KDM2/7-IN-1 (TC-E 5002) is a selective histone demethylase KDM2/7 subfamily inhibitor (IC50 values are 0.2, 1.2, 6.8, 55, 83, >100 and >120 μM for KDM7A, KDM7B, KDM2A, KDM5A, KDM4C, KDM6A and KDM4A respectively). KDM2/7-IN-1 inhibits growth of HeLa and KYSE-150 cancer cells in vitro[1].
Angophorol is a flavonone compound. Angophorol exerts potential anticancer activity through growth inhibition and apoptosis in K562 cells[1].
N3-PEG2-C2-PFP ester is a nonclaevable 2-unit PEG linker used in the synthesis of antibody-drug conjugates (ADCs).
AGI-5198 is a potent and selective mutant IDH1R132H inhibitor with an IC50 of 0.07 μM.
8-Azaguanine is a purine analogue which shows antineoplastic activity.
Isobutylquinoleine is a fragrance ingredient[1].
Sudocetaxel is a microtubule depolymerization inhibitor for pH-sensitive docetaxel delivery.
N3PT(N3-pyridyl thiamine) is a potent and selective transketolase(TK) inhibitor (IC50= 22 nM for Apo-TK) both in vitro and in vivo.IC50 Value: 22 nM( Apo-TK) ; 26 nM (EC50, Cellular TK) [1]Target: transketolasein vitro: N3PT inhibits transketolase activity in a cell based assay. Competitive inhibition of TK by N3PT in cells treated with increasing doses of thiamine, expressed as percentage enzymatic activity (the slope of initial linear range) of controls not treated with compounds [1].in vivo: Tumors were induced in mice at day 0 and mice were then treated at day 7 with vehicle alone or with N3PT [2]. Low-thiamine diet enhances the sensitivity to N3PT inhibition of TK in spleen. Animals were switched to diets containing 16.5 mg/kg (unchanged), 5 mg/kg, 1 mg/kg, or 0 mg/kg thiamine, from a normal chow containing 16.5mg/kg thiamine [1].
8-Methoxyadenosine 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].
MT-VC-ZD02044 is a cytotoxic and anti-mitotic agent[1].
BDP FL-PEG5-acid is a BDP FL acid linker containing a hydrophilic PEG spacer arm. BDP FL-PEG5-acid can be used in the synthesis of PROTACs. BDP FL is a green-fluorescent dye, and the hydrophilic PEG spacer arm increases water solubility and membrane permability.
HER2/neu (654-662) GP2 is a nine amino acid peptide derived from the human epidermal growth factor receptor 2 (HER2/nue, 654–662), induces HLA-A2-restricted cytotoxic T lymphocytes (CTL) reactive to various epithelial cancers[1][2].
IDO1-IN-19 (Compound 17) is a potent inhibitor of IDO1. IDO1-IN-19 has the potential for the research of cancer diseases[1].
Mycro2 is an inhibitor of c-Myc/Max dimer and DNA binding, with an IC50 value of 23 μM for the inhibition of Myc/Max DNA binding activity. Mycro2 can inhibit c-myc-dependent cell proliferation, gene transcription and oncogenic transformation[1].
Myosin light chain kinase fragment 11-19 amide (MLCK(11-19) amide) is a substrate-specific peptide inhibitor of MLCK. Myosin light chain kinase fragment 11-19 amide inhibits hypotonicity-induced Ca2+ entry. Myosin light chain kinase fragment 11-19 amide can be used in the research of human cervical cancer[1][2].
Onfekafusp alfa (L19TNF) is a homotrimer that forms from engineered peptides for the L19 antibody in scFv format fused to human TNF. Onfekafusp alfa can be used for malignant glioma research[1][2].
Microtubule inhibitor 5 (compound 17f) is a potent microtubule inhibitor. Microtubule inhibitor 5 shows cytotoxicity with an IC50 value of 154.5 nM for NCI-H460 cells. Microtubule inhibitor 5 shows good cell permeability[1].
Dehydrotrametenolic acid is a sterol isolated from the sclerotium of Poria cocos. Dehydrotrametenolic acid induces apoptosis through caspase-3 pathway. Dehydrotrametenolic acid has anti-tumor activity, anti-inflammatory, anti-diabetic effects[1].
Lenalidomide-4-aminomethyl hydrochloride is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-4-aminomethyl hydrochloride can be connected to the ligand for protein by a linker to form PROTAC[1]
Pacritinib hydrochloride is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib hydrochloride also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM). Pacritinib hydrochloride can be used for the research of acute myeloid leukemia (AML) and myelofibrosis (MF)[1][2][3].
ARB-272572 is a potent small-molecule PD-L1 inhibitor with an IC50 value of 400 pM.
Periplocin is a cardiotonic steroid isolated from Periploca forrestii. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase[1][2].
LY3009120 is a pan RAF inhibitor which inhibits BRAFV600E, BRAFWT and CRAFWT with IC50s of 5.8, 9.1 and 15 nM, respectively.
NSC23925 is a novel, selective and effective P-glycoprotein (Pgp) inhibitor.
CC-90003 is an irreversible and selective inhibitor of ERK 1/2 with antitumor activity.
Hematin, an iron-containing porphyrin, inhibits the activity of clotting factors and also fibrin clot lysis through the mechanism of binding to and inactivation of hemostatic proteins[1]. Hematin can be used for the research of acute porphyrias and cancer[1][2][3][4][5].
UNC-926 is a methyl-lysine (Kme) reader domain inhibitor; inhibits L3MBTL1 with an IC50 of 3.9 μM.
Mps-BAY2a is a monopolar spindle 1 (MPS1) inhibitor with an IC50 of 1 nM against human MPS1. Mps-BAY2a induces mitotic aberrations and apoptosis in cancer cells[1].
3,3',5-Triiodo-L-thyronine sodium is an active form of thyroid hormone, which binds to β1 thyroid hormone receptor (TRβ1), and activates its activity.