Fotemustine is a DNA-alkylating agent, with antitumor activity.
BRACO-19 is a potent small molecule Telomerase inhibitor (IC50=115 nM) that inhibits expression of human telomerase reverse transcriptase (hTERT); induces cellular senescence and inhibits growth of uterine cancer cells in vitro, inhibits growth of uterine tumor xenografts in vivo.
Tetroxoprim is an antimicrobial DHFR inhibitor[1].
2’-Deoxy-2’-fluoro-b-D-arabinocytidine 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].
Purine-9-b-D-(3’,5’-di-O-benzoyl-2’-deoxy-2’-fluoro)arabinoriboside 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].
Crebinostat is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.7 nM, 1.0 nM, 2.0 nM and 9.3 nM for HDAC1, HDAC2, HDAC3 and HDAC6, respectively. Crebinostat potently induces acetylation of both histone H3 and histone H4 as well as enhances the expression of the cAMP response element-binding protein (CREB) target gene Egr1. Crebinostat increases the density of synapsin-1 punctae along dendrites in cultured neurons. Crebinostat can modulate chromatin-mediated neuroplasticity and exhibits enhanced memory in mice[1].
7-Deaza-2',3'-dideoxyadenosine can be used in the synthesis of oligodeoxyribonucleotides[1].
Palmitic acid-d4-1 is the deuterium labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. PA can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2][3].
Parbendazole-d3 is the deuterium labeled Parbendazole. Parbendazole is a potent inhibitor of microtubule assembly, destabilizes tubulin, with an EC50 of 530 nM, and exhibits a broad-spectrum anthelmintic activity.
Fenofibric acid-d6 (FNF acid-d6) is the deuterium labeled Fenofibric acid. Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 µM, 1.47 µM, and 1.06 µM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
8-Azido-2′-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].
Tubulin polymerization-IN-14 (Compound 20a) is a tubulin polymerization inhibitor with an IC50 of 3.15 μM. Tubulin polymerization-IN-14 shows potent anti-vascular and anticancer activities, induces cancer cell apoptosis[1].
Tubacin is a potent and selective inhibitor of HDAC6, with an IC50 value of 4 nM and approximately 350-fold selectivity over HDAC1.
4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a Kd of 25 μM against eIF4E binding.
Clanfenur is a substituted benzoylphenylurea, an analogue of the pesticide fenfluramide, with potential antineoplastic activity. Clanfenur can bind to the colchicine-binding site on β-tubulin, inhibit microtubule polymerization, and thus prevent tumor cell replication[1].
TH5427 hydrochloride is a potent, selective NUDT5 inhibitor (IC50=29 nM). TH5427 hydrochloride shows an apparent 690-fold selectivity for NUDT5 over MTH1. TH5427 hydrochloride blocks progestin-dependent, PAR-derived nuclear ATP synthesis and subsequent chromatin remodeling, gene regulation and proliferation in breast cancer cells[1].
2’-O-Acetyl-3,5-bis-O-(2,4-dichlorobenzyl)adenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
KPT-9274 is an orally bioavailable, dual PAK4/Nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with IC50s less than 100 and 120 nM, respectively.
Tubulin polymerization-IN-38 a Tubulysin (HY-128914) analogue, is a potent anticancer agent. Tubulin polymerization-IN-38 inhibits tubulin polymerisation and thereby inducing apoptosis. Tubulin polymerization-IN-38 has cytotoxicity against cancer cells[1].
PARP-1/2-IN-1 is a potent PARP-1/2 inhibitor with IC50 of 0.51 nM and 23.11 nM, respectively.
5’-DMTr-dC (Ac)-Methylphosphonamidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
KIRA-7 is a small molecule inhibitor of IRE1α kinase/Rnase with IC50 of 0.11/0.22 uM, allosterically inhibits IRE1α RNase activity; reverses bleomycin-induced fibrosis when given 2 weeks after bleomycin exposure in vivo.
N3-Methyl-2’-O-methyluridine is a uridine analogue. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].
ML372 is a small molecule SMN modulator that increases SMN protein in patient fibroblasts with EC50 of 37 nM; possesses good potency, pharmacokinetics, tolerance, and CNS penetration that are able to increase levels of SMN protein in several model cell lines; increase SMN protein levels in vivo, restore motor function, and prolong survival of SMNΔ7 SMA Mice; improves the righting reflex and extended survival of a severe mouse model of SMA.
7-(2,3-Anhydro-β-D-ribofuranosyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine is a purine nucleoside analogue. 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].
HBV-IN-15 is a potent inhibitor of covalently closed circular DNA (cccDNA). cccDNA serves as the template for viral RNA transcription and subsequent viral DNA generation. HBV-IN-15 is a flavone derivative. HBV-IN-16 has the potential for the research of HBV infection (extracted from patent WO2020052774A1, compound 2)[1].
4'-Methoxychalcone regulates adipocyte differentiation through PPARγ activation. 4'-Methoxychalcone modulates the expression and secretion of various adipokines in adipose tissue that are involved in insulin sensitivity[1].
Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage, with an IC50 of 80 nM. Toyocamycin (Vengicide) induces apoptosis. Toyocamycin (Vengicide) shows no effect on IRE1α auto-phosphorylation[1].
2-Amino-3’-deoxy-3’-fluoroadenosine is a purine nucleoside analogue. 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].
2’-O-Methyl-5-iodouridine (5-Iodo-2'-O-methyluridine) 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].