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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
165 Results for "
U2OS
" in MedChemExpress (MCE) Product Catalog:
Products (165)
165 Results for "U2OS" in MCE Product Catalog:
1
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Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology
Ex26 (S1P1-IN-Ex26) is a potent and selective sphingosine 1-phosphate receptor 1 (S1P1) antagonist (IC50=0.93 nM). Ex26 shows >3,000-fold selectivity for S1P1 over other Sphingosine 1-phosphate receptors. Ex26 can be used in experimental autoimmune encephalomyelitis reseach .
1
GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK [2].
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1 Cited Publications
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NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity (IC50=47 nM; KD=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism . NVS-CECR2-1 is a chemical probe.
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1 Cited Publications
Homo-PROTAC pVHL30 degrader 1 is a Homo-PROTAC autodegraders targeting the von Hippel-Lindau E3 ubiquitin ligase (VHL), with Kd values of 11 nM and 25 nM for pVHL19-EloBC and pVHL30-EloBC, respectively. Homo-PROTAC pVHL30 degrader 1 induces Cullin2 depletion, promotes VHL dimerization to form a ternary complex, and drives proteasome-dependent and CRL2-VHL-like ubiquitination-dependent autodegradation. Homo-PROTAC pVHL30 degrader 1 does not trigger hypoxic responses, and only causes extremely mild stabilization of hypoxia-inducible factor α subunits. Homo-PROTAC pVHL30 degrader 1 can be used in studies related to cervical cancer and osteosarcoma .
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1 Cited Publications
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LEI110 is a pan-inhibitor of the HRASLS family and an inhibitor of AP-2α, with a Ki of 20 nM against PLA2G16. LEI110 exhibits inhibitory activity against PLA2G16, HRASLS2, RARRES3 and iNAT, with pIC50 values of 7.0, 6.8, 6.8 and 7.6, respectively. LEI110 binds to the active site of PLA2G16, reduces intracellular arachidonic acid levels, and attenuates oleic acid-induced lipolysis. LEI110 stabilizes AP-2α, impairs its DNA-binding ability, inhibits the transcription of DNA damage repair genes, induces the accumulation of oxidative DNA damage, suppresses cell proliferation and clonogenicity, and sensitizes HCC cells to DNA-damaging agents. LEI110 can be used in research related to obesity, fatty liver disease, the common cold and hepatocellular carcinoma [2].
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1 Cited Publications
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1 Cited Publications
Synonyms: GL13; SBB-A-B
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SBB-Analogue (GL13) Biotin (GL13; SBB-A-B) consists of a Sudan Black B (SBB) (HY-D0213) derivative conjugated with biotin. SBB-Analogue (GL13) Biotin potently detects senescent cells and eliminates the drawback of false-positive staining caused by serum starvation and cell fusion in SA-β-gal assays. SBB-Analogue (GL13) Biotin can be used in flow cytometry, immunofluorescence analysis, and other applications .
1
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
Halcinonide (SQ-18566) is an orally active Smoothened (Smo) agonist. Halcinonide activates the Hedgehog signaling pathway by binding to Smo and promoting its internalization and expression, thereby activating Gli transcription factors. Halcinonide not only stimulates cell proliferation, increases the expression of cyclin D2/CDK6 and inhibits the degradation of caspase-3, but also suppresses Bcl-2/Bax-mediated apoptosis, oxidative stress and inflammatory responses. Halcinonide activates RxRγ to upregulate the expression of myelin genes, thereby reducing cerebral infarction and improving behavioral deficits. Halcinonide has been used in studies related to multiple sclerosis and ischemic stroke [2] .
Synonyms: BTRX-335140; CYM-53093
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Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.
Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy .
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JBSNF-00002 free base is an orally active small molecule inhibitor of the tricyclic nicotinamide N-methyltransferase (NNMT) with IC50 values for human, mouse and monkey sources of NNMT of 33, 210 and 190 nM respectively. JBSNF-00002 free base can reduce endogenous MNA levels in U2OS osteosarcoma cells, with its EC50 being 2.5 μM. JBSNF-00002 free base exhibits significant anti-obesity and anti-diabetic activities in the diet-induced obesity (DIO) model. JBSNF-00002 free base can be used for the study of metabolic diseases such as obesity, type 2 diabetes and non-alcoholic fatty liver disease .
Synonyms: MC-4R Agonist 2
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Bivamelagon (MC-4R Agonist 2) is an orally active MC4R agonist with EC50 values of 0.562 nM (Luci assay) and 36.5 nM (cAMP assay), and a Ki of 65 nM. Bivamelagon can be used for the research of diseases such as obesity and diabetes .
Cat. No.: HY-114293A
CAS No.: 75520-41-1
Synonyms: Acetyl-CoA trilithium
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UNC8153 TFA is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 TFA reduces the cellular levels of both NSD2 protein (DC50 in cell U2OS is 0.35 μM) and the H3K36me2 chromatin mark. UNC8153 TFA contains a simple warhead that confers proteasome-dependent degradation of NSD2 .
Synonyms: CINK4
GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer [2].
Dyrk1A-IN-4 is a potent and orally active Dyrk1A inhibitor. Dyrk1A-IN-4 exhibits IC50s against DYRK1A and DYRK2 of 2 nM and 6 nM. Dyrk1A-IN-4 exhibits the inhibition of the DYRK1A pSer520 autophosphorylation in U2OS cells with an IC50 of 28 nM. Dyrk1A-IN-4 can be used for the studies of ovarian adenocarcinoma, neuroblastoma and cervical squamous cell carcinoma .
Cat. No.: HY-151500B
Purity: 95.64%
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JBSNF-00002 hydrochloride is an orally active small molecule inhibitor of the tricyclic nicotinamide N-methyltransferase (NNMT) with IC50 values for human, mouse and monkey sources of NNMT of 33, 210 and 190 nM respectively. JBSNF-00002 hydrochloride can reduce endogenous MNA levels in U2OS osteosarcoma cells, with its EC50 being 2.5 μM. JBSNF-00002 hydrochloride exhibits significant anti-obesity and anti-diabetic activities in the diet-induced obesity (DIO) model. JBSNF-00002 hydrochloride can be used for the study of metabolic diseases such as obesity, type 2 diabetes and non-alcoholic fatty liver disease .
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Cat. No.: HY-P10426
CAS No.: 1446322-73-1
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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
