lsd1

GSK-LSD1 is a selective LSD1 inhibitor with potential anticancer activity that attenuates the expression of CTGF CCN2, MMP13, LOXL4, and waveform proteins in cancer cells.GSK-LSD1 regulates the cell cycle, induces apoptosis, and can be used to study breast cancer.

Lsd1-in-20 is a potent dual inhibitor of LSD1 G9a with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 showed antiproliferative activity against THP-1 leukemia cells and MDA-MB-231 breast cancer cells in vitro, with IC50 of 0.51 and 1.60 μM, respectively, at 72 h.

LSD1-IN-27 is a potent LSD1 inhibitor with an IC50 value of 13 nM.LSD1-IN-27 inhibited the stemness and migration of gastric cancer cells.LSD1-IN-27 inhibited the expression of PD-L1 in BGC-823 and MFC cells.LSD1-IN-27 potentiated the T-cell immune response against gastric cancer.

LSD1-IN-24 is a selective and potent LSD1 inhibitor with an IC50 value of 0.247 μM.LSD1-IN-24 induces PD-L1 expression and enhances the T cell killing response, and can be used in cancer-related diseases.

GSK-LSD1 dihydrochloride (GSK-LSD1 2HCl) is a specificity irreversible LSD1 inhibitor (IC50: 16 nM). The selectivity of GSK-LSD1 for LSD1 is >1000 fold over other closely related FAD utilizing enzymes (i.e. MAO-A, LSD2, MAO-B).

LSD1-IN-18 is a potent, non-covalent, selective inhibitor of LSD1 (Ki:0.156 μM; KD: 0.075 μM).LSD1-IN-18 exhibited anti-proliferative effects in THP-1 leukemia cells and MDA-MB-231 breast cancer cells with IC50 (72 h) of 0.16 and 0.21 μM, respectively.

LSD1-IN-25 (Compound 9j) is a potent, selective, and orally active LSD1 inhibitor with an IC50 of 46 nM (Ki = 30.3 nM) that induces apoptosis in cancer cells [1].

LSD1-IN-14, a powerful and specific inhibitor of LSD1 (with an IC50 value of 0.89 μM), effectively suppresses the growth of A549 and THP-1 cells and promotes the apoptosis of tumor cells [1].

LSD1-IN-13 hydrochloride (compound 7e) is an orally active LSD1 inhibitor with an IC50 of 24.43 nM that induces differentiation of AML (acute myeloid leukemia) cell lines.

LSD1-IN-37 (Compound 5g) is an inhibitor of lysine-specific demethylase 1 (LSD1), developed through an efficient synthesis strategy incorporating a hexafluoroisopropyl group. This approach does not require metal catalysts and offers excellent reaction stability and adaptability. LSD1-IN-37 exhibits outstanding LSD1 inhibitory activity and has potential for further research.

HSP90 LSD1-IN-1 (compound 6) is a dual inhibitor of HSP90 and LSD1. This compound effectively inhibits the proliferation of prostate cancer cell lines PC-3 and DU145, with GI50 values of 0.24 μM and 0.30 μM, respectively.

LSD1-IN-19 (compound 29) is a selective and potent non-covalent inhibitor of LSD1 with a Ki of 0.108 μM and a KD of 0.068 μM. Its 72h IC50 values are 0.17 μM and 0.40 μM, respectively.

LSD1 2-IN-4, a derivative of PCPA, functions as an inhibitor for both lysine-specific demethylase 1 (LSD1) and lysine-specific demethylase 2 (LSD2), demonstrating K i values of 0.11 μM and 130 μM against LSD1 and LSD2, respectively. This compound is utilized in researching various cancers, notably T-cell acute lymphoblastic leukemia (TALL) [1].

LSD1-IN-16 (compound 4b) is a potent inhibitor of LSD1 that inhibits LSD1-CoREST, MAO-A, and MAO-B with IC50 values of 0.015, 0.024, and 0.366 μM, respectively. LSD1-IN-16 also induces cell growth arrest in prostate cancer LNCaP cells with an IC50 value of 15.2 μM [1].

LSD1-IN-26 (compound 12u), a potent LSD1 inhibitor, exhibits an IC50 of 25.3 nM. It also demonstrates inhibition of MAO-A (IC50 = 1234.57 nM) and MAO-B (IC50 = 3819.27 nM), significantly inducing apoptosis in MGC-803 cells. This compound is applicable in gastric cancer research [1].

LSD1 EGFR-IN-1 (compound L-1) is an effective inhibitor of LSD1, EGFRT790M L858R, and EGFRL858R T790M C797S, with IC50 values of 6.24, 2.06, and 5.01 μM, respectively. This compound plays a significant role in cancer research.

LSD1-IN-39 (Compound 14) is a reversible inhibitor of LSD1 with an IC50 of 0.18 μM, showing broad-spectrum antiproliferative activity against cancer cells, inhibiting HepG2 cell migration, and suppressing epithelial-mesenchymal transition. Additionally, LSD1-IN-39 exhibits antitumor activity in mouse models.

LSD1-IN-34 (Compound 7d) is an orally effective inhibitor of lysine-specific demethylase (LSD) and monoamine oxidase (MAO), exhibiting IC50 values of 4.51 nM for LSD1 and 18.46 nM for MAO A. This compound inhibits activation of neonatal rat cardiac fibroblasts (NRCF) induced by angiotensin II (Ang II) and shows no significant toxicity at 20 μM. LSD1-IN-34 also inhibits the TGFβ Smad signaling pathway, contributing to the improvement of heart failure in mice. Moreover, it demonstrates favorable pharmacokinetic properties in rats.

LSD1-IN-33 (7d) is an orally effective inhibitor of LSD1, exhibiting an IC50 of 4.51 nM. It alleviates the activation of NRCFs induced by Ang II and reduces pathological cardiac hypertrophy and heart failure due to TAC-induced cardiac remodeling.

LSD1-IN-36, an effective LSD1 inhibitor with an IC50 value of 0.8 nM, induces cell apoptosis and arrests the cell cycle. This compound also exhibits antitumor activity.

LSD1-IN-29 (compound 6) serves as an inhibitor of Lysine specific demethylase 1 (LSD1), exhibiting an IC50 value of 19 nM [1].

LSD1-UM-109 is a highly potent and reversible inhibitor of LSD1, demonstrating an IC50 of 3.1 nM. This compound exhibits strong antiproliferative activity, inhibiting cell growth with IC50 values of 0.6 nM in the MV4;11 acute leukemia cell line and 1.1 nM in the H1417 small-cell lung cancer cell line [1].

LSD1 ER-IN-1 (compound 11g) is a potent inhibitor of ER and LSD1, targeting LSD1 with an IC50 of 1.55 μM and exhibiting significant anti-proliferative effects on MCF-7 breast cancer cells with an IC50 of 8.79 μM.

LSD1 2-IN-3 is a selective inhibitor of lysine-specific demethylase 1 (LSD1) with a Ki value of 11 nM, compared to 7 μM for LSD2. Aberrant expression of LSD1 is found in tumor stem cells, and LSD1 2-IN-1 inhibits LSD1 cell proliferation [1].