| Bioactivity | (S)-PFI-2 hydrochloride is an inhibitor of lysine methyltransferase SETD7 and is approximately 500-fold more active than its enantiomer (R)-PFI-2. (R)-PFI-2 is a cofactor-dependent and substrate-competitive inhibitor. (R)-PFI-2 can occupy the substrate peptide binding groove of SETD7 (including the catalytic lysine binding channel) and interact with the cofactor The donor methyl group is in direct contact. However, (S)-PFI-2 was not observed to have the same interaction as (R)-PFI-2[1][2]. |
| Target | Lysine methyltransferase SETD7 |
| Invitro | (S)-PFI-2 hydrochloride (10 μM; 2 h) 不能导致 MCF7 细胞中核 YAP 呈剂量依赖性增加，或者使 YAP 靶基因 AREG 和 CYR61 的表达增强；而 (R)-PFI-2 可以增加 YAP、AREG 和 CYR61 的表达[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> (S)-PFI-2 hydrochloride 相关抗体: |
| CAS | 1627607-88-8 |
| Formula | C23H26ClF4N3O3S |
| Molar Mass | 535.98 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Niu Y, et al. Revealing inhibition difference between PFI-2 enantiomers against SETD7 by molecular dynamics simulations, binding free energy calculations and unbinding pathway analysis. Sci Rep. 2017 Apr 18;7:46547. [2]. Barsyte-Lovejoy D, et al. (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells. Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):12853-8. |
(S)-PFI-2 hydrochloride
CAS: 1627607-88-8 F: C23H26ClF4N3O3S W: 535.98
(S)-PFI-2 hydrochloride is an inhibitor of lysine methyltransferase SETD7 and is approximately 500-fold more active than
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