DNA Damage, Repair & Cell Cycle

Oxaliplatin

CAS 61825-94-3

Oxaliplatin is a DNA synthesis inhibitor. It causes DNA crosslinking damage, prevents DNA replication and transcription and causes cell death.

BOS172722

CAS 1578245-44-9

BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1) checkpoint with an IC50 of 2 nM.

Amifostine

CAS 112901-68-5

Amifostine trihydrate (WR2721 trihydrate) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine trihydrate selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine trihydrate is potent…

GeA-69

CAS 2143475-98-1

GeA-69 is a selective, highly cell permeable allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2, with a Kd of 2.1 µM[1].

KU-55933

CAS 587871-26-9

KU-55933 is a potent ATM inhibitor with an IC50 and Ki of 12.9 and 2.2 nM, respectively, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.

Filanesib(ARRY-520)

CAS 885060-09-3

Filanesib (ARRY-520) is a synthetic kinesin spindle protein (KSP) inhibitor with IC50 of 6 nM.

GSK 2830371

CAS 1404456-53-6

GSK 2830371 is a highly selective Wip1 phosphatase inhibitor with IC50 of 6 nM.

BIBR-1532

CAS 321674-73-1

BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay.

ROSCOVITINE(Seliciclib)

CAS 186692-46-6

Roscovitine is a potent and selective CDKs inhibitor with IC50s of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5, Cdc2, and CDK2, respectively.

PF07104091(Tagtociclib)

CAS 2460249-19-6

PF-07104091 is an orally bioavailable inhibitor of cyclin-dependent kinase 2 (CDK2), with potential antineoplastic activity. Upon administration, CDK2 inhibitor PF-07104091 selectively targets, binds to and inhibits the activity of CDK2. This may lead to cell…

Gartisertib

CAS 1613191-99-3

Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity.

Vinorelbine Ditartrate

CAS 125317-39-7

Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.

Hydrazinocurcumin

CAS 131068-23-0

Hydrazinocurcumin is a synthetic curcumin derivative that inhibits the proliferation of bovine aortic endothelial cells (BAECs) with IC50 of 520 nM without cytotoxicity, inhibits STAT3 phosphorylation and downregulates an array of STAT3 downstream targets;…

2OH-BNPP1

CAS 833481-73-5

2OH-BNPP1 is an inhibitor of BUB1 kinase, a Ser/Thr kinase, used for the treatment of cancer.

Onvansertib (NMS-P937)

CAS 1034616-18-6

NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with an IC50 of 2 nM.

SR-4835

CAS 2387704-62-1

SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13.

Rucaparib(AG-014447)

CAS 283173-50-2

Rucaparib is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, and also shows binding affinity to eight other PARP domains.

BAY1217389

CAS 1554458-53-5

BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC50 value less than 10 nM.

Epothilone B

CAS 152044-54-7

Epothilone B is a microtubule stabilizer with a Ki of 0.71μM. It acts by binding to the αβ-tubulin heterodimer subunit which causes decreasing of αβ-tubulin dissociation.

TH9619

CAS 2379556-22-4

TH9619 (TH-9619) is a potent and selective inhibitor of folate metabolism enzyme MTHFD2 with IC50 of 47 nM.TH9619 demonstrated efficacy on HL-60 cell viability with EC50 of 11 nM.TH9619 potently inhibits related MTHFD proteins MTHFD2L and MTHFD1-(DC) with…

Acelarin

CAS 840506-29-8

Acelarin (NUC-1031) is a ProTide transformation and enhancement of the widely-used nucleoside analogue, gemcitabine.

Treosulfan

CAS 299-75-2

Treosulfan (NSC 39069, Treosulphan) is an alkylating agent used for conventional and high-dose chemotherapy regimens. Treosulfan is potently cytotoxic against pancreatic cancer cell lines.

BO-264

CAS 2408648-20-2

BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces spindle assembly checkpoint…

Uridine,5-chloro-2'-deoxy-

CAS 50-90-8

5-Chloro-2'-deoxyuridine, a thymine analog, is to study the potential of hypochlorous acid damage to DNA and DNA precursors.

Empesertib(BAY 1161909)

CAS 1443763-60-7

Empesertib(BAY 1161909) is a potent Mps1 inhibitor, with an IC50 of < 1 nM.

(R)-RP-6306

CAS 2719793-91-4

(R)-RP-6306 (183) can be used for the research of Myt1 mediated diseases and kinds of cancer for slowing the progression of cancer.

AZD-1152-HPQA

CAS 722544-51-6

AZD1152-HQPA is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, and appr 3700 fold more selective for Aurora B over Aurora A.

RX-3117

CAS 865838-26-2

RX-3117(TV-1360; Fluorocyclopentenylcytosine) is novel a cytidine analog; shows anticancer activity in several cancer cell lines, including gemcitabine-resistant variants.

COTI-2

CAS 1039455-84-9

COTI-2 is a small molecule candidate anti-cancer drug which can convert mutant p53 to wild-type conformation.

Mitomycin C

CAS 50-07-7

Mitomycin C is an antitumor drug and antibiotic that shows extraordinary ability to inhibit DNA synthesis.

Paprotrain

CAS 57046-73-8

Reversible, non-ATP competitive inhibitor of mitotic kinesin-like protein 2 (MKLP-2)

ART812

CAS 2607138-82-7

ART812 is a DNA polymerase Polθ inhibitor with an IC50 value of 7.6 nM. ART812 has an IC50 value of 240 nM for cell based microhomology-mediated end joining (MMEJ)[1][2].

NSC319726

CAS 71555-25-4

NSC319726 is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.in vitro: For NSC319726, the effect was even greater as the IC50 for the 175 mutant was 8 nM…

Ellipticine

CAS 519-23-3

Ellipticine hydrochloride is a potent antineoplastic agent; inhibits DNA topoisomerase II activities.

AZD-2281 (Olaparib)

CAS 763113-22-0

Olaparib (AZD2281;KU0059436) is a potent and oral PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively.

PF-07220060

CAS 2380321-51-5

PF-07220060 is a potent CDK4/CDK6 inhibitor with a Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively.

SY-5609 (CDK7-IN-3)

CAS 2417302-07-7

SY-5609 (CDK7-IN-3) is a selective CDK7 inhibitor with a KD of 0.059 nM. CDK7-IN-3 shows poor inhibition on CDK2 (Ki=390 nM), CDK9 (Ki=290 nM), CDK12 (Ki=78 nM). CDK7-IN-3 induce apoptosis in tumor cells and has antitumor activity.

GENZ-644282 TFA salt

Genz-644282, also known as SAR402674, is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity. Topoisomerase I inhibitor Genz-644282 binds to and inhibits the enzyme topoisomerase I, which may result in the inhibition of…

Tirapazamine

CAS 27314-97-2

Tirapazamine is an anticancer agent that shows selective cytotoxicity for hypoxic cells in solid tumors, thereby inducing single-and double-strand breaks in DNA, base damage, and cell death.

Allopole-A

CAS 3057557-03-3

Allopole-A is the first allosteric, specfic inhibitor of the noncatalytic polo-box domain (PBD) of PLK1 (Polo-like kinase 1) with IC50 of 2.5 nM in FP-based assays, Allopole-A is the active form of Allopole.

Aurora A Inhibitor I

CAS 1158838-45-9

Aurora A inhibitor I is a potent and highly selective Aurora A inhibitor with with an IC50 of 3.4 nM.

NSC59984

CAS 803647-40-7

NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway. The EC50 of NSC59984 in most cancer cells is significantly lower than those of normal cells, with EC50 of 8.38 μM for p53-null HCT116 cells.

Bohemine

CAS 189232-42-6

Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory…

5-Azacytidine

CAS 320-67-2

5-Azacytidine is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases.

B02

CAS 1290541-46-6

B02 is a cell-permeable pyridinylvinyl-quinazolinone compound that is shown to specifically inhibit human RAD51 (IC50 = 27.4 µM). Does not affect RecA even at much higher concentration (~250 µM). Directly interacts with RAD51 (Kd = 5.6 µM), and disrupts its…

DB818

CAS 790241-43-9

DB818 (DB-818, DB 818) is a small molecule inhibitor of HOXA9/DNA interaction through binding as minor groove DNA ligand on the HOXA9 cognate sequence; directly bind to HOXA9-cognate sequence with Kd value of 4.6 nM (HBS sequence); alters HOXA9-mediated…

Alsterpaullone

CAS 237430-03-4

Alsterpaullone (9-Nitropaullone;NSC 705701) is a potent cyclin-dependent kinases (CDK) inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP…

Auristatin E

CAS 160800-57-7

Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAE analog and cytotoxin in Antibody-drug conjugates.