Scientific Reviews
Product Guides
Blogs
Topics
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
26 Results for "
half-maximal
" in MedChemExpress (MCE) Product Catalog:
Products (26)
26 Results for "half-maximal" in MCE Product Catalog:
14
6
Target:
Research Areas:
Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
5
5 Cited Publications
Cat. No.: HY-16910
CAS No.: 838818-26-1
WIKI4 is a potent tankyrase inhibitor with an IC50 of 26 nM for TNKS2. WIKI4 potently inhibits Wnt/β-catenin signaling and that its half-maximal response dose is 75 nM. WIKI4 mediates its effects on Wnt/β-catenin signaling by inhibiting the enzymatic activity of TNKS2 . WIKI4 is cytotoxic to SCLC cells with an IC50 value of 0.02 μM .
3
3 Cited Publications
Target:
Research Areas:
ZXH-3-26 is a PROTAC connected by ligands for Cereblon and BRD4 with a DC50/5h of 5 nM. The DC50/5h refers to half-maximal degradation after 5 hours of treatment of ~ 5 nM .
1
1 Cited Publications
Cat. No.: HY-162501
CAS No.: 3041134-13-5
Target:
Research Areas:
Yaddle1 is an agonist of the mechano-activated ion channel (Piezo1) with a half-maximal effective concentration (MEC50) of 0.40 μM. Yaddle1 can significantly trigger Ca 2+ inflow in T cells and induce T cell activation response. Yaddle1 can be used in the study of vaccine adjuvants .
Synonyms: Ro 16-6028
Target:
Research Areas:
Bretazenil (Ro 16-6028) is a partial agonist at the gamma-aminobutyric acid A (GABAA) receptor-linked benzodiazepine site. Bretazenil is potent benzodiazepine examined, exhibiting an IC50 (concentration at which half-maximal inhibition of specific [35S]TBPS binding occurs) of 6.1 nM. Bretazenil shows an EC50 of 10 nM for recombinant α1β1γ2. Anticonvulsant effects .
Cat. No.: HY-P5485
CAS No.: 271798-75-5
Cat. No.: HY-130654
CAS No.: 2597167-24-1
Synonyms: VH032-C2-PEG4-N3
Research Areas:
(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-124892A
CAS No.: 103994-00-9
Synonyms: Acetyl-AF64
Target:
Research Areas:
Acetylethylcholine mustard hydrochloride (Acetyl-AF64) is an inhibitor of choline acetyl-transferase that reduces the contraction frequency of the myotubes by inhibiting the synthesis of acetylethylcholine (Ach) with the half-maximal inhibitory concentration (IC50) of 1.22 mM. Acetylethylcholine mustard hydrochloride is an irreversible ligand for the high affinity choline transport system. Acetylethylcholine mustard hydrochloride is also a cholinotoxin. Acetylethylcholine mustard hydrochloride is a precursor for ethylcholine mustard aziridinium ion .
Cat. No.: HY-177122
CAS No.: 3034857-88-7
Target:
Research Areas:
Raxlaprazine etomoxil is a small molecule compound with dopamine D2 and D3 receptor modulating activity, which has potential application value in research related to mental illnesses. Raxlaprazine etomoxil exhibits high affinity for human recombinant D2L receptors, with an inhibition constant (Ki) of 1.95 nM. Raxlaprazine etomoxil effectively inhibits forskolin-stimulated cAMP accumulation, with an half maximal effective concentration (EC50) of 3.72 nM in functional activity experiments .
Cat. No.: HY-W040263
CAS No.: 91000-53-2
Synonyms: TAPS Na
Cat. No.: HY-138642A
CAS No.: 2229711-08-2
Synonyms: (Rac)-ARV-471
Target:
Research Areas:
(Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
Cat. No.: HY-125627
CAS No.: 305822-63-3
Research Areas:
CP-394531 is an efficient and highly selective non-steroidal glucocorticoid receptor (GR) antagonist, with a Ki value of 0.1 nM. CP-394531 has a weak binding to androgen receptor (AR) (Ki = 130 nM), and has almost no effect on progesterone receptor (PR) and estrogen receptors (ERα, ERβ). CP-394531 completely blocks the half-maximal agonistic effect induced by Dexamethasone (HY-14648G), with a Kif of 4.1 nM. CP-394531 can be used to study various diseases such as diabetes, obesity, depression, neurodegenerative diseases, glaucoma and Cushing's disease .
Cat. No.: HY-106560
CAS No.: 57132-53-3
Research Areas:
Proglumetacin is an orally active and potent cyclo-oxygenase inhibitor. Proglumetacin can inhibits SARS-CoV Mpro (main protease of the SARS-CoV-2), with an AC50 of 8.9 μM (activity concentration at half maximal activity). Proglumetacin has anti-inflammatory activity, can be used for inflammation (such as Rheumatoid arthritis, and Allergic air pouch inflammation) research[1][2][3].
Cat. No.: HY-116197
CAS No.: 133345-68-3
Target:
Research Areas:
CGP44532 is a GABAB receptor agonist with a pEC50 (geometric mean of the half-maximal effective concentration) value of 5.63 μM .
Cat. No.: HY-145432
CAS No.: 2747100-02-1
PI3K-IN-28 (Compound 6c) is a potent inhibitor of PI3K. PI3K-IN-28 displays the most potent activity with lower toxic effects on MCF-10a. PI3K-IN-28 displays half-maximal inhibitory concentration (IC50, μM) values of 5.8, 2.3, and 7.9. PI3K-IN-28 is the most potent one with a selectivity index (SI) of 39 and is considered as a latent lead for further optimization of anticancer agents .
Cat. No.: HY-158053
CAS No.: 3030502-21-4
Antifungal agent 94 (Compound 49) is a Flavonoid derivative, which exhibits antifungal activity with EC50 of 0.28 μM and a half-maximal effective concentration of 0.46 μg/mL against Rhizoctonia solani .
Cat. No.: HY-144107
CAS No.: 2425805-22-5
HCV-IN-34 (compound 3i) is an orally active and potent HCV entry inhibitor. HCV-IN-35 shows excellent antiviral activity, with an EC50 of 0.010 μM and a CC50 (half-maximal cytotoxic concentration) of 8.23 μM .
Cat. No.: HY-144109
CAS No.: 2757963-81-6
HCV-IN-36 (compound (S)-3h) is an orally active and potent HCV entry inhibitor. HCV-IN-36 shows excellent antiviral activity, with an EC50 of 0.016 μM and a CC50 (half-maximal cytotoxic concentration) of 8.78 μM .
- 1
- 2
-
-
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
