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(R)-NX-2127 (compound 28) is an orally bioavailable Bruton’s Tyrosine Kinase (Btk) degrader. (R)-NX-2127 mediates the degradation of transcription factors IKZF1 and IKZF3 through molecular glue interactions with the cereblon E3 ubiquitin ligase complex. NX-2127 degrades common BTK resistance mutants, including BTKC481S. NX-2127 can bind and proteasomally degrade each mutant BTK proteoform, resulting in potent blockade of BCR signaling. NX-2127 exhibited rapid association and dissociation rates, with Kd values of 18 nM (for WT BTK), 45 nM (BTK C481S), 18 nM (BTK T474I), 44 nM (BTK M437R), 97 nM (BTK V416L), and 88 nM (BTK L528W).
| Cell Experiment | |
|---|---|
| Cell lines | knock-in BTK WT, C481S, V416L, T474I, or L528W TMD8 cells |
| Preparation method | Calcium flux Intracellular calcium levels in knock-in BTK WT, C481S, V416L, T474I, or L528W TMD8 cells were either treated with vehicle [dimethyl sulfoxide (DMSO)] or 1 mM of NX-2127 for 24 hours before staining using Indo-1 on an LSR-Fortessa-HTS flow cytometer. Indo-1 Violet and Indo-1 Blue levels were measured for two minutes immediately followed by stimulation with 10 μg/ml of anti-human IgM and then measured continuously for 10 min. BTK WT or L528W mutant cells expressing shHCK or shILK were treated with doxycycline for 48 hours before being stained using Indo-1 and measured as described above. |
| Concentrations | 1 mM |
| Incubation time | 24 hours |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 719.83 |
| Formula | C39H45N9O5 |
| CAS Number | 3024312-52-2 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related BTK Products |
|---|
| BIIB129
BIIB129 is a covalent, selective inhibitor of Bruton's tyrosine kinase (BTK) capable of penetrating the blood-brain barrier. BIIB129 inhibits the activity of BTK by covalently binding to Cys481 in BTK, thereby affecting the function of B cells and myeloid cells. |
| UBX-382
UBX-382 is an orally available proteolysis-targeting chimeras (PROTACs) that target BTK to inactivate B-cell receptor signaling. |
| GDC-0834
GDC-0834 is a potent and selective BTK inhibitor. |
| DD-03-171
DD-03-171 is a BTK, IKFZ1 and IKFZ3 degrader, the BTK IC50 a value of 5.1 nM. |
| N-piperidine Ibrutinib hydrochloride
N-piperidine Ibrutinib hydrochloride is a reversible Ibrutinib derivative. |
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