PARP1-IN-14 (compound 19k) is a potent PARP1 inhibitor, with an IC50 of 0.6 ± 0.1 nM. PARP1-IN-14 exhibits antiproliferative effect against both MDA-MB-436 (BRCA1−/−) and Capan-1 (BRCA2−/−) cells with IC50 values below 0.3 nM[1].
2’-dG (iBu)-2’-phosphoramidite is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity[1].
IKKγ NBD Inhibitory Peptide is a NEMO-binding domain peptide (NBD peptide) corresponding to the NEMO amino-terminal alpha-helical region, which is shown to block TNF-alpha-induced NF-kB activation[1].
GSK484 is a peptidylarginine deiminase 4 (PAD4) inhibitor. GSK484 demonstrates high affinity binding to PAD4 with IC50s of 50 nM in the absence of Calcium. In the presence of 2 mM Calcium, notably lower potency (250 nM) is observed.
Gossypol, a natural product isolated from cottonseeds and roots, binds to Bcl-xL protein and Bcl-2 protein with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively.
2-tert-Butyl-1,4-benzoquinone is an electrophilic metabolite of butylated hydroxyanisole and an oxidation product of 2-tert-butylhydroquinone[1].
Arylquin 1, a prostate-apoptosis-response-4 (Par-4) secretagogue, targets vimentin to induce Par-4 secretion. Arylquin 1 induces non-apoptotic cell death in cancer cells through the induction of lysosomal membrane permeabilization (LMP)[1].
Eftozanermin alfa (ABBV-621) is a second-generation tumor necrosis factor-related apoptosis-inducing ligand receptor (TRAIL-R) agonist. Eftozanermin alfa induces apoptosis in tumor cells by activation of death receptors 4/5. Eftozanermin alfa can be used for the research of multiple solid and heme malignancies[1][2].
Lirilumab (IPH2102) is an anti-KIR monoclonal antibody, and shows antitumor activity. Lirilumab can be used in Leukemia, squamous cell carcinoma of the head and neck (SCCHN) research[1][2].
GR 128107 is an antagonist of melatonin receptor.
LDN193189 is a BMP signaling inhibitor, inhibiting ALK1, ALK2, ALK3 and ALK6 with IC50s of 0.8, 0.8, 5.3, 16.7 nM, respectively.
Adenosine-2′-13C is the 13C labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiolo
2-Chloro-3′-deoxyadenosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Cyclo(Ala-Pro) is an anticancer agent that is toxic to cancer cells such as A549, HCT-116 and HepG2[1].
DMH-1 is a potent and selective BMP inhibitor with IC50s of 27/107.9/<5/47.6 nM for ALK1/ALK2/ALK3/ALK6, respectively.
1,2-Di-O-isopropylidene-5-O-(4-methylbenzoyl)-α-D-xylofuranose is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
AMI-1 is a potent, cell-permeable compound which inhibits protein arginine N-methyltransferases (PRMTs), including human PRMT1 (IC50 = 8.8μM) and yeast-Hmt1p (IC50 = 3.0μM), by blocking peptide-substrate binding.IC50 value: 8.8μM (human PRMT1), 3.0μM (yeast-Hmt1p)Target: human PRMT1, yeast-Hmt1pin vitro: AMI-1 suppresses the transcriptional coactivator activity of PRMT1 and PRMT4 and it inhibits HIV-1 RT polymerase (IC50 = 5.0μM). PRMT1 methylates histone H4, and is essential for other subsequent histone modifications.[1] AMI-1 is the most active nonpeptidic inhibitor reported to be selective against PRMT1. AMI-1 is a selective PRMT inhibitor with a bisanionic structure that is related to compounds known to generate pleiotropic interactions with many proteins, should be further optimized before exploring additional binding pockets. [2]in vivo: AMI-1 is administered intranasally to chronic AIPI rats to determine PRMT effects on asthmatic parameters. AMI-1 inhibited the expression of COX2 in TGF-β-stimulated cells. AMI-1 administered to AIPI rats reduced COX2 production and humoral immune response, and it abrogated mucus secretion and collagen generation.[1]
α-Hexylcinnamaldehyde, a compound derived from Cinnamaldehyde. α-Hexylcinnamaldehyde has the potential antimutagenic and chemosensitizing properties. α-Hexylcinnamaldehyde is widely used as an ingredient in many personal care, and as an additive in food and the pharmaceutical industry[1].
(2,4-Dichloro-3,5-dimethoxyphenyl) methyl 6-O-β-D-glucopyranosyl-β-D-glucopyranoside is an anticancer agent that inhibits the proliferation of lung cancer A549 cells (IC50=29 μΜ). (2,4-Dichloro-3,5-dimethoxyphenyl) methyl 6-O-β-D-glucopyranosyl-β-D-glucopyranoside can be obtained from Lilium regale and can be used in cancer research[1].
Proscillaridin A is a potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively[1].
EBI-1051 is a highly potent and orally efficacious MEK inhibitor with an IC50 of 3.9 nM.
Boc-NH-PEG3-CH2COOH is a PEG-based PROTAC linker can be used in the synthesis of PROTAC[1].
MRT68921 hydrochloride is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.
Naringenin is the predominant flavanone in grapefruit; displays strong anti-inflammatory and antioxidant activities.
PI3K/Akt/mTOR-IN-2 is a PI3K/AKT/mTOR pathway inhibitor. PI3K/Akt/mTOR-IN-2 possess anti-cancer effects and selectivity against MDA-MB-231 cells with IC50 value of 2.29 μM. PI3K/Akt/mTOR-IN-2 can induce cancer cell cycle arrest and apoptosis[1].
ODN 1585 is a potent inducer of IFN and TNFα production. ODN 1585 is a potent stimulator of NK (natural killer) function. ODN 1585 increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 induces regression of established melanomas in mice. ODN 1585 can confer complete protection against malaria in mice. ODN 1585 can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 can be used as a vaccine adjuvant[1][2][3].
Adamtsostatin 18 is an anti-angiogenic peptide derived from proteins containing type I thrombospondin motifs. Adamtsostatin 18 inhibits cell migration and proliferation[1].
SGI-7079 is an Axl inhibitor, significantly inhibits the proliferation of SUM149 or KPL-4 cells with an IC50 of 0.43 or 0.16 μM, respectively.Ic50 value:Target: Axlin vitro: SGI-7079 treatment inhibits the phosphorylation of Axl at Tyr 702 upon Gas6 stimulation in SUM149 cells. The growth of SUM149 and KPL-4 in soft agar, one of the hallmark characteristics of cellular transformation and uncontrolled cell growth, is also significantly inhibited by SGI-7079 treatment. SGI-7079 treatment also significantly decreases the migration and invasion of SUM149 cells and the invasion of KPL-4 cells. Taken together, Axl inhibitor SGI-7079 significantly inhibits the proliferation, migration, and invasion of IBC cells, suggesting that Axl may be a promising therapeutic target in patients with IBC. [1]in vivo: SGI-7079 inhibits tumor growth in a dose dependent manner, and at the maximum dose, inhibited tumor growth by 67%, compared to control. The combined inhibition of Axl (SGI-7079) plus EGFR (Erlotinib) is significantly more effective than either drug alone. Notably, SGI-7079 + Erlotinib (25/100 mg/kg) reduced the tumor growth by 82%. Axl blockade by SGI-7079 inhibits the growth of mesenchymal NSCLC xenograft tumors. [2]
Erythrodiol 3-O-palmitate is a natural product isolated from Dicranostigma leptopodum (Maxim) Fedde, Gentiana rhodantha Franch or Swertia kouitchensis. Erythrodiol 3-O-palmitate has antitumor activity, and inhibits the proliferation of K562 cells with the inhibition rate of 47% at 100 ug/mL[1][2][3].