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| Cat. No. | Product Name | CAS No. | Information |
|---|---|---|---|
| CSN23159 | 4'-(5-((4-((Cyclopropylamino)methyl)phenyl)amino)-1H-pyrazol-3-yl)-[1,1'-biphenyl]-2,4-diol | 838823-31-7 | TCS2312 is a novel potent and selective CHK1 kinase inhibitor. |
| CSN16539 | SCH900776 (S-isomer) | 891494-64-7 | SCH-900776 is the S-isomer form of SCH900776 which is a potent selective and orally bioavailable inhibitor of checkpoint kinase Chk1 IC50 3 nM highly selective against Chk2 IC50 1500 nM and cyclin-dependent kinase CDK2 IC50 160 nM |
| CSN20306 | SAR-020106 | 1184843-57-9 | SAR-020106 is an ATP-competitive potent and selective CHK1 inhibitor with an IC 50 of 133 nmolL on the isolated human enzyme This compound abrogates an etoposide-induced G 2 arrest with an IC 50 of 55 nmolL in HT29 cells and significantly enhances the cell killing of gemcitabine and SN38 by 30- to 29-fold in several colon tumor lines in vitro and in a p53-dependent fashion |
| CSN26617 | Prexasertib Mesylate Hydrate | 1234015-57-6 | Prexasertib, also known as LY2606368, is a potent and selective Chk1/Chk2 inhibitor. Prexasertib increases the effectiveness of conventional therapy in B-/T- cell progenitor acute lymphoblastic leukemia. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Treatment of cells with LY2606368 results in the rapid appearance of TUNEL and pH2AX-positive double-stranded DNA breaks in the S-phase cell population. |
| CSN26616 | Prexasertib dimesylate | 1234015-58-7 | Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity[1][2]. |
| CSN17165 | PF 477736 | 952021-60-2 | PF-477736 is a selective, potent and ATP-competitive Chk1 inhibitor with Ki of 0.49 nM and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes and shows 100-fold selectivity for Chk1 than Chk2. |
| CSN23027 | PD 407824 | 622864-54-4 | PD 407824 is a potent and selective inhibitor of checkpoint kinases Chk1 and Wee1 with IC50s of 47 and 97 nM respectively. |
| CSN23009 | NSC 109555 Ditosylate | 66748-43-4 | NSC 109555 Ditosylate is a selective, reversible, ATP-competitive Chk2 inhibitor with IC50 of 0.2 μM. |
| CSN20298 | MU380 | 2109805-78-7 | MU380 is a potent selective inhibitor of CHK1 kinase possessing unusual N-trifluoromethylpyrazole pharmacophore resistant to metabolic N-dealkylation |
| CSN17600 | Prexasertib dihydrochloride | 1234015-54-3 | LY2606368 Prexasertib is a selective Chk1 inhibitor with IC50 value 1nM modest to Chk2 and Rsk with IC50 values of 8nM and 10nM |
| CSN17225 | Prexasertib | 1234015-52-1 | LY2606368 is a potent and selective ATP competitive inhibitor IC5015 nM in SW1990 cell of the Chk1 protein kinase |
| CSN17143 | Rabusertib | 911222-45-2 | LY2603618 is a highly selective Chk1 inhibitor with potential anti-tumor activity In a cell-free assay it shows an IC50 of 7 nM approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated |
| CSN21202 | SB-218078 | 135897-06-2 | Inhibitor of checkpoint kinase 1 Chk1 that displays selectivity over other protein kinases IC50 values are 15 250 and 1000 nM for Chk1 cdc2 and PKC respectively Abrogates G2 cell cycle arrest caused by -irradiation and topoisomerase I inhibition Potentiates cytotoxicity of DNA-damaging drugs enhancing the efficacy of some chemotherapeutics |
| CSN23328 | GDC-0575 | 1196541-47-5 | GDC-0575 is a potent and selective CHK1 inhibitor. |
| CSN22108 | CHK1 inhibitor | 2097938-64-0 | GDC-0575 is a potent and selective CHK1 inhibitor |
| CSN20165 | GDC-0425 | 1200129-48-1 | GDC-0425 is an oral selective Chk1 inhibitor GDC-0425 enhances gemcitabine gem efficacy in tumor xenograft models and shows greater chemopotentiation in cancer cell lines lacking p53 activity |
| CSN16590 | CHIR-124 | 405168-58-3 | CHIR-124 is a potent Chk1 inhibitor with IC50 of 03 nM with 2000-fold selectivity against Chk2 500- to 5000-fold less activity against CDK24 and Cdc2 |
| CSN18829 | CCT245737 | 1489389-18-5 | CCT245737 is a potent ATP-competitive CHK1 inhibitor with an IC50 of 30-220 nM |
| CSN18925 | CCT244747 | 1404095-34-6 | CCT244747 is potent highly selective orally active ATP competitive CHK1 inhibitor with IC50 of 29-170nM |
| CSN17641 | CCT241533 | 1262849-73-9 | CCT241533 is a potent serinethreonine checkpoint kinase Chk2 inhibitor with IC50 of 3 nM and shows minimal cross-reactivity against a panel of kinases at 1 M |
| CSN17848 | CCT241533 hydrochloride | 1431697-96-9 | CCT241533 HCl is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM and shows minimal cross-reactivity against a panel of kinases at 1 μM. |
| CSN16323 | BML-277 | 516480-79-8 | BML-277 is a selective Chk2 (checkpoint kinase 2) inhibitor with IC50 of 15 nM. |
| CSN15785 | AZD-7762 | 860352-01-8 | AZD7762 is a potent and selective inhibitor of Chk1 with IC50 of 5 nM, being equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck. |
| CSN22704 | (S)-5-(3-Fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide hydrochloride | 1246094-78-9 | AZD 7762 HCl is a potent and selective ATP-competitive inhibitor of Chk1 and Chk2, both with IC50 of 5 nM. |
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