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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
183 Results for "
functional selectivity
" in MedChemExpress (MCE) Product Catalog:
Products (183)
183 Results for "functional selectivity" in MCE Product Catalog:
2
2 Cited Publications
Synonyms: 3-(2-Aminoethyl)indole~2-(3-Indolyl)ethylamine
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1 Cited Publications
Cat. No.: HY-19618
CAS No.: 1550053-02-5
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BRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC50 of 1.26 μM) or HDAC2 (IC50 of 1.34 μM). BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release. BRD3308 activates HIV-1 transcription and disrupts HIV-1 latency .
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1 Cited Publications
CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12 .
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3-Aminophenylboronic acid (m-Aminophenylboronic acid) is a phenylboronic acid derivative. 3-Aminophenylboronic acid reacts covalently with cis-diol groups of glycoproteins, enabling selective capture and detection of glycoproteins through fluorescence quenching of APBA-functionalized copper nanoclusters .
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1 Cited Publications
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RS 17053 (hydrochloride) is a potent and selective α1A adrenoceptor antagonist, with a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays.
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1 Cited Publications
Cat. No.: HY-W000897
CAS No.: 206658-89-1
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3-Aminophenylboronic acid monohydrate is a phenylboronic acid derivative. 3-Aminophenylboronic acid monohydrate reacts covalently with cis-diol groups of glycoproteins, enabling selective capture and detection of glycoproteins through fluorescence quenching of APBA-functionalized copper nanoclusters .
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1 Cited Publications
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A-77636 hydrochloride is a potent, orally active, selective and long acting dopamine D1 receptor agonist (pKi=7.40; Ki=39.8 nM) with antiparkinsonian activity. A-77636 hydrochloride is functionally inactive at dopamine D2 receptor .
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Tedalinab (GRC-10693) is a potent, orally active, and selective cannabinoid receptor 2 (CB2) agonist. Tedalinab has >4700-fold functional selectivity for CB2 over CB1. Tedalinab has potential for neuropathic pain and osteoarthritis treatment .
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1 Cited Publications
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Bisindolylmaleimide III is a protein kinase C (PKC) inhibitor with IC50 values of 0.26, 5.7, and 6 μM against PKCα, PKCδ, and PKCμ, respectively. Bisindolylmaleimide III also exhibits inhibitory activity against other off-targets, with IC50 values of 0.17, 1, and 2 μM against SLK, adenosine kinase (AK), and CDK2, respectively; its Ki for NQO2 is 16.5 μM. Bisindolylmaleimide III selectively binds to activated Rsk1 following EGF stimulation, and serves as a tool for detecting the activation status of intracellular Rsk1 and PKCα, as well as for functional analysis of SLK. Bisindolylmaleimide III can be used in studies of signal transduction and colorectal cancer .
1
1 Cited Publications
Cat. No.: HY-148775B
Purity: ≥95.0%
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PLGA-PEG-MAL (20KDA-5.0KDA, LA:GA RATIO 40:60) is a biodegradable amphipathic polymeric nanocarrier of poly (lactic-co-glycolic acid)-block-poly (ethylene glycol) (PLGA-PEG-Mal) that allows covalent modification of functional molecules. PLGA-PEG-MAL (20KDA-5.0KDA, LA:GA RATIO 40:60) modified with Angiopep-2 can cross the blood-brain barrier and exhibits targeting selectivity for glioblastoma cells. PLGA-PEG-MAL (20KDA-5.0KDA, LA:GA RATIO 40:60) can capture tumor-derived protein antigens, and exerts immunomodulatory effects when conjugated with anti-OX40 antibody; when used in combination with A2-CL/Dbait nanoparticles and radiotherapy, it prolongs survival time and reduces tumor volume in glioblastoma mouse models. PLGA-PEG-MAL (20KDA-5.0KDA, LA:GA RATIO 40:60) can be used for studies related to bacterial wound infections and glioblastoma .
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GDC-2394 is an orally active and selective NLRP3 inhibitor, and also inhibits IL-1β with IC50s of 0.4 μM (human IL-1β) and 0.1 μM (mouse IL-1β). GDC-2394 inhibits NLRP3-induced caspase-1 activity without inhibiting NLRC4-dependent inflammasome activation. GDC-2394 could be used to study gouty arthritis.
Cat. No.: HY-173455
CAS No.: 2930070-08-7
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NP1867 is a potent, selective, covalent PMS2 inhibitor. NP1867 functionally inhibits DNA mismatch repair. NP1867 enhances immune surveillance. NP1867 can be used in the research of colorectal cancer .
Synonyms: Z-338 free base; YM443 free base
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Acotiamide is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC50 of 1.79 μM. Acotiamide can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .
Cat. No.: HY-173268
CAS No.: 3051784-94-9
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UNC9426 is a potent and selective TYRO3 inhibitor (IC50 = 2.1 nM), demonstrating 276-fold and 90-fold selectivity over MERTK and AXL, respectively. UNC9426 reduces platelet aggregation without increasing bleeding time and blocks TYRO3-dependent functions in tumor cells and macrophages. UNC9426 demonstrates a favorable safety profile with no significant increase in bleeding risk in vivo. UNC9426 can be used for functional studies of TYRO3-dependent phenotypes such as non-small cell lung cancer (NSCLC) .
Cat. No.: HY-147403S
CAS No.: 1637681-55-0
Synonyms: JNJ-61393215
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MF-766 is a highly potent, selective and orally active EP4 antagonist with a Ki of 0.23 nM. MF-766 behaves as a full antagonist with an IC50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay. MF-766 can be used for cancer and inflammation diseases research .
Cat. No.: HY-126220
CAS No.: 1372642-77-7
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KMG-301AM is the acetoxy methyl esterified form of KMG-301. KMG-301AM successfully accumulates in mitochondria and then it is hydrolyzed to KMG-301. KMG-301 is an Mg 2+-selective fluorescent probe functional in mitochondria in intact cells. Since the mitochondrial membrane is impermeable to KMG-301, it is not released upon depolarization of the mitochondrial membrane potential. KMG-301 can indicate changes in mitochondrial Mg2+ concentration and shows Mg 2+ transport across the mitochondrial membrane in the early phases of a cellular model .
Cat. No.: HY-W400925
CAS No.: 1481447-40-8
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Sulfo-Cy5-N3 is an azide-functionalized sulfonated cyanine 5 Fluorescent dye and also serves as click chemistry coupling reagent. Sulfo-Cy5-N3 undergoes copper (I)-catalyzed azide-alkyne cycloaddition with alkyne-functionalized antibody constructs and peptide probes for site-selective fluorescent labeling. Sulfo-Cy5-N3 also acts as an emission dye for STORM super-resolution imaging. Sulfo-Cy5-N3 is applicable to the study of HER2-positive breast cancer .
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JNJ-39758979, a chemical probe, is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity .
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GS39783 is a positive allosteric modulator (PAM) of GABABR. Positive modulation of the GABABR can be used for the research of Nicotine addiction .
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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
