TAS-116 is a novel, small-molecule HSP90 inhibitor which inhibits geldanamycin-FITC binding to HSP90 proteins with Ki values of 34.7 nmol/L, 21.3 nmol/L, >50,000 nmol/L, and >50,000 nmol/L for HSP90α, HSP90β, GRP94, and TRAP1, respectively. Furthermore, TAS-116 does not inhibit other ATPases such as HSP70 (IC50 >200 μmol/L).
| Molecular Weight | 454.53 |
| Formula | C25H26N8O |
| CAS Number | 1260533-36-5 |
| Solubility (25°C) | DMSO 91 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 HSP Products |
|---|
| Hsp70-derived octapeptide
Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs. |
| p5 Ligand for Dnak and DnaJ
p5 Ligand for Dnak and DnaJ is a nonapeptide, which corresponds to the main binding site for the 23-residue part of the presequence of mitochondrial aspartate aminotransferase. |
| Tertomotide hydrochloride
Tertomotide hydrochloride is a peptide consisting of 16 amino acids containing sequences derived from human telomerase reverse transcriptase (TERT).Tertomotide penetrates cells and interacts with HSP70 and HSP90, as well as inhibiting amyloid beta and tau, and inhibiting aging-related signaling in the brain. pathways, which could be used in aging and Alzheimer's disease related studies. |
| BMS-986263
BMS-986263 is a small interfering RNA (siRNA) that targets Hsp47 and can be used in studies related to idiopathic pulmonary fibrosis (IPF). |
| AT-533
AT-533 is a potent Hsp90 and HSV inhibitor. |
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