XMD8-92, via inhibition of BMK1 activation, significantly induces p21 expression in cells, and mediates suppression of cancer cell proliferation. XMD8-92 markedly abrogates the inhibitive effects of hydroxysafflor yellow A (HSYA) on hepatic stellate cell (HSC) activation, and blockes the HSYA-mediated MEF2C down-regulation.
| Cell Experiment | |
|---|---|
| Cell lines | A549 cell lines |
| Preparation method | Control and shBNIP3/shBNIP3L A549 sphere cells were treated with/without 4 μmol/L XMD8-92 for 36 hrs, and collected by trypsinization and centrifugation at 300 G for 5 mins. The resultant cells were washed twice with cold PBS and resuspended in 100 μL Annexin-binding buffer. |
| Concentrations | 4 μmol/L |
| Incubation time | 36 h |
| Animal Experiment | |
|---|---|
| Animal models | Nod/Scid mice bearing HeLa xenograft, C57Bl/6 mice bearing LL/2 xenograft |
| Formulation | |
| Dosages | ~50 mg/kg twice a day |
| Administration | i.p. |
| Molecular Weight | 474.55 |
| Formula | C26H30N6O3 |
| CAS Number | 1234480-50-2 |
| Solubility (25°C) | DMSO 48 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related ERK Products |
|---|
| PACAP-38 (31-38), human, mouse, rat
PACAP-38 (31-38), human, mouse, rat is a PAC1 receptor activator and increases the α-secretase activity. |
| Endothelin-1 (1-31) (Human)
Endothelin-1 (1-31) (Human) is a potent vasoconstrictor and hypertensive agent. |
| ZINC12409120
ZINC12409120 is a high selective ERK inhibitor. |
| Tizaterkib (hexanedioic acid)
Tizaterkib hexanedioic acid is a potent and selective ERK2 inhibitor, with an IC50 of 0.6 nM. |
| TAT-MEK1
TAT-MEK1 is an inhibitor ofERK2, consisting of TAT and MEK1 (N-terminal), TAT (YGRKKRRQRRR) derived from human immunodeficiency (HIV-1) transcriptional trans activator (TAT), is a cell-penetrating peptide. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
