Bexarotene D4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma[1][2][3][4][5].
SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity[1].
Amino-PEG9-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
DCG066 is a G9a inhibitor in vitro.
Arctiin(NSC 315527), a plant lignan that can be extracted from the Arctium lappa (burdock) seeds, is a possible environmental endocrine disruptor compounds and have been shown to influence sex hormone metabolism as well as protein synthesis, steroid biosynthesis. IC50 Value:Target: Othersin vitro: Treatment of PC-3 cells with arctiin decreased the cell number in a concentration- and time-dependent manner in serum-containing condition. Arctiin preferentially induced cell detachment, but did not have anti-proliferation or cytotoxic effects in PC-3 cells. The arctiin-induced effect was inhibited by cycloheximide, indicating that protein synthesis was required [1]. Although arctiin, the active component of AL that has been described in the literature, was not able to reduce degranulation in RBL-2H3 cells, a single high-performance liquid chromatography (HPLC) fraction from the AL extract inhibited beta-hexosaminidase release (IC(50) = 22.2 microg/ml) [2]. The growth inhibition caused by arctiin is associated with the down-regulation of cyclin D1 protein expression. Furthermore, thearctiin-induced suppression of cyclin D1 protein expression occurs in various types of human tumor cells, including osteosarcoma, lung, colorectal, cervical and breast cancer, melanoma, transformed renal cells and prostate cancer. Depletion of the cyclin D1 protein using small interfering RNA-rendered human breast cancer MCF-7 cells insensitive to the growth inhibitory effects of arctiin, implicates cyclin D1 as an important target of arctiin [6]. in vivo: Histopathological evaluation of prostate revealed that all the rats in any group developed adenocarcinoma in dorsolateral lobe of prostate, except two rats in 0.1% arctiin treated and one rat in 0.002% arctiin treated groups without prostate adenocarcinoma development [3]. After oral administration of arctiin (30, 60, 120 mg/kgd) for three weeks, the levels of serum creatinine (Scr) and blood urea nitrogen (BUN) and 24-h urine protein content markedly decreased, while endogenous creatinine clearance rate (ECcr) significantly increased [4]. STZ-induced diabetic rats were treated witharctiin at the dosage of 60 or 40 mg/kg/day via intraperitoneal injection for 8 weeks. Blood glucose and 24-h urinary albumin content were measured, and kidney histopathological changes were monitored [5].
Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research[1][2].
Odoroside H is a natural cardenolide with anticancer activities[1].
Ociperlimab is a humanized IgG1 anti-TIGIT antibody. Ociperlimab binds to the extracellular domain of human TIGIT with high affinity (KD = 0.135 nM). Ociperlimab blocks the interaction between TIGIT and its ligands PVR or PVR-L2. Ociperlimab can be used in research of cancer[1][2].
AT7519 trifluoroacetate as a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
ABCG2-IN-1 (compound K2), a Ko143 analog, is an orally active ABCG2 inhibitor with an IC50 of 0.13 μM. ABCG2-IN-1 has favorable oral pharmacokinetic profiles in mice[1].
Antitumor agent-110 (compound 13) is an anticancer imidazotetrazine with good permeability properties. Antitumor agent-110 arrests cell cycel at G2/M phase, and induces apoptosis[1].
Ammonium iron(III) citrate (Ammonium ferric citrate), a physiological form of nonetransferrin-bound iron, induces intracellular iron overload to cause ferroptosis[1]. Ammonium iron(III) citrate can enhance protein production[2].
AS-1763 is a potent, selective, noncovalent, and orally available inhibitor of Bruton’s tyrosine kinase (IC50 = 0.85 nM).
Glucocorticoid receptor agonist-1 phosphate Gly-Glu-Br is an ADC linker that can be used to synthesize ABBV-154, ABBV-927, ABBV-368 or their analogs[1].
Teniposide is a podophyllotoxin derivative, acts as a topoisomerase II inhibitor, and used as a chemotherapeutic agent.
Anticancer agent 83 is a potent anticancer agent, inhibits LOX IMVI cells growth with a GI50 value of 0.15 mM. Anticancer agent 83 reduces mitochondrial membrane potential and induces DNA damage to induces leukemia cells apoptosis[1].
Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [3H]SP binding to the NK1 receptor with pKi values of 9.5 and 10.6 in rat and human membranes respectively, acts as a potential broad-spectrum anti-emetic agent[1].
Velpatasvir-d7 (GS-5816-d7) is the deuterium labeled Velpatasvir. Velpatasvir (GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons. Velpatasvir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.16 μM[2].
MMP-2/9-IN-1 (Compound 4a) is a potent dual MMP-2 and MMP-9 inhibitor with IC50 values of 56 nM and 38 nM, respectively. MMP-2/9-IN-1 inhibits tumor growth, strongly induces cancer cell apoptosis, inhibits cell migration, and suppresses cell cycle progression leading to DNA fragmentation[1].
Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations[1].
Tephrosin is a natural rotenoid which has potent antitumor activities. Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors[1].
Shizukaol D is a dimeric sesquiterpene isolated from Chloranthus serratus. Shizukaol D induces apoptosis and attenuated Wnt signalling[1].
L67 is a novel, competitive human DNA ligase inhibitor, inhibits DNA ligases I and III with IC50 of 10 μM and 10 μM.IC50 value: 10 μM [1]Target: DNA ligasesin vitro: L67 significantly increases the cytotoxicity of DNA damaging agents.[1] L67 also inhibits cell proliferation. [2]
Zelenectide (BCY8116) is a Bicycle peptide targeting to Nectin-4, which is a cell adhesion molecule. Zelenectide serves as a Bicycle tumor-targeted immune cell agonist[1].
MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53, induces apoptosis, and has anti-tumor activity[1].
GDC-0810 is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.
PROTAC BRD4 ligand-2 is a ligand for target BRD4 protein for PROTAC CFT-2718.
Lucidin primeveroside (Lucidin 3-O-β-primeveroside) is an anthraquinone derivative present in madder root, which has been used as a coloring agent and food additive. Lucidin primeveroside can be metabolically converted to genotoxic compound Lucidin, which subsequently forms lucidin-specific DNA adducts[1][2].
CC-115 hydrochloride is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
viFSP1 is a species-independent inhibitor of FSP1 that induces ferroptosis in FSP1-dependent cells. viFSP1 targets the highly conserved NAD(P)H binding pocket of FSP1 and directly inhibits FSP1. viFSP1 induces lipid peroxidation and has anticancer activity[1].