| Bioactivity | S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models[1]. |
| Sequence | Ac-Pro-Arg-cyclo(Cys-Phe-Leu-Val-Met)-Lys-Pro-Arg-Arg-Arg-Arg-Trp-NH2 (Cyclization Bridge via Benzene-1,3-bismethylene: Cys3-Met7) |
| Shortening | Ac-PR-Cyclo(CFLVM)-KPRRRRW-NH2 (Cyclization Bridge via Benzene-1,3-bismethylene: Cys3-Met7) |
| Formula | C97H151F3N32O17S2 |
| Molar Mass | 2158.57 |
| 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]. Luo Q, et al. Covalent Peptide LSD1 Inhibitor Specifically Recognizes Cys360 in the Enzyme-Active Region. J Med Chem. 2023 Nov 23;66(22):15409-15423. |