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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
103 Results for "
phase 1
" in MedChemExpress (MCE) Product Catalog:
Products (103)
103 Results for "phase 1" in MCE Product Catalog:
496
496 Publications Verification
Synonyms: MK-2206 (2HCl)
Target:
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MK-2206 dihydrochloride (MK-2206 2HCl) is an orally active pan-AKT inhibitor, with IC50 values of 8 nM, 12 nM and 65 nM against AKT1, AKT2 and AKT3, respectively. MK-2206 dihydrochloride inhibits the Akt/mTOR signaling pathway and reduces the levels of downstream GSK3β and Mcl-1 via proteasomal degradation. MK-2206 dihydrochloride induces G1-phase cell cycle arrest, apoptosis, epithelial-mesenchymal transition, fibroblast activation and extracellular matrix deposition. MK-2206 dihydrochloride causes transient hyperglycemia and hyperinsulinemia in animals. MK-2206 dihydrochloride can be used in research related to solid tumors, renal fibrosis and hypercholesterolemia .
496
496 Publications Verification
Target:
Research Areas:
MK-2206 is an orally active pan-AKT inhibitor, with IC50 values of 8 nM, 12 nM and 65 nM against AKT1, AKT2 and AKT3, respectively. MK-2206 inhibits the Akt/mTOR signaling pathway and reduces the levels of downstream GSK3β and Mcl-1 via proteasomal degradation. MK-2206 induces G1-phase cell cycle arrest, apoptosis, epithelial-mesenchymal transition, fibroblast activation and extracellular matrix deposition. MK-2206 causes transient hyperglycemia and hyperinsulinemia in animals. MK-2206 can be used in research related to solid tumors, renal fibrosis and hypercholesterolemia .
19
2
2 Cited Publications
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T2AA is a monoubiquitinated proliferating cell nuclear antigen (PCNA) inhibitor that prevents DNA repair, increases double-strand break (DSB) formation and promotes necroptosis and cell cycle arrest in G1 phase .
2
2 Cited Publications
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PCAF-IN-2 (compound 17) is a potent PCAF inhibitor with an IC50 value of 5.31 µM. PCAF-IN-2 shows anti-tumour activity. CAF-IN-2 induces apoptosis and arrest the cell cycle at the G2/M phase .
2
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Phleomycin D1 (PLM D1), a glycopeptide antibiotic, is a member of the Bleomycin/Phleomycin family. Phleomycin D1 causes cell death by binding and cleaving DNA. Phleomycin D1 induces cell cycle arrest at S phase .
1
1 Cited Publications
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CDC25B-IN-1 (compound 4a) is a potent inhibitor of cell division cycle 25B (CDC25B) phosphatase, with a Ki of 8.5 μM. CDC25B-IN-1 potently inhibits cell proliferation and colony formation, causes an increase of the G2/M phase .
1
1 Cited Publications
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AD4 is a PROTAC that induces the degradation of PCLAF by recruiting cereblon. AD4 is also an artemisinin derivative. AD4 directly binds to PCLAF with a KD of 6.1 μM, and induces apoptosis and G1-phase cell cycle arrest. By degrading PCLAF, AD4 upregulates p21, reduces Rb phosphorylation, downregulates Bcl-2 and upregulates Bax, thereby activating the p21/Rb axis. AD4 can be used in studies related to acute B-lymphoblastic leukemia and PCLAF-dependent anticancer mechanisms .
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Acenocoumarol is an anticoagulant that functions as a Vitamin K antagonist. Acenocoumarol inhibits MAPK/ERK/JNK signaling pathway, reduces the nuclear translocation of NF-κB p65, activates Akt/GSK3β signaling pathway. Acenocoumarol induces apoptosis in cell A549, arrests cell cycle at S phase .
Cat. No.: HY-174979
CAS No.: 3084407-00-8
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Dac590 is an orally active and selective obesity-associated protein (FTO) inhibitor with an IC50 of 6.06 nM. Dac590 shows highly selective over ALKBH5 and ALKBH3. Dac590 suppresses oncogenic FTO signaling, induces myeloid differentiation, G1-phase cell cycle arrest, and apoptosis in acute myeloid leukemia (AML) cells. Dac590 inhibits xenograft tumor growth and prolongs survival in acute myeloid leukemia mouse models with no observed toxicity. Dac590 can be used for the research of AML .
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KS100 is a potent ALDH inhibitor with IC50s of 230, 1542, 193 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS100 shows antiproliferative and anticancer effects with low low toxic. KS100 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS10600 induces apoptosis and cell cycle arrest at the G2/M phase .
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Cat. No.: HY-N0475
CAS No.: 74285-86-2
Synonyms: Hypolide; (+)-Triptophenolide
Cat. No.: HY-119487
CAS No.: 1895957-18-2
Research Areas:
Cardiovascular Disease Metabolic Disease Inflammation/Immunology Cancer
MMPP is an orally active inhibitor of STAT3 and VEGFR2, as well as an activator of PPARγ. MMPP blocks the VEGFR2/AKT/ERK/NF-κB signaling pathway to inhibit angiogenesis. MMPP inhibits ferroptosis and inflammation, and alleviates sepsis-induced myocardial injury. MMPP induces G1-phase cell cycle arrest and apoptosis, and inhibits the growth of non-small cell lung cancer (NSCLC) and solid tumors. MMPP promotes adipogenesis and glucose uptake. MMPP can be used in research related to NSCLC, type 2 diabetes and myocardial injury .
Synonyms: CDK4/6-IN-11
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BSJ-02-162 (CDK4/6-IN-11) is a CDK4/CDK6 and IKZF1/IKZF3 degrader, with DC50 values of 32 nM and 6.1 nM against CDK4 and CDK6, respectively; its IC50 ranges from 1 to 50 nM. BSJ-02-162 induces G1-phase cell cycle arrest, reduces phosphorylated retinoblastoma protein levels, and exerts antiproliferative activity in mantle cell lymphoma cells. BSJ-02-162 is applicable to research related to mantle cell lymphoma .
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KS106 is a potent ALDH inhibitor with IC50s of 334, 2137, 360 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS106 shows antiproliferative and anticancer effects with low low toxic.KS106 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS106 induces apoptosis and cell cycle arrest at the G2/M phase .
Cat. No.: HY-168967
BAY-277 is a selective METAP2 degrader and inhibitor. BAY-277 induces ubiquitination and proteasomal degradation of METAP2, triggers G1-phase cell cycle arrest, and inhibits angiogenesis and endothelial cell proliferation. BAY-277 serves as a chemical probe for investigating the biological functions of METAP2. BAY-277 is applicable to cancer-related research.
Cat. No.: HY-163622
CAS No.: 3059565-11-3
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USP10-IN-3 (compound D1) is a potent USP10 inhibitor with an IC50 value of 7.2 µM. USP10-IN-3 inhibits cell proliferation. USP10-IN-3 induces apoptosis and cell cycle arrest at S-phase .
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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
