antiproliferation

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.

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].

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.

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

PROTAC BRD4 Degrader-8 is a potent BRD4 inhibitor, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells[1]. PROTAC BRD4 Degrader-8 (compound 8; 6 days) inhibits the proliferation of PC3 prostate cancer cells, with an IC50 of 28 nM[1].PROTAC BRD4 Degrader-8 (4 h) suppresses MYC gene transcript in MV4-11 AML cells, with an IC50 of 11 nM[1].PROTAC BRD4 Degrader-8 (4 h) potently degrades the BRD4 protein in PC3 prostate cancer cells, with an DC50 of 7.5 nM[1]. [1]. Dragovich PS, et, al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64(5):2576-2607.

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].

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

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.

Tyrphostin AG 879 (AG 879) effectively inhibits HER2/ErbB2 (IC50: 1 μM), 100- and 500-fold higher selective to ErbB2 than EGFR and PDGFR.

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

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.

ACC1/2-IN-2 (compound PF-3) is a potent inhibitor of ACC1/2 with IC50s of 22 and 48 nM for ACC1 and ACC2, respectively. ACC1/2-IN-2 shows antiproliferation activity and has research value in cancer research.

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.