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Takinib is an inhibitor of autophosphorylated and non-phosphorylated TAK1 that binds within the ATP-binding pocket and inhibits by slowing down the rate-limiting step of TAK1 activation. At 10 μM, Takinib shows significant inhibitory activity (<10% enzyme activity after exposure) on six serine/threonine kinases, including TAK1, IRAK4, IRAK1, GCK, CLK2, and MINK1. TAK1/MAP3K7 is most potently inhibited with a half maximal inhibitory concentration (IC50) value of 9.5 nM. In cell models of rheumatoid arthritis and metastatic breast cancer, Takinib treatment results in TNF-a-dependent induction of apoptosis due to inhibition of TAK1 as a key switch between survival and cell death. Takinib does not inhibit any of the MAP2Ks or MAP3Ks family members, i.e., MKK6/MAP2K6, MEKK1/ MAP3K1, MKK1/MAP2K1. Takinib also shows no efficacy toward the TAK1-closely related MAP3K5/ASK1. Takinib potently and selectively targets TAK1 and induces apoptosis in TNF-a-stimulated breast cancer and RA in vitro models.
| Cell Experiment | |
|---|---|
| Cell lines | MDA-MB-231 cells |
| Preparation method | MDA-MB-231 cells (1,000 cells/well) are seeded in a 96-well plate with 10% FBS, 5% Pen/Strep, 4g/l glucose DMEM medium. After 24h, cells are serum starved with 1% FBS, 5% Pen/Strep, 4g/l glucose DMEM medium for 4h. Cells are treated with titrations of Takinib in the presence or absence of 30 ng/mL TNFa. Plates at 0h and 24h following treatment were frozen at -80℃ after removal of media. After 24h, 100 μl ddH2O is added to each well and plates are refrozen. 1 μl from Hoechst stock [1 mg/ml in 1:4 DMSO/H2O] is dissolved in 1 ml of TNE buffer (10mM Tris, 2M NaCl, 1 mM Na2EDTA) and 100 μl of this solution is added to each well. The fluorescence is determined at 355/460 nm. |
| Concentrations | |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 322.36 |
| Formula | C18H18N4O2 |
| CAS Number | 1111556-37-6 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related MAPKAPK2/MAP3K/MAP4K Products |
|---|
| ASK1-IN-1
ASK1-IN-1 is a novel CNS-penetrant apoptosis signal-regulating kinase 1 (ASK1) inhibitor with good potency (cell IC50 = 138 nM), low clearance (rat Cl/Clu = 0.36/6.7 L h-1 kg-1) and good CNS penetration (rat K p,uu = 0.38). |
| GNE-8505
GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK). |
| TAK1-IN-3
TAK1-IN-3 is a potent ATP-competitive TAK1 inhibitor. |
| MSC 2032964A
MSC 2032964A is an orally active, selective inhibitor for apoptosis signal-regulating kinase 1(ASK1) with IC50 of 96 nM. |
| INS018 055
INS018 055 is a TNIK and MAP4K4 inhibitor with IC50 values of 12-120 nM, respectively. INS018 055 exhibits anti-fibrotic activity across different organs in vivo through oral, inhaled or topical administration. INS018 055 possesses anti-inflammatory effects in addition to its anti-fibrotic profile, validated in multiple in vivo studies. |
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