sub-g1

1. Thonningianin A has anti-cancer activities.2. Thonningianin A represents a new potent glutathione S-transferase in vitro inhibitor.3. Thonningianin A has antioxidant property, involves radical scavenging, anti-superoxide formation and metal chelation.

Iberdomide (CC-220) is a modulator of cereblon( IC50 value of 60 nM in a competitive TR-FRET assay).

RLX (PD 139530) is a PI3K/Akt/FoxO3a signal inhibitor with anticancer activity against tumour cell lines such as colon cancer, inducing sub-G1 arrest and mitochondrial potential loss, thereby inhibiting tumour growth. RLX also exhibits antitussive and anti-asthmatic activity, reducing eosinophils and total lymphocytes in bronchoalveolar lavage (BAL) fluid, and exhibits toxicity toward A549 cells.

HTR2A antagonist 1 (Compound 15f) is an HTR2A antagonist with an IC50 of 42.79 nM. It induces sub-G1 cell cycle arrest and apoptosis in colorectal cancer cells by activating the p53/p21/caspase 3 signaling pathway. HTR2A antagonist 1 exhibits good liver microsomal stability and is useful for colorectal cancer research.

BPU inhibits cell cycle progression at the sub-G1 phase. It acts as an anti-cancer agent by preventing angiogenesis in tumor tissues.

Cantharidic acid is a selective inhibitor of protein phosphatase 2 (PP2A) and protein phosphatase 1 (PP1). It impedes cell viability by upregulating the ERK1/2, p38, and JNK1/2 pathways, causes cell cycle arrest at the sub-G1 phase, and induces apoptosis in NPC-39 and HONE-1 cells.

HDAC8-IN-14 is a curcumin derivative serving as a selective HDAC8 inhibitor with a Ki of 9 nM. It induces reactive oxygen species (ROS) production, disrupts mitochondrial membrane potential, and promotes apoptosis. Furthermore, HDAC8-IN-14 significantly triggers cell accumulation in the sub-G0/G1 phase, indicative of apoptosis or necroptosis. It upregulates cytochrome c, cleaved caspase-3, and pro-apoptotic protein Bak expression, while maintaining anti-apoptotic protein Bcl-2 levels unchanged, making it a valuable compound for leukemia research.

EGFR-IN-207 (Compound 5h) is an epidermal growth factor receptor (EGFR) kinase inhibitor with an IC50 of 0.21 μM. It can induce cell cycle arrest at the Sub-G1 phase and promote apoptosis. EGFR-IN-207 exhibits anticancer activity against lung cancer and shows minimal toxicity in non-cancer cell lines. This compound is useful for lung cancer-related research.

ZW-49 is a pan-EGFR inhibitor with oral bioavailability, showing IC50 values ranging from 0.03 to 1.5 nM. It effectively inhibits all EGFR mutant subtypes and demonstrates selectivity for wild-type EGFR and other target families. ZW-49 blocks the ATP binding site and occupies a conserved hydrophobic sub-pocket, preventing steric clashes with P-loop mutations (PACC). It suppresses cancer cell proliferation, induces G0/G1 cell cycle arrest and apoptosis, and exhibits antiproliferative activity in xenograft mouse models. ZW-49 is applicable in cancer research, including studies on non-small cell lung cancer.

3-O-acetyloleanolic acid dose-dependently inhibited the viability of HCT-116 cells. Apoptosis was characterized by detection of cell surface annexin V and sub-G1 apoptotic cell populations.

Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine .1,2 Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA.3,1 Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts.1 It also halts the cell cycle at the sub-G1 phase and induces apoptosis in CEM cells.3 Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM) ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.4References1. Leanza, L., Miazzi, C., Ferraro, P., et al. Activation of guanine-β-D-arabinofuranoside and deoxyguanosine to triphosphates by a common pathway blocks T lymphoblasts at different checkpoints. Exp. Cell Res. 316(20), 3443-3453 (2010).2. Lambe, C.U., Averett, D.R., Paff, M.T., et al. 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies. Cancer Res. 55(15), 3352-3356 (1995).3. Rodriguez, C.O., Jr., Stellrecht, C.M., and Gandhi, V. Mechanisms for T-cell selective cytotoxicity of arabinosylguanine. Blood 102(5), 1842-1848 (2003).4. Kurtzberg, J. Guanine arabinoside as a bone marrow-purging agent. Ann. N.Y. Acad. Sci 685(1), 225-236 (1993). Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine .1,2 Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA.3,1 Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts.1 It also halts the cell cycle at the sub-G1 phase and induces apoptosis in CEM cells.3 Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM) ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.4 References1. Leanza, L., Miazzi, C., Ferraro, P., et al. Activation of guanine-β-D-arabinofuranoside and deoxyguanosine to triphosphates by a common pathway blocks T lymphoblasts at different checkpoints. Exp. Cell Res. 316(20), 3443-3453 (2010).2. Lambe, C.U., Averett, D.R., Paff, M.T., et al. 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies. Cancer Res. 55(15), 3352-3356 (1995).3. Rodriguez, C.O., Jr., Stellrecht, C.M., and Gandhi, V. Mechanisms for T-cell selective cytotoxicity of arabinosylguanine. Blood 102(5), 1842-1848 (2003).4. Kurtzberg, J. Guanine arabinoside as a bone marrow-purging agent. Ann. N.Y. Acad. Sci 685(1), 225-236 (1993).

DNA topoisomerase II inhibitor 1 is a potent inhibitor of DNA topoisomerase II that arrests the cell cycle in sub-G1 phase and induces apoptosis with anti-value-added effects.

HSP90-IN-11 is a potent inhibitor of HSP90 and induces significant accumulation of the sub-G1 population. HSP90-IN-11 has a potent HSP90α inhibitory effect comparable to that of AUY-922 (Luminespib). In CRC and NSCLC cells, HSP90-IN-11 exhibited significant anti-proliferative activity in the double-digit nM range.HSP90-IN-11 was able to rapidly degrade client proteins EGFR and Akt in NSCLC cells.

Anticancer agent 67 is a ciprofloxacin analogue, an anticancer agent that induces apoptosis and increases sub-G1 cell populations in MCF-7 cells.

MHY219 is a novel HDAC inhibitor. MHY219 induces apoptosis via up-regulation of androgen receptor expression in human prostate cancer cells. MHY219 was shown to enhance the cytotoxicity on DU145 cells (IC50, 0.36 μM) when compared with LNCaP (IC50, 0.97 μM) and PC3 cells (IC50, 5.12 μM). MHY219 showed a potent inhibition of total HDAC activity when compared with SAHA. MHY219 increased histone H3 hyperacetylation and reduced the expression of class I HDACs (1, 2 and 3) in prostate cancer cells. MHY219 effectively increased the sub-G1 fraction of cells through p21 and p27 dependent pathways in DU145 cells. MHY219 significantly induced a G2/M phase arrest in DU145 and PC3 cells and arrested the cell cycle at G0/G1 phase in LNCaP cells. Furthermore, MHY219 effectively increased apoptosis in DU145 and LNCaP cells, but not PC3 cells, according to Annexin V/PI staining and Western blot analysis. These results indicate that MHY219 is a potent HDAC inhibitor that targets regulating mu......

CDKI-83 is a potent CDK9 inhibitor. The compound shows effective anti-proliferative activity in human tumour cell lines with GI50 <1 μM, and is capable of inducing apoptosis in A2780 human ovarian cancer cells as determined by the activated caspase-3, Annexin V/PI double staining and accumulated cells at the sub-G1 phase of cellcycle. The research results suggest that combined inhibition of CDK9 and CDK1 may result in the effective induction of apoptosis and CDKI-83 has the potential to be developed as an anti-cancer agent.

Kobusine derivative-2, a kobusine derivative, exhibits antiproliferative activity against cancer cells, particularly by inducing the arrest of MDA-MB-231 cells in the sub-G1 phase, thus highlighting its potential anticancer activity.

Anticancer agent 66, a ciprofloxacin analog, functions as an anti-cancer agent by inducing apoptosis and elevating the sub-G1 cell population in MCF-7 cells.

BK50164, a potent CD73 inhibitor, exhibits an IC50 of 13.089 µM and demonstrates affinity for CD99 with a KD value of 1.5 µM. This compound not only possesses antiproliferative activity but also induces apoptosis and cell cycle arrest at the Sub-G1 phase [1].

CTL-06, a Fatty Acid Synthase (FASN) inhibitor with an IC50 of 3 μM, induces apoptosis, while CTL-12 impedes cell cycle progression in the Sub-G1/S phase and modulates apoptotic and anti-apoptotic markers by upregulating caspase-9 and Bax and downregulating Bcl-xL. Additionally, CTL-12 suppresses de novo lipogenesis, curtailing the metabolic needs of tumor cells, with utilization in breast and colorectal cancer studies [1].

CTL-12, a fatty acid synthase (FASN) inhibitor (IC50: 2.5 μM), induces apoptosis and disrupts the cell cycle at the Sub-G1/S phase. It upregulates caspase-9 and the apoptosis marker Bax, while downregulating the anti-apoptotic marker Bcl-xL. By inhibiting de novo lipogenesis, CTL-12 thwarts tumor cells' metabolic requirements and is frequently employed in breast and colorectal cancer studies [1].

Alpha-terthienylmethanol possesses potent cytotoxic activity against human endometrial cancer cells; it inhibits growth mediated by the induction of apoptosis, as shown by the accumulation of sub-G1 and apoptotic cells.

Cristacarpin is a natural product with antibacterial and anticancer activity that promotes endoplasmic reticulum stress and ROS production.