Casein kinase 1δ-IN-3 (Compound 23a) is a casein kinase 1 delta (CK1d) inhibitor with a pIC50 of 6.5376 M[1].
BAY-707 is a highly potent, selective and substrate-competitive inhibitor of MTH1 (NUDT1) with IC50 of 2.3 nM; demonstrates high selectivity in an in-house kinase panel, and shows an overall favorable physicochemical profile and in vitro pharmacokinetic properties with high metabolic stability; demonstrates a superior cellular target engagement with an EC50 of 7.6 nM compared with TH588, increases the cellular thermal stabilization of MTH1 with no effect on the expression of MTH2, OGG1, and MUTYH; shows a clear lack of in vitro or in vivo anticancer efficacy either in mono- or in combination therapies in vivo.
PF-3758309 is an inhbitor of PAK with IC50 of 1.3 nM for PAK4.
KU-55933 is a potent ATM inhibitor with an IC50 and Ki of 12.9 and 2.2 nM, respectively, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.
5’-O-(4,4’-Dimethoxytrityl)-3’-O-methyluridine is a uridine analog. 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].
DMTr-TNA-G(O6-CONPh2)(N2Ac)-amidite 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].
2-Methoxy-9-β-D-ribofuranosyl-9H-purine 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].
PCLX-001 is an orally acitve, small-molecule, dual N-myristoyltransferase (NMT) inhibitor, with IC50s of 5 nM (NMT1) and 8 nM (NMT2), respectively. PCLX-001 exhibits anti-tumor activity and inhibits early B-cell receptor (BCR) signaling, can be used to B-cell malignancies research[1][2].
T0070907 is a potent PPARγ antagonist with a Ki of 1 nM.
MLN0905 is a potent PLK1 inhibitor, with an IC50 of 2 nM.
Procarbazine Hydrochloride is an alkylating agent, with anticancer activity.
5-Hydroxy-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].
LTURM34 is a specific DNA-PK inhibitor with an IC50 of 0.034 μM.
5-Methoxy-2-thiouridine 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].
SNS-314 is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively[1].
Idarubicin hydrochloride is an anthracycline antileukemic drug. It inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription.
Plinabulin (NPI-2358) is a vascular disrupting agents (VDA) against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells.IC50 Value: 9.8~18 nMTarget: Microtubule/Tubulinin vitro: NPI-2358 binds to the colchicine-binding site of tubulin and has potent inhibitory to human tumor cell lines which have overexpressed Pgp or reduced nuclear Topo II catalytic activity, with IC50 from 9.8 to 18 nM. NPI-2358 is able to rapidly induce tubulin depolymerization in HUVECs and monolayer permeability even at 20 nM. NPI-2358 induces cell death in MM cells with IC50 of 8-10 nM, which due to trigger early mitotic arrest in MM cells. NPI-2358 also inhibits tubule formation and migration of endothelial as well as MM cells, which leads to disrupt tumor vasculature. NPI-2358 could induces cell death in patient MM (CD138+) cells without effecting viability of normal mononuclear cells. Blockade of JNK abrogates NPI-2358-induced mitotic arrest or MM cell death. in vivo: NPI-2358 (7.5 mg/kg) inhibits tumor growth in human plasmacytoma mouse xenograft models at well-tolerated doses. NPI-2358 induces a time- and dose-dependent decrease in tumour perfusion. NPI-2358 is more sensitive to the KHT sarcoma than the C3H tumour, while radiation response could enhance the antitumor activity in both models.
Eribulin mesylate is a microtubule targeting agent that is used in the treatment of metastatic breast cancer. It inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules.
Tubulin polymerization-IN-9 is a potent tubulin inhibitor with IC50 of 1.82 μM. Tubulin polymerization-IN-9 causes cell cycle arrest at G2/M phase, and induces cell apoptosis and depolarized mitochondria of K562 cells. Tubulin polymerization-IN-9 has potent anti-vascular and antitumor activities[1].
Py-MAA-Val-Cit-PAB-DX8951 is a purine toxin. Py-MAA-Val-Cit-PAB-DX8951 can be used as an intermediate in the synthesis of antibody-drug conjugates[1].
Palmitic acid-1,2,3,4-13C4 is the 13C-labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid 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].
SJG-136 is a DNA cross-linking agent, with an XL50 of 45 nM for pBR322 DNA; SJG-136 has potent antitumor activity.
Aurora kinase inhibitor-10 (Compound 6c) is an orally active Aurora B inhibitor with an IC50 of 8 nM. Aurora kinase inhibitor-10 shows antitumor activity[1].
N6-Benzoyl-3’-O-(2-methoxyethyl)adenosine 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].
CRT0066854 hydrochloride is a potent and selective atypical PKCs inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC50 values of 132 nM, 639 nM, and 620 nM, respectively[1].
2-Bromo-6-chloro-9-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)-9H-purine 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].
Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin[1].
L-Fd4A is an adenine derivative. L-Fd4A has anti-human immunodeficiency virus (HIV) (EC50=1.5 μM) and anti-hepatitis B virus (HBV) (EC50=1.7 μM) activity. L-Fd4A has low cytotoxicity[1].
9-(3-Deoxy-3-fluoro-β-D-ribofuranosyl)-6-methyl-9H-purine 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].