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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
36 Results for "
no obvious cytotoxicity
" in MedChemExpress (MCE) Product Catalog:
Products (36)
36 Results for "no obvious cytotoxicity" in MCE Product Catalog:
10
10 Publications Verification
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TAS4464 is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 has a wide selcetive window, without obvious toxicity. TAS4464 can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
10
10 Publications Verification
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LDC1267 is a AXL/TAM/FLT3 inhibitor with IC50 values of 42 nM, 130 nM, and 63 nM against AXL, MERTK, and TYRO3, respectively. LDC1267 blocks GAS6-induced AXL phosphorylation and the downstream AKT/ERK1/2 signaling pathway. LDC1267 inhibits cancer cell proliferation, colony formation, and glioblastoma cell invasion, without causing obvious impairment of cytotoxic autophagic flux. LDC1267 exerts a synergistic effect when used in combination with Imatinib (HY-15463) in chronic myeloid leukemia models. LDC1267 can be widely applied in studies related to glioblastoma and chronic myeloid leukemia .
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10 Publications Verification
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TAS4464 hydrochloride is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 hydrochloride against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 hydrochloride targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 hydrochloride exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 hydrochloride has a wide therapeutic window, without obvious toxicity. TAS4464 hydrochloride can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
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PKR-IN-C51 is an ATP-competitive protein kinase R (PKR) inhibitor with a human IC50 of 9 μM and a human Ki of 3.4 μM. PKR-IN-C51 blocks the activation of PKR, inhibits intracellular PKR activation in primary mouse macrophages, and shows no obvious cytotoxicity. PKR-IN-C51 can be used in studies related to the regulation of PKR-mediated signaling pathways .
Cat. No.: HY-162562
CAS No.: 930017-01-9
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E28362 is an orally active lipid-lowering agent and a selective PCSK9 antagonist. E28362 blocks the interaction between PCSK9 and LDLR, and induces PCSK9 degradation via the ubiquitin-proteasome pathway. E28362 significantly increases the levels of cell surface and total LDLR proteins, enhances low-density lipoprotein uptake, thereby effectively reducing plasma lipids, hepatic cholesterol and triglyceride levels. E28362 shows no obvious cytotoxicity at high concentrations, and significantly attenuates atherosclerotic lesions in animal models. E28362 is an important molecule in research of hyperlipidemia and atherosclerosis .
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HIF-IN-1 (Compound 3c) is a hypoxia-inducible factor (HIF)-1 inhibitor. HIF-IN-1 suppresses HIF-1α protein accumulation without affecting the levels of HIF-1α mRNA. HIF-IN-1 shows no obvious cytotoxicity .
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GPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, IC50 is 0.680 μM. GPR34 receptor antagonist 3 inhibited ERK1/2 phosphorylation induced by lysophosphatidylserine in a dose-dependent way without obvious cytotoxicity. GPR34 receptor antagonist 3 shows antisensory activity in mouse neuropathic pain model .
Cat. No.: HY-136797
CAS No.: 1622060-51-8
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BP13944 is a potential small molecule inhibitor discovered by high-throughput screening. It can effectively inhibit the expression of dengue virus (DENV) replicons with an EC50 value of 1.03±0.09 μM. BP13944 can inhibit the replication or viral RNA synthesis of all four serotypes of DENV, but is ineffective against Japanese encephalitis virus. BP13944 may target the DENV NS3 protease, and the E66G amino acid substitution in the NS3 protease region will cause the virus to become resistant to BP13944. BP13944 has no obvious cytotoxicity. As there is currently no effective dengue vaccine and treatment, BP13944, as an effective small molecule inhibitor, may become a potential agent for the treatment of dengue in the future.
Cat. No.: HY-156240
CAS No.: 2247060-97-3
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DI-1548 is a potent, selective, and irreversible covalent inhibitor of DCN1 (IC50 = 4.6 nM). DI-1548 potently and selectively inhibits cullin 3 neddylation at nanomolar concentrations, and exhibits no obvious effect on the neddylation of other cullin members (including cullin 1, 2, 4A, 4B, and 5). DI-1548 exhibits no cytotoxicity. DI-1548 covalently binds to DCN1, disrupting the DCN1-UBC12 interaction, causing the collapse of the neddylation complex, inactivating CRL3, leading to NRF2 accumulation and upregulation of its target genes, and ultimately protecting mice from liver damage. DI-1548 can be used in liver injury research .
Cat. No.: HY-146819
CAS No.: 2439165-37-2
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Compound 9 is the most effective against tumor specific Ca ix/ca XII (ki=29.1 and 8.8 nm), so it is possible to evaluate its cytotoxicity and selectivity to HepG-2, HCT-116 and MCF-7 cancer cell lines in vitro, and its IC50 values to tumor cells are 1.78, 1.94 and 3.07, respectively μ M. It showed that it had obvious cytotoxicity.
Cat. No.: HY-145842
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Encephalitic alphavirus-IN-1 has antiviral activity for VEEV and EEEV with EC50s of 0.24 μM and 0.16 μM, respectively. Encephalitic alphavirus-IN-1 has robust mouse plasma stability, and no obvious cytotoxicity .
Cat. No.: HY-N7980
CAS No.: 2170211-22-8
Category:
Quinones Rubia podantha Rubiaceae Plants Disease Research Fields Naphthalene Quinones Cancer
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Cat. No.: HY-163695
CAS No.: 1209698-02-1
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NLRP3-IN-41 (compd S-9) is an orally active and brain-penetrant NLRP3 inhibitor with anti-inflammatory activities, anti-neuroinflammatory effect and without obvious cytotoxicity. NLRP3-IN-41 inhibits the priming and activation stages of the NLRP3 inflammasome and can be used for inflammasome-related diseases research .
Cat. No.: HY-P11227
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Cat. No.: HY-149263
CAS No.: 1422051-33-9
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HAA-09 is an orally active and potent anti-influenza agent, targeting the influenza PB2_cap binding domain. HAA-09 displays potent anti-influenza A virus activity, with an EC50 of 0.03 μM. HAA-09 shows polymerase inhibition, with an IC50 of 0.06±0.004 μM. HAA-09 blocks virus replication without causing obvious cytotoxicity .
Cat. No.: HY-168175
PROTAC HDAC8 Degrader-2 is a HDAC6/8 PROTAC degrader, with IC50 values of 0.042 μM and 0.147 μM against human HDAC8 and HDAC6, respectively, and exhibits selectivity over other class I HDAC isozymes. PROTAC HDAC8 Degrader-2 induces apoptosis (apoptosis) in leukemia cells, shows no obvious cytotoxicity to normal cells, and has favorable chemical stability. PROTAC HDAC8 Degrader-2 can be used in research related to acute myeloid leukemia .
Cat. No.: HY-149719
CAS No.: 2798922-35-5
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Ferroptosis-IN-4 (compound 6k) is a ferroptosis inhibitor with EC50 value of 20 μM. Ferroptosis-IN-4 has no obvious cytotoxicity. Ferroptosis-IN-4 has a protective effect in glycerol-induced RM-AKI mice with alleviating kidney dysfunction .
Cat. No.: HY-115969
CAS No.: 1572464-22-2
F-17 is a potential inhibitor of virulence factor. F-17 shows very significant inhibitory effect on biofilm, elastase, pyocyanin, and swarming motility. F-17 also shows a good binding effect on LasR and PqsR. F-17 has no obvious cytotoxicity .
Cat. No.: HY-P10858
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Cat. No.: HY-W009160S
Synonyms: UV-329-d4
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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
