AR03 (BMH-23) is an apurinic/apyrimidinic endonuclease 1 (Ape1) inhibitor with an IC50 of 2.1 µM. AR03 has low affinity for double-stranded DNA. AR03 potentiates the cytotoxicity of methyl methanesulfonate and temozolomide in SF767 cells[1].
Troglitazone is a PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively.
Casein Kinase II Receptor Peptide is a substrate for casein kinase II with an Km value of 500 µM. Casein Kinase II Substrate can be used for measure casein kinase II activity in crude enzyme preparations[1].
N2-Phenoxyacetylguanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].
2,4-D-d3 is the deuterium labeled 2,4-D[1]. 2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development[2].
Mauritianin is a kaempferol glycoside isolated from the flowers and leaves of Acalypha indica. Mauritianin is a topoisomerase I inhibitor[1][2].
Luotonin A is an antiviral and antiphytopathogenic fungus agent. Luotonin A has good antiviral activity against tobacco mosaic virus (TMV). Luotonin A also has certain inhibitory activity on topoisomerase I and topoisomerase II. Luotonin A shows antitumor activity[1][2].
SCH900776 is a potent, selective and oral inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. It shows 50- and 500-fold selectivity over CDK2 andChk2, respectively.
CDK5-IN-3 (compound 11) is a potent and selective CDK5 inhibitor, with IC50s of 0.6 nM and 18 nM for CDK5/p25 and CDK2/CycA, respectively. CDK5-IN-3 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD)[1].
NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma)[1].
GW 501516 is a PPARδ agonist with an EC50 of 1.1 nM.
Palifosfamide (tromethamine) is a synthetic alkylating agent with potential antineoplastic activity. As the stabilized active metabolite of ifosfamide, palifosfamide (tromethamine) irreversibly alkylates and crosslinks DNA through GC base pairs. This leads to an inhibition of DNA replication and ultimately cell death. Compared to ifosfamide, palifosfamide (tromethamine) is less toxic.
ROCK-IN-D2 is an effective and selective inhibitor of ROCK.
Antitumor agent-63 (Compound 40), a 20 (S)-O-linked camptothecin (CPT) glycoconjugate, is an antitumor agent without toxicity towards normal cells. Antitumor agent-63 shows high stability and very weak direct topoisomerase I (Topo I) inhibition[1].
Cyclophosphamide-d8 is deuterium labeled Cyclophosphamide. Cyclophosphamide is a synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic activity, a immunosuppressant.
SKLB0565 is a potent tubulin inhibitor. SKLB0565 shows significant anti-proliferative activity against CRC (colorectal carcinoma) cell lines, with IC50 values ranging from 0.012 μM to 0.081 μM. SKLB0565 causes G2/M phase arrest and mitochondria-mediated intrinsic apoptosis. SKLB0565 inhibits cell migration and disrupted the tube formation of HUVECs[1].
AZD-7648 is a potent and selective DNA-PK inhibitor. Anti-tumour activity[1].
Butyric acid-13C1 is the 13C labeled Butyric acid. Butyric acid is a histone deacetylase (HDAC) inhibitor, with anti-tumor effects in several cancers.
4’-α-C-Methylcytidine 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].
Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM[1].
Pyridostatin is a G-quadruplexe stabilizer, with a Kd of 490 nM.
NW 1028 is a potent VCP/p97 inhibitor. NW 1028 targets the ND1L domain of p97 and inhibits the degradation of a p97-dependent reporter. NW 1028 has good binding affinity with Kd values of 100 and 285 nM for ND1L and full length p97, respectively. NW 1028 has the function of regulating the mitotic spindle of cells[1].
2’-Azido-2’-deoxy-5’-O-(4,4’-dimethoxytrityl)-5-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].
Epigenetic factor-IN-1 (40569Z) is a epigenetic factor inhibitor. Epigenetic factor-IN-1 has strong binding effect on SIRT7. Epigenetic factor-IN-1 can be used for liver cancer research[1].
3',4'-Dimethoxyflavone is a lipophilic flavone, can be isolated from the leaves of Primula veris. 3',4'-Dimethoxyflavone can reduce the synthesis and accumulation of PARP and protect cortical neurones against cell death induced by Parthanatos. 3',4'-Dimethoxyflavone is also an aryl hydrocarbon receptor antagonist in human breast cancer cells. 3',4'-Dimethoxyflavone can promote the proliferation of human hematopoietic stem cells. 3',4'-Dimethoxyflavone has various biological activities, including antioxidant, anti-cancer, anti-inflammatory, anti-atherogenic, hypolipidaemic, and neuroprotective or neurotrophic effects[1][2][3][4].
2’-Deoxy-N1-methylguanosine 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].
Fenofibrate is a PPARα agonist with an EC50 of 30 μM.
DMT-2'-F-dA Phosphoramidite is a phosphoramidite that can be used in the synthesis of oligonucleotides.
Cemdomespib (KU-596) is a highly bioavailable second-generation Hsp90 modulator. Cemdomespib has shown efficacy in improving sensory deficits in models of diabetic peripheral neuropathy. Cemdomespib induces Hsp70 levels and manifest neuroprotective activity through induction of the heat shock response[1][2][3].
CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histonedeacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform[1].