Formylmelphalan was approved in China for treating cancer. Formylmelphalan is an alkylating agents, which could cross-link DNA.

Flutamide, also known as SCH13521, is a toluidine derivative and nonsteroidal antiandrogen that is structurally related to bicalutamide and nilutamide. Flutamide and its more potent active metabolite 2-hydroxyflutamide competitively block dihydrotestosterone binding at androgen receptors, forming inactive complexes which cannot translocate into the cell nucleus. Formation of inactive receptors inhibits androgen-dependent DNA and protein synthesis, resulting in tumor cell growth arrest or transient tumor regression. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Floxuridine is a fluorinated pyrimidine monophosphate analogue of 5-fluoro-2'-deoxyuridine-5'-phosphate (FUDR-MP) with antineoplastic activity. As an antimetabolite, floxuridine inhibits thymidylate synthetase, resulting in disruption of DNA synthesis and cytotoxicity. This agent is also metabolized to fluorouracil and other metabolites that can be incorporated into RNA and inhibit the utilization of preformed uracil in RNA synthesis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Estramustine phosphate sodium is a synthetic molecule that combines estradiol and nornitrogen mustard through a carbamate link. Estramustine and its major metabolite estramustine bind to microtubule-associated proteins (MAPs) and tubulin, thereby inhibiting microtubule dynamics and leading to anaphase arrest in a dose-dependent fashion. This agent also exhibits anti-androgenic effects. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Degarelix, also known as FE-200486 and ASP-3550, is a long-acting, synthetic peptide with gonadotrophin-releasing hormone (GnRH) antagonistic properties. Degarelix targets and blocks GnRH receptors located on the surfaces of gonadotroph cells in the anterior pituitary, thereby reducing secretion of luteinizing hormone (LH) by pituitary gonadotroph cells and so decreasing testosterone production by interstitial (Leydig) cells in the testes. Degarelix acetate was approved in 2008.

Carmofur (INN) or HCFU (1-hexylcarbamoyl-5-fluorouracil) is a pyrimidine analogue used as an antineoplastic agent. It is a derivative of fluorouracil.

Bicalutamide is a synthetic, nonsteroidal antiandrogen. Bicalutamide competitively binds to cytosolic androgen receptors in target tissues, thereby inhibiting the receptor binding of androgens. This agent does not bind to most mutated forms of androgen receptors.

Amsacrine is an aminoacridine derivative with potential antineoplastic activity. Although its mechanism of action is incompletely defined, amsacrine may intercalate into DNA and inhibit topoisomerase II, resulting in DNA double-strand breaks, arrest of the S/G2 phase of the cell cycle, and cell death. This agent's cytotoxicity is maximal during the S phase of the cell cycle when topoisomerase levels are greatest. In addition, amsacrine may induce transcription of tumor promoter p53 protein and block p53 ubiquitination and proteasomal degradation, resulting in p53-dependent tumor cell apoptosis.

Aclarubicin is an oligosaccharide anthracycline antineoplastic antibiotic isolated from the bacterium Streptomyces galilaeus. Aclarubicin intercalates into DNA and interacts with topoisomerases I and II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. Aclarubicin is antagonistic to other agents that inhibit topoisomerase II, such as etoposide, teniposide and amsacrine. This agent is less cardiotoxic than doxorubicin and daunorubicin.

Asulam is a wild oat herbicide used in prairie regions for control of wild oats in cereal grains such as wheat.

Px-104(Px-102) is a farnesoid X receptor (FXR) agonist potentially for the treatment of non-alcoholic fatty liver disease.

NSC-87877 is a cell-permeable inhibitor of both SHP-1 and SHP-2 with IC50 values of 355 and 318 nM respectively. It also inhibits EGF-induced Erk1/2 activation in HEK293 cells and significantly reduces MDA-MB-468 cell viability/proliferation.

WZ8040-hydroxy is a WZ8040 (MedKoo Cat#406574) derivative or analog molecule. Compared to WZ8040, WZ8040-hydroxy has an extra hydroxy group in the benzene ring. WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor with potential anticancer activity. WZ8040 is about 30-fold more potent against EGFR T790M, and up to 100-fold less potent against wild-type EGFR, than other quinazoline-based EGFR inhibitors such as CL-387785 and HKI-272. WZ-8040 may be clinically more effective and better tolerated than quinazoline-based inhibitors.

WZ4002-hydroxy is a WZ4002 (MedKoo Cat#: 203170) derivative or WZ4002 analog. In which the methoxy group is replaced by hydroxy group. WZ4002 is EGFR inhibitor against EGFR T790M (mutation of the gatekeeper T790 residue) which is detected in 50% of clinically resistant patients to gefitinib or erlotinib. WZ4002 has a basic chemical framework (covalent pyrimidine) which is different from that of other EGFR inhibitors.

Paclitaxel-MVCP, also known as MC-Val-Cit-PAB-Paclitaxel, is a paclitaxel derivative with a MC-Val-Cit-PAB linker. Mc-Val-Cit-PAB is a cathepsin cleavable ADC peptide linker. Paclitaxel-MVCP can be used to conjugate with other molecules such as peptides, proteins, antibodies or enzymes, or polymers. Paclitaxel-MVCP is a useful agent to make Paclitaxel-conjugate for drug delivery, nanodrug research.

Spiromesifen is a useful insecticide and miticide in plant breeding. It is particuarly useful against spider mites and whiteflies in vitro.

Chloroguanabenz acetate is an antiprion agent. It is derived from the α2-adrenergic receptor agonist guanabenz. Chloroguanabenz reduces the levels of both soluble and aggregated forms of the truncated Huntingtin derivative Htt48 in an HEK293T cellular model of Huntington’s disease.

N-desmethyl Rosuvastatin sodium salt hydrate is an active metabolite of the HMG-CoA reductase inhibitor Rosuvastatin. N-desmethyl Rosuvastatin is formed when Rosuvastatin undergoes demethylation, primarily by the cytochrome P450 (CYP) isoform CYP2C9 and to a lesser extent by CYP2C19 and CYP3A4.

4-hydroxy Nebivolol HCl is a major metabolite of nebivolol. It is formed by the hydroxylation of nebivolol by the cytochrome P450 (CYP) isoform CYP2D6.

Sitagliptin N-sulfate is a phase II metabolite of the dipeptidyl peptidase 4 (DPP-4) inhibitor (-)-sitagliptin. Sitagliptin N-sulfate is formed via sulfation.

Moxifloxacin N-sulfate is a metabolite of Moxifloxacin --- a fluoroquinolone antibiotic. Formulations containing moxifloxacin have been used in the treatment of bacterial infections such as sinusitis, chronic bronchitis, and pneumonia.

Tenofovir diphosphate sodium salt is an inhibitor of HIV reverse transcriptase and hepatitis B virus (HBV) polymerase. It is selective for these enzymes over DNA polymerase α and β, as well as mitochondrial DNA polymerase γ. Tenofovir diphosphate is formed intracellularly through phosphorylation of the prodrugs tenofovir and tenofovir disoproxil by nucleotide kinases. Increased levels of tenofovir diphosphate in isolated peripheral blood mononuclear cells (PBMCs) correlate with a decrease in the risk of simian HIV (SHIV) acquisition in a macaque model of rectal SHIV transmission.

NG-25 HCl hydrate is a type II kinase inhibitor that inhibits MAP4K2 and TAK1. It also inhibits the Src family kinases Src and LYN and Abl family kinases as well as CSK, FER, and p38α. NG 25 prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively. NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration-dependent manner. It also reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12D mouse orthotopic model of colorectal cancer.

YnMyr Diazirine X10 is a cell-permeable photoreactive probe for protein myristoylation.1,2 It contains a terminal clickable alkyne moiety and a photoactivatable diazirine group at carbon 10 that allow its incorporation into myristylated proteins and photo-activated cross-linking of their interacting partners, respectively.

Avanafil metabolite M16 is a major inactive metabolite of the phosphodiesterase 5 (PDE5) inhibitor avanafil. Avanafil is metabolized by the cytochrome P450 (CYP450) isoforms CYP3A4 and CYP2C to the major metabolites avanafil metabolite M16 and avanafil metabolite M4 as well as minor metabolites.

Avanafil metabolite M4 is a major active metabolite of the phosphodiesterase 5 (PDE5) inhibitor avanafil. Avanafil is metabolized by the cytochrome P450 (CYP450) isoforms CYP3A4 and CYP2C to the major metabolites avanafil metabolite M4 and avanafil metabolite M16 as well as minor metabolites. Avanafil metabolite M4 inhibits PDE5 with 18% of the potency of avanafil.

UF-17 HCl is an analytical reference standard that is structurally similar to known utopioids.

K-TMZ is a DNA alkylating agent. It increases the concentration of O6-methylated deoxyguanosine in U87 glioblastoma multiforme (GBM) cells in a concentration-dependent manner. K-TMZ reduces cell viability of GBM cell lines lacking or expressing O6-methylguanine DNA methyltransferase (MGMT).

MAGL Inhibitor Compound 23 is an inhibitor of monoacylglycerol lipase (MAGL). It is selective for MAGL over cannabinoid receptor 1 (CB1), CB2, fatty acid amide hydrolase (FAAH), α/β-hydrolase domain-containing protein 6 (ABHD6), and ABHD12. MAGL inhibitor compound 23 inhibits the growth of HCT116, MDA-MB-231, Caov-3, OVCAR-3, and SKOV3 cells but not MRC5 cells. It increases the levels of 2-arachidonoyl glycerol (2-AG) in mouse brain and plasma when administered at a dose of 50 mg/kg.

MGR2 is a negative control compound for the activity of the reactive oxygen species-generating probe MGR1. Unlike MGR1, MGR2 does not induce superoxide production or cell death in HEK293T cells.