derivative, is a potent anti-tumor agent. Spliceostatin A inhibits splicing and promotes pre-mRNA accumulation by binding SF3B1. SF3B1 is a subcomplex of U2 small nuclear ribonucleoprotein in the spliceosome. Spliceostatin A induces Apoptosis in chronic lymphocytic leukemia (CLL) cells .
HTT-D3 is a potent and orally active huntingtin (HTT)splicing modulator. HTT-D3 acts by promoting the inclusion of a pseudoexon containing a premature termination codon (stop-codon psiExon), leading to HTT mRNA degradation and reduction of HTT levels. HTT-D3 reduces p-glycoprotein (P-gp) efflux, and can be uesd for Huntington's disease research .
NVS-SM2 is a potent, orally active and brain-penetrant SMN2 splicing enhancer with an EC50 of 2 nM for SMN. NVS-SM2 enhances U1-pre-mRNA association. NVS-SM2 promotes exon 7 inclusion and restores normal survival motor neuron (SMN) protein expression. NVS-SM2 can be used for spinal muscular atrophy (SMA) research .
HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to agents targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50s ranging from 0.9 to 1.5 μM .
Hinokiflavone is a novel modulator of pre-mRNAsplicing activity in vitro and in cellulo. Hinokiflavone blocks splicing of pre-mRNA substrates by inhibiting spliceosome assembly, specifically preventing B complex formation. Hinokiflavone is a SUMO protease inhibitor, inhibiting sentrin-specific protease 1 (SENP1) activity .
Isoginkgetin is a pre-mRNAsplicing inhibitor inhibitor. Isoginkgetin also inhibits activities of both Akt, NF-κB and MMP-9. Isoginkgetin inhibits the activity of the 20S proteasome, induces apoptosis and activates autophagy .
Herboxidiene (GEX1A) is a potent phytotoxic polyketide from Streptomyces sp. A7847 with a diverse range of activities, including herbicidal, anti-cholesterol, anti-tumor effects. Herboxidiene inhibits the pre-mRNAsplicing process by binding to spliceosome-associated protein (SAP) 155, a subunit of SF3b, in the splicesome .
SRSF1 protein plays a crucial role in splicing regulation, preventing exon skipping and ensuring splicing accuracy. It interacts with spliceosomal components, forming a bridge between 5'- and 3'-splice site binding elements. SRSF1 stimulates U1 snRNP binding and prefers purine-rich RNA sequences, functioning as a splicing enhancer. It can act as a splicing repressor through isoforms ASF-2 and ASF-3. Additionally, SRSF1 may facilitate mRNA nuclear export and is identified in the spliceosome C complex, participating in ribonucleoprotein complexes with various RNA-binding proteins. Its interactions with multiple proteins highlight its intricate role in splicing and cellular processes. SRSF1 Protein, Human (His-SUMO) is the recombinant human-derived SRSF1 protein, expressed by E. coli, with N-SUMO, N-6*His labeled tag. The total length of SRSF1 Protein, Human (His-SUMO) is 247 a.a., with molecular weight of 43.6 kDa.
SF3B3 protein is a key splicing factor in the SF3B complex and plays a central role in pre-mRNA splicing. It is essential for "A" complex assembly and stabilizes U2 snRNP binding to branch point sequences. SF3B3 Protein, Human (Sf9) is the recombinant human-derived SF3B3 protein, expressed by Sf9 insect cells , with tag free. The total length of SF3B3 Protein, Human (Sf9) is 1216 a.a., .
BCAS2 is essential for pre-mRNA splicing and is critical for spliceosome activation as a key component of the activated spliceosome and the PRP19-CDC5L complex. It may act as a scaffold in spliceosome assembly, forming contacts with core components. BCAS2 Protein, Human (N-GST) is the recombinant human-derived BCAS2 protein, expressed by E. coli , with N-GST labeled tag. The total length of BCAS2 Protein, Human (N-GST) is 224 a.a., with molecular weight of ~53 kDa.
SF3B3 protein is a key splicing factor in the SF3B complex and plays a central role in pre-mRNA splicing. It is essential for "A" complex assembly and stabilizes U2 snRNP binding to branch point sequences. SF3B3 Protein, Human (Sf9, His, Strep) is the recombinant human-derived SF3B3 protein, expressed by Sf9 insect cells , with N-Strep, N-8*His labeled tag. The total length of SF3B3 Protein, Human (Sf9, His, Strep) is 1216 a.a., .
BCAS2 Protein, Human (His, T7) plays crucial roles in pre-mRNA splicing and androgen receptor transcription. BCAS2 helps repair radiation-induced DSBs efficiently in both human PCa cells and Drosophila.
Risdiplam-d4 is deuterium labeled Risdiplam. Risdiplam (RG7916) is an orally administered, centrally and peripherally distributed SMN2 pre-mRNAsplicing modifier that increases survival motor neuron (SMN) protein levels[1].
Risdiplam-hydroxylate-d3 is a Risdiplam-hydroxylate tritium substitute. Risdiplam (RG7916) is an orally administered, centrally and peripherally distributed SMN2 pre-mRNAsplicing modifier that increases survival motor neuron (SMN) protein levels .
Risdiplam-hydroxylate-d6 is a Risdiplam-hydroxylate tritium substitute. Risdiplam (RG7916) is an orally administered, centrally and peripherally distributed SMN2 pre-mRNAsplicing modifier that increases survival motor neuron (SMN) protein levels .
