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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
604 Results for "
SCO2 mutations
" in MedChemExpress (MCE) Product Catalog:
Products (604)
604 Results for "SCO2 mutations" in MCE Product Catalog:
Cat. No.: HY-187520
CAS No.: 3137385-11-3
KRAS-IN-62 is an orally effective pan-KRAS inhibitor that potently inhibits SOS1-mediated KRAS nucleotide exchange (IC50 < 10 nM for KRAS G12D/G12V/G12C/WT). KRAS-IN-62 inhibits pERK signaling and cell proliferation in KRAS-mutant tumor cells (pERK IC90 = 0.51 nM in GP2D cells). KRAS-IN-62 inhibits tumor growth in vivo, with plasma concentrations exceeding IC50 for ~20 h after oral administration in beagle dogs. KRAS-IN-62 can be used in studies of KRAS mutation-related cancers, such as colorectal cancer .
Cat. No.: HY-189880
PI3Kα-IN-36 is a selective and orally active PI3Kα H1047R inhibitor with a pAKT inhibition IC50 of 96 nM in T47D cells. PI3Kα-IN-36 selectively inhibits T47D cell proliferation with an IC50 of 65 nM. PI3Kα-IN-36 achieves 81% tumor growth inhibition in a T47D xenograft mouse model. PI3Kα-IN-36 can be used in research related to PI3Kα H1047R mutation-driven tumors .
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Dihydralazine sulfate (Standard) is the analytical standard of Dihydralazine sulfate (HY-N7065). This product is intended for research and analytical applications. Dihydralazine sulfate is an antihypertensive hydrazine derivative and also a low-potency genotoxic agent. Dihydralazine sulfate is a direct-acting mutagen with a mixed gene mutation mechanism, which induces DNA fragmentation in the lung, kidney and spleen of mice, and induces sister chromatid exchange in mouse bone marrow cells. Dihydralazine sulfate specifically kills DNA repair-deficient bacteria. Dihydralazine sulfate is a vasodilator and antihypertensive agent that reduces systemic vascular resistance, increases cardiac output and heart rate, thereby lowering blood pressure. Dihydralazine sulfate can be used in research related to hypertension and severe early-onset preeclampsia [2].
Cat. No.: HY-P2307
CAS No.: 847829-41-8
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Cat. No.: HY-P2307A
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Cat. No.: HY-P991223
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Cat. No.: HY-P991267A
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CAN10 (LALA) is is a humanized monoclonal antibody inhibitor targeting interleukin 1RAP (IL1RAP). CAN10 (LALA) blocks IL-1, IL-33, and IL-36 signalling by targeting IL1RAP, preventing downstream proinflammatory and profibrotic responses. The Fc region of CAN10 (LALA) incorporates the L234A and L235A mutations, which are designed to reduce the binding of the antibody to FcγRs and C1q, thereby attenuating or eliminating the antibody’s ADCC (antibody-dependent cell-mediated cytotoxicity) and CDC (complement-dependent cytotoxicity) effector functions. CAN10 (LALA) reduces dermal and pulmonary fibrosis. CAN10 (LALA) can be used for the research of immune system diseases, such as systemic sclerosis .
Cat. No.: HY-P992546
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IBI323 is a PD-L1/LAG-3 dual inhibitory antibody with Kd values of 0.0132 nM and 0.671 nM, respectively. IBI323 blocks the interaction of PD-L1 with PD-1 and CD80, as well as the interaction of LAG-3 with MHC-II. IBI323 mediates cross-linking of PD-L1-positive and LAG-3-positive cells, enhances T cell activation and cytokine secretion, and increases tumor-specific T cells in tumors and blood. IBI323 has a LALA mutation that reduces Fc-mediated effector function and inhibits tumor growth in humanized mouse models. IBI323 can be used for research on melanoma and colon cancer .
Cat. No.: HY-128866
CAS No.: 2332841-25-3
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TBAJ-876 is an orally active diarylquinoline antimycobacterial agent. TBAJ-876 targets the c and ε subunits of Mycobacterium tuberculosis F-ATP synthase to modulate energy metabolism, and it exerts bactericidal activity against replicating Mycobacterium tuberculosis and retains activity against strains carrying Rv0678 mutations. TBAJ-876 undergoes N-demethylation in vivo to form the major active metabolite TBAJ-876-M3, which has lower lipophilicity and lower binding affinity for the hERG potassium channel. TBAJ-876 is well tolerated in BALB/c mice and significantly reduces the number of colony-forming units of Mycobacterium tuberculosis in the lungs. TBAJ-876 can be used in research related to tuberculosis and Mycobacterium abscessus lung disease [2].
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 [2] .
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 [2].
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 [2].
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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) [2] .
Os30, a potent fourth-generation EGFR inhibitor, is a potent EGFRC797S-TK inhibitor with IC50 values of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively. Os30 can suppress EGFR phosphorylation, arrest at G1 phase and induce the apoptosis of KC-0116 (BaF3-EGFRDel19/T790M/C797S) cells. Os30 shows potent antitumor efficacy on non-small cell lung cancer (NSCLC) with EGFmRC797S mutation .
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 [2] .
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 [2] .
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 [2] .
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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
