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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
53 Results for "
Splicing activity
" in MedChemExpress (MCE) Product Catalog:
Products (53)
53 Results for "Splicing activity" in MCE Product Catalog:
122
122 Publications Verification
Synonyms: CB-839
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Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat inuduces autophagy and has antitumor activity .
122
122 Publications Verification
Cat. No.: HY-12248A
CAS No.: 1874231-60-3
Synonyms: CB-839 hydrochloride
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Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity .
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8 Cited Publications
Cat. No.: HY-16399
CAS No.: 445493-23-2
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-mRNA splicing. Pladienolide B induces apoptosis .
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7 Cited Publications
Cat. No.: HY-N2360
CAS No.: 19202-36-9
Category:
Flavonoids Phenols Polyphenols Plants Disease Research Fields Selaginella tamariscina (P. Beauv.) Spring Biflavones Cancer Selaginellaceae Extract
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1
1 Cited Publications
H3B-8800 is a potent and orally active SF3B splicing modulator. H3B-8800 direct interaction with the SF3b complex and shows anti-cancer activity. H3B-8800 has the potential for the research of acute myeloid leukemia (AML) with SF3B1 mutant .
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1
1 Cited Publications
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EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC) .
Cat. No.: HY-126076A
CAS No.: 2410979-04-1
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VPC-80051 is an inhibitor of hnRNP A1 splicing activity. VPC-80051 directly interacts with hnRNP A1 RBD and reduces AR-V7 messenger levels in 22Rv1 CRPC cell line. VPC-80051 can be used in prostate cancer research .
Cat. No.: HY-19828
CAS No.: 142861-00-5
Synonyms: GEX1A
Category:
Microorganisms Ketones, Aldehydes, Acids Disease Research Fields Biological Pesticide Research Cancer Agricultural Research
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GLS1 Inhibitor-1 is an orally active, allosteric, selective GLS1 inhibitor with an IC50 of 0.021 µM for GLS1 and an IC50 of 0.051 µM for the GLS1 GAC splice variant. GLS1 Inhibitor-1 increases glutamine and decreases glutamate and aspartate. GLS1 Inhibitor-1 exhibits anticancer activity against non-small cell lung cancer. GLS1 Inhibitor-1 can be used for research on non-small cell lung cancer .
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VPC-14228 is an inhibitor that selectively targets androgen receptor DNA binding domain (AR-DBD). VPC-14228 inhibits the interaction between AR and DNA, thereby blocking AR-mediated transcriptional activation. VPC-14228 does not rely on nuclear localization inhibition, but rather inhibits the activity of full-length AR and splice variant AR-V7 by interfering with AR binding to chromatin. And VPC-14228 has high selectivity for other nuclear receptors such as ER and PR. VPC-14228 can be used in the study of prostate cancer [2].
Cat. No.: HY-170935
SRSF1-IN-1 is a SRSF1 inhibitor. SRSF1-IN-1 inhibits SRSF1 expression, thereby modulating the splicing of Bcl-x pre-mRNA. SRSF1-IN-1 inhibits the proliferation of various cancer cells. SRSF1-IN-1 induces apoptosis in gastric cancer cells, reduces Bcl-xl expression, and upregulates cleaved PARP and caspase 3. SRSF1-IN-1 induces autophagy and promotes cell death. SRSF1-IN-1 exhibits anti-tumor activity in a mouse gastric cancer xenograft model. SRSF1-IN-1 can be used for the research of various cancers including liver cancer, gastric cancer, breast cancer, colon cancer, glioma, and melanoma .
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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 .
Cat. No.: HY-147412
CAS No.: 2642382-41-8
Synonyms: QR-421a
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Ultevursen (QR-421a) is a splice-modulating antisense oligonucleotide targeting exon 13 of the USH2A gene, which restores the functional expression of Usherin protein by inducing exon skipping. Ultevursen binds to USH2A pre-mRNA and modulates the splicing process to specifically skip exon 13 carrying the pathogenic mutation c.2299delG, generating an in-frame transcript and a truncated yet functionally normal protein. Ultevursen exhibits concentration-dependent exon skipping activity in human cells and retinal organoid models, and restores Usherin expression and retinal function in zebrafish and gene-edited mouse models. Ultevursen can be used for related research on type 2 Usher syndrome and non-syndromic retinitis pigmentosa .
Cat. No.: HY-P990782
CAS No.: 2566615-11-8
Synonyms: ATYR-1923; KRP-R120
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Cat. No.: HY-169257
CAS No.: 2798856-04-7
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SCR-7952 is an orally active MAT2A allosteric inhibitor (IC50 = 18.7 nM; Ki = 14.49 nM; Kd = 0.56 nM). SCR-7952 reduces SAM production, PRMT5 activity, and SDMA marks by binding to the MAT2A allosteric pocket, and dysregulates RNA splicing through FANCA intron retention, thereby selectively inhibiting the proliferation of MTAP-deleted cancer cells and producing synergistic effects with PRMT5 inhibitors. SCR-7952 can be used for research on MTAP-deleted cancers .
Cat. No.: HY-169794
CAS No.: 37571-96-3
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N-Palmitoyl-phenylalanine is an N-acyl amide that contains the long-chain saturated fatty acid Palmitic acid (HY-N0830) conjugated via an amide bond to the essential amino acid L-Phenylalanine (HY-N0215). N-Palmitoyl-phenylalanine inhibits pre-mRNA splicing in HeLa cell nuclear lysates (IC50 ＞ 400 μM) but has no splicing activity in intact HeLa cells .
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mHTT-IN-2 (compound 27) is a potent inhibitor (EC50=0.066 μM) of mutant huntingtin (mHTT). mHTT-IN-2 reduces canonical splicing of HTT RNA exons [49-50] and is a splicing regulator of the huntingtin (HTT) gene. mHTT-IN-2 exhibits inhibitory activity in vitro and in vivo in human HD stem cells and mouse BACHD models. mHTT-IN-2 may be used in the study of branaplam-related peripheral neuropathy .
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SACLAC, a Ceramide analog, is a potent and covalent acid ceramidase (ASAH1; AC) inhibitor with a Ki of 97.1 nM. SACLAC effectively blocks AC activity and induces a decrease in sphingosine 1-phosphate (S1P) and total ceramide levels. SACLAC reduces the levels of splicing factor SF3B1 and alternative Mcl-1 mRNA splicing, increases pro-apoptotic Mcl-1S levels to induce apoptosis in acute myeloid leukemia (AML) cells. SACLAC reduces the leukemic burden in human AML xenograft mouse models .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
