N1-(1,1,1-Trifluoroethyl)pseudouridine 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].
L-2'-Fd4C, is an l-nucleoside analogue. L-2'-Fd4C has anti-human immunodeficiency virus (HIV) and anti-hepatitis B virus (HBV) activity[1].
PLK1-IN-7 (compound 30e) is a potent PLK1 inhibitor, with an IC50 of 0.66 nM. PLK1-IN-7 exhibits antiproliferative and antitumor activities[1].
XPW1 is a potent and selective CDK9 inhibitor with excellent activity against clear cell renal cell carcinoma (ccRCC) and low toxicity[1].
7-n-Propyl-7,8-dihydro-8-oxo-9-(β-D-xylofuranosyl)guanine 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].
DMTr-LNA-U-3-CED-phosphora is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
Cimpuciclib is a cyclin-dependent kinase(CDK) inhibitor and antineoplastic[1].
Tubulin polymerization-IN-22 is a tubulin polymerization inhibitor with an IC50 of 8.1 μM. Tubulin polymerization-IN-22 arrests cell cycle at G2/M phase and induces apoptosis[1].
VE-465 is an Aurora kinase inhibitor. VE-465 induces cancer cell apoptosis. VE-465 has anticancer effects in multiple tumor models[1][2].
3’-Azido-3’-deoxy-5-fluoro-beta-L-cytidine 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].
BOLD-100 is a ruthenium-based anticancer agent. BOLD-100 also is an inhibitor of stress-induced GRP78 upregulation, disrupting endoplasmic reticulum (ER) homeostasis and inducing ER stress and unfolded protein response (UPR). BOLD-100 interferes with the complex interplay between ER-stress response, lysosome dynamics, and autophagy execution[1].
S26948 is a specific peroxisome proliferator-activated receptor γ (PPARγ) modulator (EC50=8.83 nM) with potent antidiabetes and antiatherogenic effects. S26948 is a specific high-affinity agonist for PPARγ[1].
Mc-MMAF is a protective group-conjugated MMAF. MMAF is a more potent drug than Monomethyl auristatin E (MMAE), but is charged and relatively membrane-impermeable, is a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate.Target:MMAF is a new auristatin derivative with a charged C-terminal phenylalanine that attenuates its cytotoxic activity compared to its uncharged counterpart, Monomethyl auristatin E (MMAE). Because of MMAF is highly toxic, it cannot be used as a drug itself. MMAF induces potent antitumor effects when conjugated via protease cleavable linkers to a monoclonal antibody targeting internalizing, tumor-specific cell surface antigens. The linker to the monoclonal antibody is stable in extracellular fluid, but is cleaved by cathepsin once the conjugate has entered a tumor cell, thus activating the anti-mitotic mechanism.
G-5555 is a potent p21-activated kinase 1 (PAK1) inhibitor with Kis of 3.7 nM and 11 nM for PAK1 and PAK2, respectively.
CP-67015, a nalidixic acid analog, is a potent topoisomerase II inhibitor. CP-67015 is a positive direct-acting mutagen in mammalian cells with both gene and chromosomal level effects[1].
Tubulin polymerization-IN-25 (compound 17f) is a dual inhibitor of tubulin polymerization and farnesyl transferase (FTase) with IC50s of 1.11 μM and 0.39 μM, respectively. Tubulin polymerization-IN-25 displays cytotoxicity and excellent antitumor activity [1].
3’-O-MOE-U-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].
Lacto-N-fucopentaose I (LNFPI) is a human milk oligosaccharide (HMO), possessing antiviral and antibacterial activity. Lacto-N-fucopentaose I can reduce capsid protein VP1 to block virus adsorption, promote CDK2 and reduce cyclin E to recover cell cycle S phase block. Lacto-N-fucopentaose I inhibits ROS production and apoptosis in virus-infected cells. Lacto-N-fucopentaose I can also regulate intestinal microbiota to affect immune system development[1].
Geldanamycin is a Hsp90 inhibitor with antimicrobial activity against many Gram-positive and some Gram-negative bacteria.
Gnetol is a phenolic compound isolated from the root of Gnetum ula Brongn. Gnetol potently inhibits COX-1 (IC50 of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC50 of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities[1][2][3].
SIRT2/6-IN-1 (Compound 5) is a SIRT6/SIRT2 inhibitor, with IC50s of 106 μM and 114 μM. SIRT2/6-IN-1 increases H3K9 acetylation, increases glucose uptake and reduces TNF-α secretion in cells[1].
Cdc7-IN-18 (compound 1-2) is a potent CDC7 inhibitor with an IC50 of 1.29 nM for Cdc7/DBF4 enzyme. Cdc7-IN-18 shows antiproliferative activities with IC50 of 53.62 nM in COLO205 cells[1].
3’-O-(2-Methoxyethyl)-5-methyluridine is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
Deoxyguanosine triphosphate (dGTP) trisodium salt is a nucleotide precursor in cells for DNA synthesis. Deoxyguanosine triphosphate trisodium salt is used in reverse transcription-polymerase chain reaction (RT-PCR) for DNA amplification[1].
ZDLD13, a β-carboline, is an orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 0.38 μM. ZDLD13 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD13 shows significant tumor growth inhibition in HCT116 tumor xenograft model[1].
Tubulin inhibitor 33, a tubulin polymerization inhibitor, inhibits tubulin polymerization in a dose-dependent manner with an IC50 of 9.05 μM. Tubulin inhibitor 33 has antitumor effects and induces cell apoptosis that can be used for antitumor research[1].
A potent, selective inhibitor of cdc2-like kinase CLK1 and CLK2 with IC50 of 1.1 and 2.4 nM, respectively; moderately inhibits PI3Kα, and >100-fold selectivity over SRPK1/2/3; inhibits phospho-SRSF4 in MDA-MB-468 cells, induces alternative splicing of the S6K pre-mRNA at 1.1-3.3 uM, exhibits growth inhibitory activity with GI50 of 3.0 uM, through splicing alterations in genes involved in growth and survival.
CCT241533 dihydrochloride is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM[1].
ddTTP is one of 2',3'-dideoxyribonucleoside 5'-triphosphates (ddNTPs) that acts as chain-elongating inhibitor of DNA polymerase for DNA sequencing[1].
A potent, specific, allosteric and cell-active inhibitor of KSP with IC50 of 11 nM; has no ihibitory activity toward other kinesins, includin CENP-E, MKLP-1, KIF-3A, and uKHC (IC50>50 uM); induces the formation of monoastral spindles, causes mitotic arrest in a dose-dependent manner (EC50=30 nM) in A2780 ovarian carcinoma cells; sustained KSP inhibition activates the proapoptotic protein, Bax, and both activation of the spindle checkpoint and subsequent mitotic slippage are required for Bax activation.