antiproliferation

Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.

BMS-202 (PD1-PDL1 inhibitor 2) is an inhibitor of the PD-1 (Programmed death- 1) PD-Ll (Programmed death-ligand 1) protein protein interaction.

EGFR-IN-12 (EGFR Inhibitor) is a cell permeable and selective inhibitor of EGFR kinase (IC50: 21 nM) and blocks receptor autophosphorylation in cells.

NG 52 (NG-52) is a cell-permeable, reversible, and ATP-compatible inhibitor of the cell cycle-regulating kinase Cdc28p and the related Pho85p kinase.

Vindesine sulfate (Desacetyl Vinblastine amide) is a vinca alkaloid which is a synthetic derivative of vinblastine, binds to the microtubular proteins of the mitotic spindle, leading to crystallization of the microtubule and mitotic arrest or cell death.

PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. It also inhibits the PDGFR, EGFR, and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively.

ACY-241, also known as Citarinostat (ACY241), is a potent, selective and orally available histone deacetylase (HDAC) inhibitor, with potential antineoplastic activity. Upon oral administration, ACY-241 inhibits the activity of HDACs; this results in an accumulation of highly acetylated chromatin histones, the induction of chromatin remodeling and an altered pattern of gene expression. This leads to the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes, which inhibit tumor cell division and induce tumor cell apoptosis.

RO2959 Hydrochloride (RO2959 HCl) is a potent and selective inhibitor of CRAC channel(IC50: 402 nM). It is also a potent inhibitor of human IL-2.

3-O-Methylgallic acid (3,4-Dihydroxy-5-methoxybenzoic acid) reduces cell proliferation in Caco-2 cells (IC50 = 24.1 μM) more effectively than anthocyanins and may offer protection against colon cancer after its formation in the gut. It inhibits transcription factors NF-κB, AP-1, STAT-1, and OCT-1, which are known to be activated in colorectal cancer.

MS8511, a selective covalent irreversible inhibitor of G9a GLP, targets a cysteine residue at the substrate binding site, displaying IC50 values of 100 nM (G9a) and 140 nM (GLP), alongside Kd values of 44 nM (G9a) and 46 nM (GLP). This compound effectively reduces cellular H3K9me2 levels and boosts antiproliferation activity, making it applicable in cancer research involving brain, breast, ovarian, lung, bladder, melanoma, and colorectal cancers, as well as studies on Alzheimer's disease (AD), sickle cell disease, and Prader−Willi syndrome (PWS) [1].

2-Nitrobenzoic acid (o-Nitrobenzoic acid) is a antiproliferation agent. 2-Nitrobenzoic acid shows IC50 of 8.3 μM to jurkat cell line expressing T type calcium channel alpha 1H or its splice variant delta 25.

CVT-11127 is an StearoylCoA Desaturase-1 (SCD1) inhibitor.

GW8510 is a CDK2 (cell cycle protein-dependent kinase 2) inhibitor and RRM2 (Ribonucleotide Reductase Regulatory Subunit M2) inhibitor that affects DNA synthesis and antiproliferation in tumor cells. In mammalian aging models, GW851 improves cognition and prolongs lifespan, which may be related to the modulation of the expression of cell cycle-related protein p21 and CDK family genes, as well as the improvement of mitochondrial function.

Sumarotene, a third-generation retinoid, is used as a topical dermatologic agent for the repair of antikeratinization, photodamage, and antiproliferation.

H8-A5, a HDAC8 inhibitor, shows antiproliferation activity in MDA-MB-231 cancer cells.

Hederacolchiside A1 (Raddeanoside R13) shows anti-leishmanial activity, it exhibits a strong antiproliferative activity on all stages of development of the parasite by altering membrane integrity and potential. Hederacolchiside A1 shows antiproliferation activities in three cancer cell lines with the IC50 value of 2.4 uM, it exhibits a preferential cytotoxicity on a pigmented melanoma cell line. It suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K Akt mTOR signaling pathway.

PROTAC BRD4 Degrader-8 is a potent BRD4 inhibitor with IC50 values of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively, effectively degrading the BRD4 protein in PC3 prostate cancer cells[1].

Tetrac (Tetraiodothyroacetic acid) is a derivative of L-thyroxine (T4), a thyroxine integrin receptor antagonist.Tetrac induces antiproliferation by blocking EGFR-mediated cell signaling in colorectal cancer cells.Tetrac blocks the effects of T4 and 3,5,3'-triiodo-L-thyronine (T3) on the cell-surface thyroxine integrin αvβ3 receptors.Tetra has anti-angiogenic, anti-tumor activity and pro-apoptotic activity.

HDAC-IN-33 is a highly potent HDAC inhibitor, effectively inhibiting HDAC1, HDAC2, and HDAC6 with IC50 values of 24, 46, and 47 nM, respectively. This compound demonstrates significant antiproliferation activity against tumor cells and exhibits remarkable in vivo antitumor efficacy. Additionally, HDAC-IN-33 initiates the activation of antitumor immunity [1].

ACC1 2-IN-2 (compound PF-3) is a potent inhibitor of ACC1 2, exhibiting IC50 values of 22 nM for ACC1 and 48 nM for ACC2. It demonstrates antiproliferative activity and holds significant research value in cancer studies.

Tyrphostin AG 879 (AG 879) effectively inhibits HER2 ErbB2 with an IC50 of 1 μM, demonstrating 100- and 500-fold higher selectivity for ErbB2 over EGFR and PDGFR, respectively.

Cmpd-A is a time-dependent CENP-E inhibitor with potent antitumor activity. Cmpd-A inhibits the ATPase activity of the CENP-E motor domain, acting as a time-dependent inhibitor with an ATP-competitive-like behavior. Cmpd-A causes chromosome misalignment on the metaphase plate, leading to prolonged mitotic arrest. Treatment with Cmpd-A induces antiproliferation in multiple cancer cell lines.

GNE-8525 is a potent and selective pan-TRK inhibitor. GNE-8525 demonstrated potent antiproliferation activity with IC50 = 0.003 μM. In a tumor xenograft model derived from the KM12 cell line, GNE-8525 demonstrated in vivo antitumor efficacy when administered at ascending doses twice daily (bid) for 14 days in rats. Deregulated kinase activities of tropomyosin receptor kinase (TRK) family members have been shown to be associated with tumorigenesis and poor prognosis in a variety of cancer types. In particular, several chromosomal rearrangements involving TRKA have been reported in colorectal, papillary thyroid, glioblastoma, melanoma, and lung tissue that are believed to be the key oncogenic driver in these tumors.