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ERK5-IN-2 is a selective, orally active, sub-micromolar ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis.
| 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.
| Molecular Weight | 388.19 |
| Formula | C17H11BrFN3O2 |
| CAS Number | 1888305-96-1 |
| Purity | >98.5% |
| Solubility | DMSO ≥ 100 mg/mL |
| Storage | 2-8°C, protect from light, dry, sealed |
| Related ERK Products |
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| Pamoic acid disodium
Pamoic acid disodium is a potent GPR35 agonist with an EC50 value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively. |
| KO-947
KO-947 is a potent and selective ERK inhibitor with slow dissociation kinetics. |
| MK-8353
MK-8353 (SCH900353) is an orally bioavailable, selective, and potent ERK1/2 inhibitor, with IC50 values of 23.0 nM and 8.8 nM, respectively. |
| JWG-071
JWG-071 is the first reported kinase-selective chemical probe for ERK5, inhibits ERK5 and LRRK2 with IC50 of 88 and 109 nM, respectively. |
| AG 126
AG 126 is a cell-permeable inhibitor of lipopolysaccharide (LPS)-induced synthesis of tumor necrosis factor-α and nitric oxide in murine peritoneal macrophages. |
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