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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
58 Results for "
integrated provirus
" in MedChemExpress (MCE) Product Catalog:
Products (58)
58 Results for "integrated provirus" in MCE Product Catalog:
40
40 Publications Verification
7
Research Areas:
Eragidomide (CC-90009) is a GSPT1 Molecular Glue degrader. Eragidomide exhibits antiproliferative and pro-apoptotic (apoptosis) activities against acute myeloid leukemia cells. Eragidomide recruits the CRL4CRBN E3 ubiquitin ligase complex to selectively target GSPT1 for ubiquitination and proteasomal degradation. Eragidomide reduces leukemia cell engraftment and eliminates leukemia stem cells. Eragidomide promotes the activation of the GCN1/GCN2/ATF4 pathway and the integrated stress response pathway, inhibits global protein translation, promotes preferential translation of ATF4, and induces the accumulation of ATF4, CHOP and ATF3. The response to Eragidomide is regulated by the ILF2/ILF3 heterodimer complex, the mTOR signaling pathway and the integrated stress response. Eragidomide can be used in research related to acute myeloid leukemia and relapsed/refractory acute myeloid leukemia .
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5 Cited Publications
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2BAct is a highly selective, orally active, and CNS-penetrant eIF2B (eukaryotic initiation factor 2B) activator with an EC50 of 33 nM. 2BAct prevents neurological defects caused by a chronic integrated stress response. 2BAct displays improved solubility and pharmacokinetics relative to eIF2B activator ISRIB trans-isomer (HY-12495) .
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1 Cited Publications
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SJ6986 is an orally active GSPT1/2 molecular glue degrader, with a DC50 of 9.7 nM at 4 h and 2.1 nM at 24 h for GSPT1 degradation in MV4-11 cells. SJ6986 recruits GSPT1/2 to the CRBN E3 ligase complex, inducing ubiquitination and proteasomal degradation of GSPT1/2. SJ6986 triggers activation of the integrated stress response pathway and apoptosis downstream of GSPT1 degradation. SJ6986 serves as a chemical probe for investigating the functions of GSPT1/GSPT2 in vitro and in vivo. SJ6986 can be used for research on acute leukemia and medulloblastoma .
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CMP-SiaNAz (CMP-NeuNAz) sodium is a sialic acid nucleotide sugar derivative. CMP-SiaNAz sodium is integrated into the glycosidic chain through the action of STs in the Golgi apparatus, forming SiaNAz substances. CMP-SiaNAz sodium can serve as a substrate for bacterial-derived sialic acid transferases and is used for chemical enzymatic labeling and imaging of cell surface glycosides .
Cat. No.: HY-160196
CAS No.: 2803470-63-3
Synonyms: GCN2 modulator-1
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HC-7366 (GCN2 modulator-1) is an orally effective GCN2 activator. HC-7366 can effectively compete and occupy the ATP binding pocket of GCN2, with its IC50 being 72 nM. This binding triggers the conformational activation of GCN2, leading to the upregulation of downstream signals (such as ATF4, ASNS) in the integrated stress response (ISR) pathway, ultimately exerting anti-tumor effects. HC-7366 also has inhibitory activity against ZAK, with its IC50 being 47 nM. HC-7366 can be used for research on fibrosarcoma and acute myeloid leukemia .
Cat. No.: HY-D2919
CAS No.: 2177287-88-4
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DNL343 is a potent, selective, orally active and brain-penetrant activator of eukaryotic initiation factor eIF2B. DNL343 inhibits the activity of the integrated stress response (ISR) in the central nervous system (CNS) and reverses neurodegeneration and neuroinflammation. DNL343 also prevents motor dysfunction and premature death in eIF2B loss-of-function (LOF) mutant mice. DNL343 can be used in the study of neurodegenerative diseases .
Cat. No.: HY-W039953
CAS No.: 98924-81-3
Synonyms: N-azidoacetylglucosamine-tetraacylated
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Ac4GlcNAz (N-azidoacetylglucosamine-tetraacylated) is an azido-containing fully acetylated N-acetylglucosamine analog, a metabolic glycan marker, and also an inducer of S-glycosylation. Ac4GlcNAz can be taken up by bacteria, processed via endogenous carbohydrate biosynthesis pathways, and integrated into glycans by replacing natural monosaccharides. Under alkali promotion, Ac4GlcNAz undergoes β-elimination to form α,β-unsaturated aldehydes, which then bind to cysteine residues via Michael addition. Ac4GlcNAz can be integrated into glycoproteins. Ac4GlcNAz is applicable to research related to Helicobacter pylori infection .
Cat. No.: HY-153399A
CAS No.: 2945073-88-9
Synonyms: ABBV-CLS-7262 THAM sodium
Research Areas:
Fosigotifator (ABBV-CLS-7262) THAM sodium is a brain penetrant, orally active EIF2b (eukaryotic initiation factor) activator. Fosigotifator THAM sodium stabilizes the elF2B complex and boosts the activity, including that of complexes carrying pathogenic vanishing white matter (VWM) mutations. Fosigotifator THAM sodium is an integrated stress response inhibitor (ISRI). Fosigotifator THAM sodium can be used for amyotrophic lateral sclerosis research .
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HR-19011 is an eIF2α phosphorylation activator targeting heme-regulated inhibitor HRI (EIF2AK1). HR-19011 exhibits growth inhibitory activity against K562 cells with an IC50 value of 3.91 µM. HR-19011 inhibits the growth of hematologic malignancies by targeting HRI to activate the integrated stress response via the HRI-eIF2α-ATF4 axis. HR-19011 shows good safety in vivo. HR-19011 can be used for research on hematologic malignancies (leukemia) .
Cat. No.: HY-172815
CAS No.: 3079913-81-5
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IDB-001 is a human ribosomal peptidyl transferase center (PTC) inhibitor that induces conformational changes and blocks translational elongation in specific sequence contexts through complementary interactions with Asp/Glu residues in nascent polypeptides. IDB-001 preferentially stalls ribosomes at positions containing acidic peptide motifs, thereby inhibiting cancer cell proliferation, and activates the integrated stress response via eIF2α phosphorylation at high concentrations. In addition, IDB-001 mildly triggers ribotoxic stress responses through phosphorylation of JNK and p38. IDB-001 has been applied to mechanistic studies of triple-negative breast cancer .
Cat. No.: HY-148837
CAS No.: 2883535-99-5
Target:
PROTACs c-Myc CD276/B7-H3 IAP Casein Kinase Eukaryotic Release Factor (eRF) Oxidative Phosphorylation Apoptosis
Research Areas:
GT19630 is an orally active c-Myc PROTAC targeted degrader based on the cereblon E3 ubiquitin ligase, with an IC50 of 1.5 nM against human c-Myc. GT19630 mediates the degradation of MYC, GSPT1, GSPT2, CK1 alpha, N-Myc, B7-H3 and XIAP, and disrupts the MYC-GSPT1 synergistic regulatory feedback loop. GT19630 inhibits cell proliferation, blocks S-phase progression of the cell cycle, promotes cell apoptosis, reduces cell migration capacity, induces integrated stress response, and blocks oxidative phosphorylation by inhibiting the TCA cycle. GT19630 can be used in the research of Myc-driven hematological cancers, small cell lung cancer, breast cancer, TP53-mutant cancers, and venetoclax-resistant cancers .
Cat. No.: HY-130514
CAS No.: 327081-00-5
SMAPP1 is an activator of protein phosphatase-1 (PP1). SMAPP1 increases phosphorylation of CDK9’s Ser90 and Thr186 residues, but not Ser175. SMAPP1 induces HIV-1 replication, upregulates HIV-1 transcription that led to the reactivation of latent HIV-1 provirus .
Synonyms: PEG-L-asparaginase; Pegasparaginase
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Oncaspar (PEG-L-asparaginase; Pegasparaginase), a pegylated form of native Escherichia coli-derived L-asparaginase, breaks down the amino acid asparagine that are circulating in the bloodstream. Oncaspar plays an important role in acute lymphoblastic leukemia (ALL) through asparagine hydrolysis and activation of the integrated stress response (ISR) pathway .
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BAMEAO16B is a lipid nanoparticle. BAMEAO16B integrated with disulfide bonds, can efficiently deliver Cas9 mRNA and sgRNA into cells while releasing RNA in response to the reductive intracellular environment for genome editing. BAMEAO16B can be used for the research of gene editing .
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ISR-IN-1 is an integrated stress response (ISR) inhibitor targeting eIF2B. ISR-IN-1 enhances eIF2B guanine nucleotide exchange factor activity, stabilizes eIF2B heteropentamer dimers via symmetrical protein-protein interface binding, and releases global protein synthesis inhibition from phosphorylated eIF2α α. ISR-IN-1 can be used for the research of prion disease .
Cat. No.: HY-W319647
CAS No.: 315705-10-3
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GCN2 activator-1 (Compound 20) is a GCN2 activator. GCN2 activator-1 binds within the ATP-pocket of GCN2 and activates GCN2 in a GCN1-independent manner. GCN2 activator-1 activates Integrated Stress Response (ISR) in cells. GCN2 activator-1 inhibits PKR with an IC50 of 3.75 µM. GCN2 activator-1 can be used for research of pulmonary veno-occlusive disease (PVOD) .
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E235 is an expression regulator of activates transcription factor 4 (ATF4). E235 reduces cell viability by activating integrated stress response (ISR) and DNA damage response signals. E235 has anti-proliferative activity and can be used for tumor research .
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ISR-IN-2 (Compound 47) is an inhibitor of the integrated stress response (EC50: 0.8 nM) .
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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
