DNA Damage/DNA Repair

5’-O-DMT-2’-O-TBDMS-Ac-rC is a modified nucleoside and can be used to synthesize DNA or RNA.

CDK-IN-6, a class of pyrazolo[1,5-a]pyrimidine compound, is a CDK inhibitor with anticancer activities.

Dxd-d5 (Exatecan-d5 derivative for ADC) is a deuterium labeled Dxd. Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) .

BSJ-4-116 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib.

YKL-5-124 TFA is a potent, selective, irreversible, and covalent CDK7 inhibitor with IC 50 values of 53.5nM and 9.7nM for CDK7 and CDK7/Mat1/CycH, respectively.

HBV-IN-4, a phthalazinone derivative, is a potent and orally active HBV DNA replication inhibitor with an IC50 of 14 nM.

CK2 inhibitor 2 is a potent, selective and orally active inhibitor of CK2, with an IC50 of 0.66 nM. CK2 inhibitor 2 shows high selectivity for Clk2 (IC50=32.69 nM)/CK2. CK2 inhibitor 2 exhibits favorable antiproliferative and antitumor activity.

USP7-IN-8 (example 81) is a selective ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 1.4 μM in an Ub-Rho110 assay. USP7-IN-8 shows no activity against USP47 and USP5. USP7-IN-8 has anticancer effects.

5-Iminodaunorubicin is a quinone-modified anthracycline that retains antitumor activity. 5-Iminodaunorubicin produces protein-concealed DNA strand breaks in cancer cells.

KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity.

SU0268 is a potent and specific inhibitor of 8-Oxoguanine DNA glycosylase 1 (OGG1).

USP30 inhibitor 18 is a selective USP30 inhibitor with an IC50 of 0.02 μM. USP30 inhibitor 18 increases protein ubiquitination and accelerates mitophagy.

GSK-3/CDK5/CDK2-IN-1, an imidazole derivative, is an inhibitor of cdk5, cdk2, and GSK-3 extracted from patent WO2002010141A1, example 9a.

ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research.

Cdc7-IN-5 (compound I-B) 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.

Casein Kinase inhibitor A51 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A51 induces leukemia cell apoptosis, and has potent anti-leukemic activities.

ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer.

IMT1B is a highly specific inhibitor of mitochondrial RNA polymerase (POLRMT), inhibiting mitochondrial gene expression.

LCAHA (LCA hydroxyamide) is a deubiquitinase USP2a inhibitor with IC50s of 9.7 μM and 3.7μM in Ub-AMC Assay and Di-Ub Assay, respectively. LCAHA destabilizes Cyclin D1 and induces G0/G1 arrest by inhibiting deubiquitinase USP2a.

AG-636 is a potent, reversible, selective and orally active dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 17 nM. AG-636 has strong anticancer effects.

PR-104A (SN 27858) is the alcohol metabolite of phosphate prodrug PR-104. PR-104A is a hypoxia-selective DNA cross-linking agent/DNA-damaging agent and cytotoxin. Antitumor Activity. PR-104A is metabolized under hypoxia by the 1-electron NADPH:cytochrome P450 oxidoreductase. PR-104A can be used for the research of relapsed/refractory T-lineage acute lymphoblastic leukemia (T-ALL).

OBI-3424 (TH-3424) is a prodrug that is selectively converted by AKR1C3 (aldo-keto reductase 1C3) to a potent DNA-alkylating agent. OBI-3424 can be used for hepatocellular carcinoma, castrate-resistant prostate cancer, and acute lymphoblastic leukemia (ALL) research.