Mixed Lineage Kinase
Inhibitory Selectivity
Isoform-specific Inhibitors
Mixed Lineage Kinase Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S8032 |
PRT062607 (P505-15) HClPRT062607 (P505-15, BIIB057, PRT-2607) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70. |
Dectin-1 is involved in activation of NLRP3-inflammasome by Malassezia spp. IL-1b secretion from mature human mono-DCs incubated with Syk-inhibitors (piceatannol, R406 or P505), 1 h prior to exposure to medium, MSU, b-glucan, nigericin or live M. furfur (MOI = 10) was determined after 6 h by ELISA.
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| S2805 |
LY364947LY364947 (HTS 466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II. |
The cytoplasmic and nuclear proteins were separated and the protein expression levels were determined by performing western blotting. LY364947 (1 uM), which is a potent ATP-competitive inhibitor of TGF-βRI, was used as the positive control. GAPDH and PARP were used as cytosolic and nuclear markers, respectively. |
|
| S7343 |
URMC-099URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. URMC-099 also inhibits ABL1 with IC50 of 6.8 nM. URMC-099 induces autophagy. |
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| S8251 |
NecrosulfonamideNecrosulfonamide is a very specific and potent necrosis inhibitor and blocks mixed lineage kinase domain-like protein (MLKL). |
Necroptotic death of HT-29 cells was verified using RIP1 or MLKL inhibitors necrostatine-1 and necrosulfonamide. HT-29 were pre-treated with the combinations of 10 nM birinapant, 50 μM z-VAD, 50 μM necrostatin and 20 μM necrosulfonamide as shown for 1 h, and then treated with 100 ng/ml of TST-TRAIL-wt, 4.2, 5.1 and 5.2 for 8 h.
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| S3238 |
ResibufogeninResibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S8032 |
PRT062607 (P505-15) HClPRT062607 (P505-15, BIIB057, PRT-2607) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70. |
Dectin-1 is involved in activation of NLRP3-inflammasome by Malassezia spp. IL-1b secretion from mature human mono-DCs incubated with Syk-inhibitors (piceatannol, R406 or P505), 1 h prior to exposure to medium, MSU, b-glucan, nigericin or live M. furfur (MOI = 10) was determined after 6 h by ELISA.
|
|
| S2805 |
LY364947LY364947 (HTS 466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM in a cell-free assay, shows 7-fold selectivity over TGFβR-II. |
The cytoplasmic and nuclear proteins were separated and the protein expression levels were determined by performing western blotting. LY364947 (1 uM), which is a potent ATP-competitive inhibitor of TGF-βRI, was used as the positive control. GAPDH and PARP were used as cytosolic and nuclear markers, respectively. |
|
| S7343 |
URMC-099URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. URMC-099 also inhibits ABL1 with IC50 of 6.8 nM. URMC-099 induces autophagy. |
||
| S8251 |
NecrosulfonamideNecrosulfonamide is a very specific and potent necrosis inhibitor and blocks mixed lineage kinase domain-like protein (MLKL). |
Necroptotic death of HT-29 cells was verified using RIP1 or MLKL inhibitors necrostatine-1 and necrosulfonamide. HT-29 were pre-treated with the combinations of 10 nM birinapant, 50 μM z-VAD, 50 μM necrostatin and 20 μM necrosulfonamide as shown for 1 h, and then treated with 100 ng/ml of TST-TRAIL-wt, 4.2, 5.1 and 5.2 for 8 h.
|
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S3238 |
ResibufogeninResibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression. |
