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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
1197 Results for "
Zanthoxylum armatum DC.
" in MedChemExpress (MCE) Product Catalog:
Products (1197)
1197 Results for "Zanthoxylum armatum DC." in MCE Product Catalog:
Cat. No.: HY-169134
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PROTAC 20S proteasome subunit β5 degrader 1 is a PROTAC degrader targeting the 20S proteasome subunit β5, with a DC50 of 0.11 μM. PROTAC 20S proteasome subunit β5 degrader 1 forms a ternary complex with the CRBN E3 ligase, induces ubiquitination of the 20S proteasome subunit β5, and promotes its degradation via the proteasomal pathway. PROTAC 20S proteasome subunit β5 degrader 1 disrupts cell cycle progression, promotes apoptosis, and inhibits cell proliferation and migration. PROTAC 20S proteasome subunit β5 degrader 1 exhibits significant proliferation-inhibitory activity against various tumor cells, suppresses tumor growth in in vivo xenograft models, and overcomes the resistance of multiple myeloma cells to Bortezomib (HY-10227). PROTAC 20S proteasome subunit β5 degrader 1 can be used in studies related to pharyngeal cancer and drug-resistant multiple myeloma .
Cat. No.: HY-178858
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PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC50 values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces Apoptosis in cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML) .
Cat. No.: HY-187387
CAS No.: 3092711-76-4
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PROTAC HDAC6/ERα degrader 1 is a dual-target PROTAC that targets HDAC6/ERα, with DC50 values of 1.21 μM (HDAC6), 0.28 μM (ERα) in MCF-7 cells and 0.67 μM (HDAC6), 0.14 μM (ERα) in LCC2 cells, respectively. PROTAC HDAC6/ERα degrader 1 selectively degrades ERα and HDAC6 via the proteasomal pathway, inhibits the transcriptional activation of ERα and blocks the estrogen signaling pathway. PROTAC HDAC6/ERα degrader 1 inhibits the function of HDAC6, attenuates hormone responses, and disrupts autophagy-lysosome function. PROTAC HDAC6/ERα degrader 1 induces cell cycle arrest, apoptosis and ferroptosis, and exhibits antiproliferative activity in breast cancer cells. PROTAC HDAC6/ERα degrader 1 can be used for breast cancer research .
Cat. No.: HY-187390
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BRD4 RIMTAC-1 is a BRD4 PROTAC degrader based on the RIPK1-mediated targeted chimera (RIMTAC) technology. It hijacks the endogenous RIPK1-VHL complex via the RIPK1 inhibitor moiety to indirectly recruit the VHL E3 ligase, forming a BRD4-Compound 10-RIPK1-VHL quaternary complex, and degrades BRD4 through the ubiquitin-proteasome system (UPS). BRD4 RIMTAC-1 exhibits selectivity over other BET proteins, induces concentration- and time-dependent, reversible post-translational degradation of BRD4 without altering the target mRNA level. BRD4 RIMTAC-1 potently induces endogenous BRD4 degradation in RAW264.7 and HEK-293T cells, with DC50 values of 179.1 nM and 54.12 nM, respectively. BRD4 RIMTAC-1 can be used for the research of cancer and inflammation-related diseases .
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BD-9136 is a selective BRD4 PROTAC degrader with a DC50 of 1.2 nM, and exhibits a selectivity of ≥1000-fold over BRD2 and BRD3. BD-9136 preferentially forms a ternary complex with the BD1 domain of BRD4, and downregulates the expression of B7-H4 by disrupting the PR-P300-BRD4 axis. BD-9136 depletes BRD4 protein in tumor tissues, inhibits tumor growth, reduces B7-H4 protein expression, increases CD8+ T cell infiltration, and enhances tumor sensitivity to anti-PD-L1. Degradation of BRD4 by BD-9136 rescues the erythroid differentiation block induced by LSD1 inhibition, and transient administration restores erythroid output while retaining HbF induction. BD-9136 causes no adverse effects in mice at effective doses. BD-9136 can be used in studies related to acute myeloid leukemia, acute lymphoblastic leukemia and breast cancer .
Cat. No.: HY-130654
CAS No.: 2597167-24-1
Synonyms: VH032-C2-PEG4-N3
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(S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-C2-PEG4-N3 can be used in the synthesis of vRucaparib-TP4 (HY-130647). vRucaparib-TP4 a highly potent PARP1 degrader with a half-maximal degrading concentration (DC50) of 82 nM . (S,R,S)-AHPC-C2-PEG4-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
Cat. No.: HY-174469
CAS No.: 3070438-79-5
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PROTACs Apoptosis PI3K Akt Bcl-2 Family P-glycoprotein Reactive Oxygen Species (ROS) Na+/K+ ATPase
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PROTAC PI3K/110β degrader-2 is a VHL-recruiting PI3K/110β PROTAC degrader, with DC50 values of 1.258 μM and 2.185 μM in MCF-7/ADM and A549/DDP cells, respectively. PROTAC PI3K/110β degrader-2 induces proteasomal degradation of PI3K/110β, inhibits phosphorylation of AKT and expression of Bcl-2, while suppressing the activity and expression of P-gp. It also induces endoplasmic reticulum stress and mitochondrial apoptosis via the PERK/CHOP pathway. PROTAC PI3K/110β degrader-2 exerts anti-tumor activity against multidrug-resistant cancer cells both in vitro and in vivo, and produces a synergistic effect when combined with Doxorubicin (HY-15142A) or Cisplatin (HY-17394), making it applicable for the research of multidrug-resistant cancers .
Cat. No.: HY-184378
CAS No.: 2922221-22-3
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MDB5 is a Hedgehog pathway and Smoothened inhibitor that binds to the 7-TM domain of Smo . MDB5 reduces hepatic stellate cell activation, extracellular matrix-related gene expression, collagen deposition, hydroxyproline content and epithelial-mesenchymal transition, and prevents sinusoidal endothelial cell capillarization . MDB5 induces G1 and S phase cell cycle arrest, triggers apoptosis by upregulating Bax and downregulating Bcl-2, and also decreases oxygen consumption rate, glucose uptake, transglutaminase activity and fibronectin matrix assembly . MDB5 reduces the levels of liver injury markers, hepatic triglyceride deposition and hepatic steatosis, restores the tissue structure of the kidney and spleen, and inhibits pancreatic tumor growth without causing body weight loss . MDB5 can be loaded into PEG-PCC-g-DC micelles, achieving high drug loading, sustained release, improved water solubility, enhanced cellular uptake and optimized hepatic distribution, with good tolerance in mice . MDB5 is applicable to research related to alcohol-associated liver disease, liver fibrosis and pancreatic cancer .
Cat. No.: HY-111997R
CAS No.: 1799506-07-2
Synonyms: HaloPROTAC 3 (Standard)
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VH285-PEG4-C4-Cl (Standard) is the analytical standard of VH285-PEG4-C4-Cl (HY-111997). This product is intended for research and analytical applications. VH285-PEG4-C4-Cl (HaloPROTAC 3) is a conjugate of ligands for E3 and 16-atom-length linker. The connector of linker is Halogen group. VH285-PEG4-C4-Cl incorporates the VH285 based VHL ligand and an alkyl/ether-based linker. VH285-PEG4-C4-Cl is a highly potent and efficacious degrader of GFP-HaloTag7 with a DC50 of 19 nM. VH285-PEG4-C4-Cl is able to induce 90 % degradation of GFP-Halotag at 625 nM. VH285-PEG4-C4-Cl binds to VHL with an IC50 of 0.54 μM .
Cat. No.: HY-170820
CAS No.: 3006788-11-7
Target:
Molecular Glues Eukaryotic Release Factor (eRF) Bcl-2 Family CDK EGFR HSP Androgen Receptor c-Myc
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XYD049 is a CRBN-based molecular glue degrader targeting GSPT1, with a DC50 of 19 nM. XYD049 mediates the formation of a ternary complex between CRBN and GSPT1, thereby triggering CRBN- and proteasome-dependent degradation of GSPT1. By degrading GSPT1, XYD049 downregulates castration-resistant prostate cancer (CRPC)-related oncogenes, including BCL2, CDK2, E2F3, EGFR, HSP90B1, TMPRSS2, AR, AR-V7, PSA and c-Myc. XYD049 inhibits cancer cell growth and suppresses tumor growth in mice. XYD049 can be used for research on castration-resistant prostate cancer. XYD049 consists of a linker (black part) NH2-C5-NH-Boc (HY-W004710), a CRBN-based E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a target protein ligand (red part) GSPT1 ligand-1 (HY-170821), among which the E3 ligase ligand plus linker forms the conjugate E3 Ligase Ligand-linker Conjugate 158 (HY-170822) .
Cat. No.: HY-174379
NTLiverTac PDE6D degrader-1 is a PDE6D NTLiverTac degrader with a DC50 of 4.09 μM. NTLiverTac PDE6D degrader-1 is formed by conjugating a PDE6D PROTAC degrader with the NTCP ligand Cholic acid (HY-N0324). NTLiverTac PDE6D degrader-1 triggers the ubiquitin-proteasome system-mediated degradation process by forming a complex with PDE6D and MDM2, inducing proteasome-dependent and NTCP-dependent degradation. NTLiverTac PDE6D degrader-1 inhibits PDE6D-dependent KRAS trafficking and suppresses KRAS-related oncogenic signaling cascades. NTLiverTac PDE6D degrader-1 inhibits the activation of the PI3K/AKT/mTOR signaling pathway and induces cellular Apoptosis. NTLiverTac PDE6D degrader-1 enters cancer cells via NTCP-mediated endocytosis. NTLiverTac PDE6D degrader-1 can be used in the research of hepatoblastoma (MDM2 ligand: (4R,5S)-Nutlin carboxylic acid (HY-128836); NTCP ligand: Cholic acid (HY-N0324); PDE6D ligand: Sorafenib (HY-10201)) .
Cat. No.: HY-176421
CAS No.: 3070438-85-3
Target:
PROTACs PI3K Apoptosis Akt Bcl-2 Family Caspase P-glycoprotein
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PROTAC PI3K/110β degrader-1 is a VHL-recruiting PROTAC degrader targeting PI3K/110β, with DC50 values of 0.416 μM (MCF-7) and 19.66 μM (A549), respectively. PROTAC PI3K/110β degrader-1 recruits VHL to induce proteasomal degradation of PI3K/110β. It activates endoplasmic reticulum stress (ERS)-mediated mitochondrial apoptosis via the PERK/ATF4/CHOP unfolded protein response (UPR) pathway, downregulates p-AKT and Bcl-2, upregulates Bax, cleaved-caspase-9 and cleaved-caspase-3, inhibits the expression and activity of P-gp, and exerts synergistic anti-tumor effects with Doxorubicin (Adriamycin, ADM) (HY-15142A) and Cisplatin (DDP) (HY-17394). PROTAC PI3K/110β degrader-1 can be used in research related to multidrug-resistant cancers .
Cat. No.: HY-P81311
Synonyms: C21; DC42; F box like/WD repeat containing protein TBL1XR1; F-box-like/WD repeat-containing protein TBL1XR1; FLJ12894; IRA1; Nuclear receptor corepressor/HDAC3 complex subunit; Nuclear receptor corepressor/HDAC3 complex subunit TBLR1; TBL1 related protein 1; TBL1-related protein 1; TBL1R_HUMAN; TBL1XR1; Transducin (beta) like 1 X linked receptor 1; Transducin beta like 1X related protein 1; Transducin beta-like 1X-related protein 1.
Cat. No.: HY-P81311A
Synonyms: C21; DC42; F box like/WD repeat containing protein TBL1XR1; F-box-like/WD repeat-containing protein TBL1XR1; FLJ12894; IRA1; Nuclear receptor corepressor/HDAC3 complex subunit; Nuclear receptor corepressor/HDAC3 complex subunit TBLR1; TBL1 related protein 1; TBL1-related protein 1; TBL1R_HUMAN; TBL1XR1; Transducin (beta) like 1 X linked receptor 1; Transducin beta like 1X related protein 1; Transducin beta-like 1X-related protein 1.
Cat. No.: HY-P81339
Synonyms: C21; DC42; F box like/WD repeat containing protein TBL1XR1; F-box-like/WD repeat-containing protein TBL1XR1; FLJ12894; IRA1; Nuclear receptor corepressor/HDAC3 complex subunit; Nuclear receptor corepressor/HDAC3 complex subunit TBLR1; TBL1 related protein 1; TBL1-related protein 1; TBL1R_HUMAN; TBL1XR1; Transducin (beta) like 1 X linked receptor 1; Transducin beta like 1X related protein 1; Transducin beta-like 1X-related protein 1.
Cat. No.: HY-P85510
Synonyms: C21; DC42; F box like/WD repeat containing protein TBL1XR1; F-box-like/WD repeat-containing protein TBL1XR1; FLJ12894; IRA1; Nuclear receptor corepressor/HDAC3 complex subunit; Nuclear receptor corepressor/HDAC3 complex subunit TBLR1; TBL1 related protein 1; TBL1-related protein 1; TBL1R_HUMAN; TBL1XR1; Transducin; beta; like 1 X linked receptor 1; Transducin beta like 1X related protein 1; Transducin beta-like 1X-related protein 1.
Cat. No.: HY-P81339A
Synonyms: C21; DC42; F box like/WD repeat containing protein TBL1XR1; F-box-like/WD repeat-containing protein TBL1XR1; FLJ12894; IRA1; Nuclear receptor corepressor/HDAC3 complex subunit; Nuclear receptor corepressor/HDAC3 complex subunit TBLR1; TBL1 related protein 1; TBL1-related protein 1; TBL1R_HUMAN; TBL1XR1; Transducin (beta) like 1 X linked receptor 1; Transducin beta like 1X related protein 1; Transducin beta-like 1X-related protein 1.
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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
