TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.
| Molecular Weight | 519.52 |
| CAS Number | 1450833-55-2 |
| Solubility (25°C) | DMSO 50 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 E1/E2/E3 Enzyme Products |
|---|
| NX-1607
NX-1607 is an oral, small molecule inhibitor of casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) that has been shown to enhance antigen recall, reduce T cell exhaustion and increase cytokine production upon T cell receptor stimulation, overcoming suppressive signals from the tumor microenvironment (TME). |
| SENP1-IN-1
SENP1-IN-1 is a specific deSUMOylation protease 1 (SENP1) inhibitor. SENP1-IN-1 can be used for tumor radiosensitivity enhancement. |
| TRAF6 peptide
TRAF6 peptide is a specific TRAF6-p62 inhibitor. |
| LTP001
LTP001 is a SMURF1 antagonist that can be used in studies related to idiopathic pulmonary fibrosis (IPF). |
| HECT E3-IN-1
HECT E3-IN-1 is a HECT E3 ligase inhibitor. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
