DNA Damage/DNA Repair

Dalpiciclib (SHR-6390) is an orally active and highly selective inhibitor of CDK4 and 6 with IC50 values of 12.4?nM and 9.9?nM, respectively. Dalpiciclib shows antitumor activity against breast cancer and esophageal squamous cell carcinoma.

Avotaciclib (BEY1107) is a potent and orally active inhibitor of cyclin dependent kinase 1 (CDK1). Avotaciclib can be used for the research of locally advanced or metastatic pancreatic cancer.

IV-361 is an orally active and selective CDK7 inhibitor (Ki≤50 nM). IV-361 has anti-cancer activity (US20190256531A1).

Casein Kinase inhibitor A86 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A86 also inhibits of CDK7 (TFIIH) and CDK9 (P-TEFb). Casein Kinase inhibitor A861 induces leukemia cell apoptosis, and has potent anti-leukemic activities.

Cirtuvivint is an orally bioavailable CDC-like kinase (CLK) inhibitor with anti-tumor activity.

CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties.

IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM.

Tetroxoprim is an antimicrobial DHFR inhibitor.

NCGC00029283 is a werner syndrome helicase-nuclease (WRN) helicase inhibitor with IC50s of 2.3 μM, 12.5 μM, and 3.4 μM for WRN, BLM and FANCJ helicase, respectively.

Abemaciclib metabolite M18 (LSN3106729) hydrochloride, the metabolite of Abemaciclib, is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader.

Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 ?M. Samuraciclib hydrochloride hydrate has anti-tumor effects.

BAY-8400 is an orally active, potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (IC50=81 nM). BAY-8400 can be used for the research of cancer.

Gemcitabine elaidate (CP-4126) hydrochloride is lipophilic pro-drug of Gemcitabine. Gemcitabine elaidate hydrochloride is converted to Gemcitabine by esterases in order to be phosphorylated. Gemcitabine elaidate hydrochloride exhibits anti-tumor activity.

IXA4 is a highly selective, non-toxic IRE1/XBP1s activator that induces endoplasmic reticulum (ER) proteostasis remodeling.

116-9e (MAL2-11B) is a Hsp70 co-chaperone DNAJA1 inhibitor.

CK7, a Cdk2/9 inhibitor, can be used for the synthesis of Nek1 inhibitor BSc5231 and BSc5367.

HQ461 is a molecular glue that promotes CDK12-DDB1 interaction to trigger cyclin K degradation. HQ461-mediated degradation of cyclin K impairs CDK12 function, resulting in decreased CDK12 substrate phosphorylation, downregulation of DNA damage response genes, and cell death.

(E/Z)-Zotiraciclib ((E/Z)-TG02) hydrochloride is a potent CDK2, JAK2, and FLT3 inhibitor.

NSC 107512 is a potent inhibitor of cyclin-dependent kinase 9 (CDK9). NSC 107512 is a class of sangivamycin-like molecules (SLM). NSC 107512 inhibits growth and induces apoptosis of multiple myeloma tumors.

KH-CB20, an E/Z mixture, is a potent and selective inhibitor of CLK1 and the closely related isoform CLK4, with an IC50 of 16.5 nM for CLK1.

Folic Acid-d2 is the deuterium labeled Folic acid. Folic acid (Vitamin M; Vitamin B9) is a B vitamin; is necessary for the production and maintenance of new cells, for DNA synthesis and RNA synthesis.

CDK7-IN-2 is a potent inhibitor of CDK7. CDK7 is implicated in both temporal control of the cell cycle and transcriptional activity. CDK7 is implicated in the transcriptional initiation process by phosphorylation of Rbpl subunit of RNA Polymerase II (RNAPII). CDK7 has the potential for the research of cancer disease, in particular aggressive and hard- to-treat cancers (extracted from patent WO2019099298A1, compound 1).

FPFT-2216, a “molecular glue” compound, degrades phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3), and casein kinase 1α (CK1α).

ddTTP is one of 2',3'-dideoxyribonucleoside 5'-triphosphates (ddNTPs) that acts as chain-elongating inhibitor of DNA polymerase for DNA sequencing.