Thalidomide-O-C3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
FGFR-IN-5 is a potent inhibitor of FGFR. Fibroblast growth factor receptor (FGFR) is a tyrosine kinase receptor that binds to fibroblast growth factor ligands. FGFR-IN-5 has the potential for the research of cancer diseases (extracted from patent WO2022042612A1, compound 3)[1].
(E/Z)-Necrosulfonamide is a racemic compound of Necrosulfonamide (HY-100573). Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis[1][2].
Encelimab is an anti-LAG3 antibody. Encelimab blocks the interaction between LAG-3 and MHC II, and enhances T-cell activation. Encelimab alone or in combination with an anti-PD-1 antibody reduces tumor size in a lymphoma mice model (A20 cell xenograft)[1].
Complanatoside A is a flavonol glycoside isolated from Astragalus complanatus, and currently it is used as a quality control index for A. complanatus in the 2010 edition of the Chinese Pharmacopoeia.
Cdc7-IN-8 is a potent inhibitor of Cdc7. Cdc7 is a serine/threonine kinase which activates MCM promotion by phosphorylating the microchromosome maintenance protein (MCM protein), an important element of the DNA replication initiator. Cdc7-IN-8 has the potential for the research of cancer diseases (extracted from patent WO2021032170A1, compound 1-1/1-2)[1].
N4-Benzoyl-3’-deoxycytidine 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].
(-)-Heraclenol is a derivative of furocoumarin isolated from Ducrosia anethifolia. (-)-Heraclenol shows antiproliferative and cytotoxic activities on cancer cell lines[1].
Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1[1].
Alloxazine is a selective A2b antagonist. Alloxazine can completely block 5’N-Ethylcarboxamido adenosine (NECA)-mediated cyclic AMP accumulation with an IC50 of 2.9 μM. Alloxazine can be used for the research of cancer[1][2].
2-Deoxy-2’-fluoroisocytidine 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].
TRK-IN-21 (5n) is an orally activity TRK inhibitor. TRK-IN-21 inhibits TRKAWT, TRKAG667C, TRKAF589L, and TRKAG595 with IC50s of 0.3, 2.3, 0.4 and 0.5 nM, respectively. TRK-IN-21 can be used for the research of cancer[1].
Momelotinib (CYT387) sulfate is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).
TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is a potent serine protease inhibitor that reacts with the retinoblastoma protein (RB)-binding core of HPV-18 E7 protein and abolish its RB-binding capability. TPCK is able to modify E7 protein in live keratinocytes following its addition to the culture medium[1].
sulfo-DGN462 sodium is degraded to DGN462 in culture medium and plasma. DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML)[1].
D-Glucose-13C,d1 is the deuterium and 13C labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical sig
MMAF (Monomethylauristatin F) is an antitubulin agent that inhibit cell division; inhibits H3397 cell growth with an IC50 of 105 nM.
ATM-3507 is a potent tropomyosin inhibitor with IC50s from 3.83-6.84 μM in human melanoma cell lines.
IRAK4-IN-13 (compound 21) is a potent and selective IRAK4 inhibitor with an IC50 of 0.6 nM. IRAK4-IN-13 shows high metabolic clearance with human liver microsomes (HLM) intrinsic clearance is 96 µL/min/mg[1].
CBLB 612 is an anti-radiation auxiliary agent and anti-tumor agent[1].
Tos-PEG4-CH2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Oprozomib (ONX 0912; PR047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.IC50 value: 36 nM/82 nM(20S proteasome β5/LMP7) [1]Target: 20S proteasomeThe anti-MM activity of Oprozomib is associated with activation of caspase-8, caspase-9, caspase-3, and PARP, as well as inhibition of migration of MM cells and angiogenesis. Oprozomib is demonstrated an absolute bioavailability of up to 39% in rodents and dogs. It is well tolerated with repeated oral administration at doses resulting in >80% proteasome inhibition in most tissues and elicited an antitumor response in multiple human tumor xenograft and mouse syngeneic models.
ODM-204 is novel nonsteroidal dual inhibitor of both androgen receptor and CYP17A1 enzyme, with IC50s of 80 nM and 22 nM, respectively.
Tubulin polymerization-IN-28 (compound-4) is a microtubule protein polymerization inhibitor with highly selective anticancer activity. Tubulin polymerization-IN-28 can be activated by NQO1 and effectively release combretastatin A-4 to kill tumor cells. Tubulin polymerization-IN-28 can induce cell apoptosis and be used in anti-cancer research[1].
GLPG0634 (analog) (compound176)is a pan JAK inhibitor with IC50s of 50-200 nM for JAK1/JAK2/JAK3; more information can be found in the reference patents.
JG-231 is an allosteric inhibitor that disrupts the Hsp70-BAG3 interaction (Ki=0.11 uM), inhibits breast cancer cells MCF-7 and MDA-MB-231 with IC50 of 0.12 and 0.25 uM, respectively; reduces tumor burden in an MDA-MB-231 xenograft model (4 mg/kg, ip).
Me-Tet-PEG4-NH2 is an ADC Linker containing 4 PEG units. Me-Tet-PEG4-NH2 can use its own Tetrazine group to undergo a specific inverse electron demand Diels-Alder reaction (iEDDA) with compounds with TCO groups.
HO-3867 is a selective and potent STAT3 inhibitor and shows good antitumor activity.
Koaburaside is a cytoprotective and anti-inflammatory natural compound. Koaburaside shows antioxidant activity with an IC50 of 9.0 μM for DPPH-free radical scavenging assay. Koaburaside inhibits histamine release and expressions of IL-6 and TNF-α in human mast cells. Koaburaside also effectively inhibits influenza A neuraminidase[1].
3’-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].