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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
746 Results for "
Mutation
" in MedChemExpress (MCE) Product Catalog:
Products (746)
746 Results for "Mutation" in MCE Product Catalog:
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FRM-024 is a central nervous system-penetrant, orally active γ-secretase modulator and Aβ42 lowering agent. FRM-024 is used for the research of familial Alzheimer's disease .
Cat. No.: HY-187793
CAS No.: 2412854-49-8
Synonyms: ABSK061
Lavengratinib (ABSK061) is a FGFR2/FGFR3 inhibitor. Lavengratinib selectively inhibits FGFR2 and FGFR3 signaling pathways and reduces the risk of FGFR1-mediated hyperphosphatemia. Lavengratinib is suitable for research on advanced solid tumors (including cholangiocarcinoma, gastric cancer, non-small cell lung cancer, cervical cancer and urothelial cancer) .
Cat. No.: HY-W012248
CAS No.: 349-58-6
KG-655 is a ligand that specifically binds to the ARNT PAS-B domain. KG-655 binds to the internal cavity of ARNT PAS-B to restrict its variable folded conformation, disrupts the interaction between ARNT PAS-B and the transcriptional coactivator TACC3, and promotes the homodimerization of ARNT PAS-B. KG-655 is widely applicable to cancer-related research .
Cat. No.: HY-141876
CAS No.: 2278356-90-2
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PRT543 is an orally active selective PRMT5 inhibitor. PRT543 reduces intracellular symmetric dimethylarginine (sDMA) levels, downregulates the expression of genes related to DNA damage repair and DNA replication pathways, and induces abnormal alternative splicing. PRT543 inhibits the MYB, NOTCH1 and PI3K/AKT signaling pathways, promotes nuclear translocation of FOXO1, upregulates the pro-apoptotic protein BAX, and enhances cellular sensitivity to BCL-2 inhibition. PRT543 disrupts the normal RNA splicing process and exerts a synthetic lethal effect on myeloid tumor cells carrying splicing factor mutations. PRT543 can be used in research related to various cancers including breast cancer, ovarian cancer and acute myeloid leukemia .
Cat. No.: HY-145737A
Purity: 99.38%
PROTAC SOS1 degrader-1 TFA is a degrader of SOS1 PROTAC, with a DC50 of 98.4 nM and a Kd value of 44 nM. PROTAC SOS1 degrader-1 TFA induces the formation of a ternary complex with SOS1 and the VCB E3 ubiquitin ligase complex, thereby promoting the ubiquitination and proteasomal degradation of SOS1. PROTAC SOS1 degrader-1 TFA reduces KRAS-GTP levels, inhibits the phosphorylation of ERK in the RAS-RAF-MEK-ERK pathway, and suppresses the proliferation of cancer cells carrying KRAS mutations. PROTAC SOS1 degrader-1 TFA inhibits tumor growth in mouse xenograft models. PROTAC SOS1 degrader-1 TFA can be used for the research of KRAS-driven cancers .
Cat. No.: HY-147412D
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FAM labled Ultevursen sodiumis a FAM labled Ultevursen sodium (HY-147412A). Ultevursen sodium (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 sodium 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 sodium 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 sodium can be used for related research on type 2 Usher syndrome and non-syndromic retinitis pigmentosa .
Cat. No.: HY-147412E
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Cy3 labled Ultevursen sodium is a Cy3 labled Ultevursen sodium (HY-147412A). Ultevursen sodium (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 sodium 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 sodium 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 sodium can be used for related research on type 2 Usher syndrome and non-syndromic retinitis pigmentosa .
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GBD-9 is a degrader based on the E3 ubiquitin ligase CRBN that targets BTK and the G1 to S phase transition protein GSPT1. GBD-9 has both PROTAC and molecular glue properties by inducing ubiquitination and proteasomal degradation of target proteins. GBD-9 can efficiently degrade wild-type and mutant BTK (such as C481S mutation) and GSPT1. GBD-9 significantly inhibits tumor cell proliferation by inducing G1 phase arrest in cancer cells, downregulating anti-apoptotic proteins (BCL-2, MCL-1) and activating Caspase-3 to induce apoptosis. GBD-9 is mainly used in the research of hematological tumors such as diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML) .
Cat. No.: HY-156794A
Synonyms: DSP-5336 enantiomer
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Enzomenib enantiomer (DSP-5336 enantiomer) is an enantiomer of Enzomenib (HY-156794). Enzomenib (DSP-5336) is an orally active Menin inhibitor (IC50=1.4 nM, Kd=6.0 nM). Enzomenib disrupts the interaction between Menin and KMT2A/MLL fusion proteins, specifically inhibits the expression of leukemia driver genes such as HOX/MEIS1, and upregulates ITGAM. Enzomenib effectively induces cell differentiation, inhibits tumor cell proliferation, and suppresses primitive cell colony formation. Enzomenib reduces disease burden and prolongs survival, but causes adverse reactions including differentiation syndrome and QTc interval prolongation. Enzomenib is used for research on relapsed/refractory acute myeloid leukemia, acute lymphoblastic leukemia, and other hematologic malignancies with mixed lineage leukemia (MLL) rearrangements or NPM1 mutations .
Cat. No.: HY-169481
CAS No.: 3027918-96-0
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AP-1 is a targeted ALK PROTAC degrader. AP-1 effectively degrades various ALK fusion/mutation forms, including degradation of NPM-ALK (DC50 = 4.6 nM) and EML4-ALK (DC50 = 357.6 nM), and exhibits a typical hook effect at high concentrations. AP-1 inhibits phosphorylation of downstream STAT3, downregulates gene expression in the JAK-STAT pathway, and kills ALK-positive tumor cells via activating the caspase-3-dependent apoptosis pathway. AP-1 shows cytotoxicity against a variety of cancer cells and possesses anti-tumor activity. AP-1 can be used in research related to non-small cell lung cancer, neuroblastoma, and anaplastic large cell lymphoma .
Cat. No.: HY-175320
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PROTAC c-Met degrader-5 is an orally active c-Met PROTAC degrader. PROTAC c-Met degrader-5 induces c-Met degradation via Cullin-CRBN, with a DC50 value of 0.32 nM, and inhibits the phosphorylation of c-Met and its downstream signaling molecule STAT3. PROTAC c-Met degrader-5 inhibits cancer cell proliferation, migration and invasion, induces apoptosis, alters cell cycle distribution, and suppresses the growth of EBC-1 xenograft tumors. PROTAC c-Met degrader-5 can be used to study MET-driven cancers as well as Tepotinib (HY-14721)-resistant cancers harboring c-Met D1228N and c-Met Y1230H mutations .
Cat. No.: HY-184264
CAS No.: 1309199-94-7
CHVB-066 is an alphavirus non-structural protein nsP1 inhibitor that exhibits varying degrees of inhibitory activity against nsP1 of CHIKV and VEEV. CHVB-066 inhibits MTase and GTase activities and disrupts the capping process of viral RNA, including inhibiting CHIKV replication, reducing progeny viruses, and preventing cytopathic effects. It shows varying degrees of inhibitory activity against nsP1 of CHIKV and VEEV but lacks anti-SFV replication activity, displays cross-resistance with MADTP series compounds, and requires nsP2/nsP3 mutations to develop complete drug resistance. This inhibitor with varying inhibitory activity against nsP1 of CHIKV and VEEV can be widely applied to relevant studies on chikungunya virus infection and chikungunya fever .
Cat. No.: HY-185899
CAS No.: 72052-96-1
Synonyms: 5-Aza-2'-deoxycytidine-5′-triphosphate
5-Aza-dCTP (5-Aza-2'-deoxycytidine-5′-triphosphate) is a nucleotide analog that acts as a substrate for mammalian DNA polymerase α (Km = 3.0 μM) and a weak competitive inhibitor of this enzyme (Ki = 4.3 μM). 5-Aza-dCTP inhibits DNA polymerase α via incorporation into DNA through Watson-Crick base pairing, inhibits DNA methyltransferases via incorporation into hemimethylated DNA, and induces mutations in HIV-1 via incorporation into viral DNA during synthesis. 5-Aza-dCTP reverses the inhibitory effect of dTTP on dCMP deaminase, and allosterically activates dCMP deamination to the same extent as dCTP. 5-Aza-dCTP is applicable to research related to leukemia and type 1 human immunodeficiency virus infection .
Cat. No.: HY-P992482
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Oxiran-2-ylmethanol (Standard) is the analytical standard of Oxiran-2-ylmethanol (Glycidol) (HY-Y1010). This product is intended for research and analytical applications. Oxiran-2-ylmethanol is an ester product. Oxiran-2-ylmethanol induces base pair point mutations in bacterial strains and structural chromosome aberrations in cultured cells. Oxiran-2-ylmethanol forms N-(2,3-dihydroxypropyl)valine hemoglobin adducts. Oxiran-2-ylmethanol acts as an animal carcinogen but does not significantly induce micronucleated immature erythrocytes in animal bone marrow. Oxiran-2-ylmethanol enables anionic polymerization to produce linear poly(glycidol). Oxiran-2-ylmethanol can be used for cancer-related research .
Cat. No.: HY-Y1010S
CAS No.: 1246819-20-4
Synonyms: Glycidol-d5
Cat. No.: HY-161796
CAS No.: 2929304-05-0
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UNC8732 is an NSD2 degrader with a Kd value of 76 nM for NSD2, and achieves highly selective degradation of NSD2 across the detectable proteome. UNC8732 acts as a prodrug; its primary amine is metabolized to an aldehyde, which forms a reversible covalent interaction with Cys326 in the FIST_C domain of FBXO22, recruiting the SCFFBXO22 ubiquitin ligase complex to mediate polyubiquitination and proteasomal degradation of NSD2. UNC8732 serves as a chemical probe to investigate NSD2-associated disease phenotypes and study the functions of NSD2 in nuclear signaling and epigenetics. UNC8732 can be used in studies of acute lymphoblastic leukemia .
Cat. No.: HY-164717
CAS No.: 2922789-15-7
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FORX-428 is an orally active, selective poly (ADP-ribose) glycohydrolase (PARG) inhibitor. FORX-428 reversibly inhibits PARG, thereby blocking PAR chain dissociation, inhibiting DNA repair, inducing tumor cell death, and targeting replication stress in cancer cells. FORX-428 can be used in the research of ovarian cancer and triple-negative breast cancer .
Cat. No.: HY-180485
PROTAC D16-M1P2 is an orally active CRBN-mediated selective PKMYT1 PROTAC degrader, with a DC50 of 0.7 nM in CCNE1-amplified HCC1569 breast cancer cells. PROTAC D16-M1P2 induces PKMYT1 degradation via the ubiquitin-proteasome system, directly inhibits PKMYT1 kinase activity, suppresses Thr14 phosphorylation of CDK1, and depends on functional CRBN and ubiquitination-like modification processes. PROTAC D16-M1P2 can be used for the research of CCNE1-amplified breast cancer, FBXW7-mutated cholangiocarcinoma, and PPP2R1A-deficient cancers .
Cat. No.: HY-179562
CAS No.: 2649400-05-3
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BTK degrader-2 (Example 2) is a dual-functional BTK molecular glue degrader, which causes the degradation of BTK through the ubiquitin-proteasome pathway. BTK degrader-2 can be used for the study of B-cell-related diseases .
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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
