5-Methyl-5,6-dihydrouridine is a minor constituent in the chromosomal RNA of the rat ascites tumor. 5-Methyl-5,6-dihydrouridine can be used for nucleic acid modification.

5-Aminouridine can modify nucleobases and can be incorporated into the target DNA. 5-Aminouridine exhibits a wide range of biological activity and it inhibits the growth of tumors, fungi and viruses.

5-Hydroxy-2'-deoxyuridine (5-OHdU) is a major stable oxidation product of 2'-Deoxycytidine. 5-Hydroxy-2'-deoxyuridine can be incorporated into DNA in vitro by DNA polymerase.

GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease.

ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.

PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with CRBN ligand.

MDM2-IN-1 (Compound 30) is a synthetic MDM2-p53 interaction (MDM2) inhibitor and contains the trans (D-)configuration.

Azido-PEG4-C2-acid a PEG-based PROTAC linker can be used in the synthesis of vRucaparib-TP4. Azido-PEG4-C2-acid is also a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Thalidomide-NH-PEG7 is a synthesized E3 ligase ligand-linker conjugate for ADC. Thalidomide-NH-PEG7 can be connected to the ligand for protein by a linker to form PROTAC iRucaparib-AP6, a highly specific PARP1 degrader.

iRucaparib-AP6 is a highly efficient and specific PARP1 degrader based on Rucaparib by using the PROTAC approach. iRucaparib-AP6, a non-trapping PARP1 degrader, blocks both the catalytic activity and scaffolding effects of PARP1.

PERK-IN-3 is a potent PERK inhibitor with an IC50 of 7.4 nM.

LT052 is a highly selective BET BD1 inhibitor. LT052 displays inhibitory activity against BRD4 (BD1), BRD3 (BD1) and BRDT (BD1) with IC50s of 87.7, 246.3, and 357.1 nM, respectively. LT052 shows nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2. LT052 has inhibitory activities against BRPF1b (IC50=567.5 nM). LT052 has anti-inflammatory activity.

PROTAC EED degrader-2 is a PROTAC targeting EED with a pKD of 9.27. PROTAC EED degrader-2 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.11) targeting the EED subunit.

PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit.

PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A.

Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease.

Aβ42-IN-1, compound 1v, is a novel, potent and orally active γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC50 value of 0.091 µM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile.

Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively.

IDO1-IN-2 (compound 16) is a potent and selective IDO1 inhibitor with IC50s of 81 nM, 59 nM (mouse) and 28 nM (rat), respectively. IDO1-IN-2 has anti-cancer activity.

Nampt-IN-5 is a potent and orally active nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 inhibits CYP3A4 activity and has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively.

MS432 is a first-in-class and highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively.

Propargyl-PEG4-Br is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

m-PEG9-Amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Hydroxy-PEG3-SS-PEG3-alcohol is also a cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Azido-PEG6-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG6-alcohol is also a non-cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

m-PEG7-Ms is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Amino-PEG4-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Amino-PEG4-CH2COOH is also a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Cdc7-IN-4 (compound I-C) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-C. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.

Cdc7-IN-3 (compound I-A) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.

N-Boc-PEG7-alcohol is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).