INCA-6 is a inhibitor of interaction between calcineurin and its substrate nuclear factor of activated T cells (NFAT). INCA-6 blocks at the substrate recognition site but not at the catalytic site (Kd = 0.8 mM). INCA-6 inhibits NFAT dephosphorylation and nuclear import. INCA-6 also prevents induction of cytokine mRNAs that are downstream targets of NFAT.
| Molecular Weight | 284.31 |
| Formula | C20H12O2 |
| CAS Number | 3519-82-2 |
| Form | Solid |
| Solubility (25°C) | DMSO 5.69 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 NFAT Products |
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| Cyclosporin D
Cyclosporin D, a metabolite of Cyclosporin A, is a weak immunosuppressant. Cyclosporin D is used as internal standard for quantification of Cyclosporin A. Cyclosporin A is a potent immunosuppressant agent, suppress T cell activation by inhibiting calcineurin and the calcineurin-dependent transcription factors nuclear factor of activated T cells (NFAc). |
| (+)-Syringaresinol
(+)-Syringaresinol, a lignan, is a NFAT transcription factor inhibitor, with an IC50 of 329.4 μM. (+)-Syringaresinol also can be used for the research of lymphocytic leukemia. |
| NFAT Inhibitor-1 (VIVIT peptide)
NFAT Inhibitor-1 (VIVIT peptide) is a cell-permeable peptide inhibitor of nuclear factor of activated Tcells (NFAT), it is superior at inhibiting calcineurin-mediated dephosphorylation of NFAT1, NFAT2, and NFAT4 in cell extracts. |
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