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Chk2 inhibitor is an inhibitor of checkpoint kinase 2 (Chk2; IC50 = 13.5 nM). Chk2 inhibitor enhances survival of 184B5, but not MDA-MB-231, cells following ionizing radiation and inhibits cell cycle arrest at the G2 stage induced by ionizing radiation in 184B5 cells. It also inhibits the production of IL-2 in Jurkat cells, the production of TNF-α in LPS-stimulated THP-1 cells and the growth of CEM leukemia T cells. Synonyms: SC-203885; (5Z)-5-(2-amino-1,5-dihydro-5-oxo-4H-imidazol-4-ylidene)-3,4,5,10-tetrahydro-azepino[3,4-b]indol-1(2H)-one; Hymenialdisine Analogue 1. CAS No. 724708-21-8. Molecular formula: C15H13N5O2. Mole weight: 295.3.
ATR Inhibitor IV (VE821, 3-amino-6- (4- (methylsulfonyl) phenyl) -N-phenylpyrazine-2-carboxamide, VE-821, ATM and Rad3-Related Inhibitor IV)
A cell-permeable phenylpyrazine derivative that acts as a potent, ATP-competitive (Ki= 13nM; IC50/[ATP] = 70nM/50uM and 128nM/100uM), ATR-selective inhibitor with much reduced or little potency against 4 related PIKKs (Ki= 2.2, 3.9, 16, and >1uM, respectively, against DNA-PK, PI 3-K-gamma, ATM, and mTOR) and 50 other kinases. Shown to selectively inhibit ATR-dependent H2AX Ser139 & Chk1 Ser345 phosphorylation (complete inhibition at 10uM in HT29 and HFL1 cultures) without affecting ATM- and DNA-PK-mediated H2AX or ATM-mediated Chk2 phosphorylation. Short-term (24h) VE-821 treatment, either alone or in synergy with Cisplatin, results in reversible cytostatic growth arrest regardless of cellular ATM-p53 pathway activity, while cytotoxicity and Cisplatin synergism in cell death induction is reported to occur only upon long-term VE-821 exposure (≥72h) in cultures with ATM-p53 pathway defects.CAS No.1232410-49-10. Group: Biochemicals. Grades: Highly Purified. CAS No. 1232410-49-10. Pack Sizes: 10mg. Molecular Formula: C??H??N?O?S. US Biological Life Sciences.
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AZD 7762 hydrochloride
AZD 7762 hydrochloride is the hydrochloride salt of AZD 7762, which is a selective and potent ATP-competitive inhibitor of Chk1 and Chk2 with IC50 values of 5 nM for both kinases. It shows at least >10 fold selectivity over a panel of 164 kinases. It is used as a potentiation cytotoxicity DNA-damaging agent. It is active in vivo. Synonyms: AZD 7762 hydrochloride; AZD7762 hydrochloride; AZD-7762 hydrochloride; 5-(3-Fluorophenyl)-3-ureidothiophene-2-carboxylic acid N-[(S)-piperidin-3-yl]amide hydrochloride; 3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-thiophenecarboxamide hydrochloride. Grades: ≥98% by HPLC. CAS No. 1246094-78-9. Molecular formula: C17H20FN4O2SCl. Mole weight: 398.88.
BML-277
BML-277 is a selective APT-competitive inhibitor of the DNA damage response signaling enzyme CHK2 ( IC50 =15 nM). Uses: A selective apt-competitive inhibitor. Synonyms: BML-277; BML 277; BML277; Chk2 Inhibitor II;2-[4-(4-chlorophenoxy)phenyl]-3H-benzimidazole-5-carboxamide. Grades: ≥98%. CAS No. 516480-79-8. Molecular formula: C20H14ClN3O2. Mole weight: 363.80.
BML-277
BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 15 nM. Uses: Scientific research. Group: Signaling pathways. Alternative Names: Chk2 Inhibitor II. CAS No. 516480-79-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg. Product ID: HY-13946.
CCT 241533 dihydrochloride
CCT 241533 dihydrochloride is a potent Chk2 inhibitor (IC50 = 3 nM) displaying >63-fold selectivity for Chk1 over Chk2 and a panel of 84 other kinases. CCT 241533 inhibits Chk2 activation in response to etoposide-induced DNA damage in HT29 cells, and blocks ionizing radiation-induced apoptosis of mouse thymocytes. Synonyms: CCT 241533 dihydrochloride; CCT241533 dihydrochloride; CCT-241533 dihydrochloride; (3R,4S)-4-[[2-(5-Fluoro-2-hydroxyphenyl)-6,7-dimethoxy-4-quinazolinyl]amino]-α,α-dimethyl-3-pyrrolidinemethanol dihydrochloride. Grades: ≥98% by HPLC. CAS No. 1962925-28-5. Molecular formula: C23H27FN4O4.2HCl. Mole weight: 515.41.
CCT241533 hydrochloride
CCT241533 hydrochloride is a potent and selective CHK2 inhibitor with an IC 50 of 3 nM and a K i of 1.16 nM [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1431697-96-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-14715B.
CCT245737
CCT245737 is an orally bioactive CHK1 inhibitor (IC50 of 1.4 nM), displaying >1,000-fold selectivity against CHK2 and CDK1. It potently inhibits cellular CHK1 activity (IC50 30-220nM) and enhances gemcitabine and SN38 cytotoxicity in multiple human tumor cell lines and human tumor xenograft models. It causes inhibition of tumor growth in an Eμ-Myc mouse model of human B-cell lymphocytic leukemia. Synonyms: CCT-245737; CCT 245737; CCT245737; 5-[(4-{[(2R)-morpholin-2-ylmethyl]amino}-5-(trifluoromethyl)pyridin-2-yl)amino]pyrazine-2-carbonitrile. CAS No. 1489389-18-5. Molecular formula: C16H16F3N7O. Mole weight: 379.347.
Debromohymenialdisine
Protein kinase C (PKC) inhibitor. Inhibits the ATP binding site. Cytotoxic and insecticidal. G2 DNA damage checkpoint inhibitor. Check point kinases 1 (Chk1) and 2 (Chk2) inhibitor. Does not inhibit ataxia-telangiectasia mutated (ATM) or ATM-Rad3-related proteins. MAP kinase kinase 1 (MEK-1) inhibitor. Interleukin-1 (IL-1) inhibitor. Anti-osteoarthritic. Potential anti-Alzheimer agent. Group: Biochemicals. Grades: Highly Purified. CAS No. 75593-17-8, 125118-55-0. Pack Sizes: 100ug. Molecular Formula: C11H11N5O2. US Biological Life Sciences.
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NSC 109555 dimesylate
NSC 109555 is a potent and selective inhibitor of checkpoint kinase 2 (Chk2), displaying no effect against other kinases. It inhibits H1 phosphorylation and attenuates mitochondrial ATP synthesis. NSC 109555 can be used in cancer therapy. Synonyms: DDUG; NCI C04808; Carbanilide, 4,4'-diacetyl-, 4,4'-bis(amidinohydrazone), dimethanesulfonate. CAS No. 15427-93-7. Molecular formula: C19H24N10O·2CH3SO3H. Mole weight: 600.7.
NSC 109555 ditosylate
NSC-109555 Ditosylate is an ATP-competitive Chk2 inhibitor with IC50 value of 0.2 μM. It acts by inhibiting histone H1 phosphorylation and attenuating mitochondrial ATP synthesis. It is an antileukemic agent. Synonyms: NSC-109555 Ditosylate; NSC 109555 Ditosylate; NSC109555 Ditosylate; 4,4'-diacetyldiphenylurea bis(guanylhydrazone) ditosylate. Grades: ≥98% by HPLC. CAS No. 66748-43-4. Molecular formula: C19H24N10O.2C7H8O3S. Mole weight: 752.86.
PF 477736
PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo[1][2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: PF 00477736. CAS No. 952021-60-2. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-10032.
PF 477736
Selective checkpoint kinase 1 (Chk1) inhibitor (Ki values are 0.49 and 47 nM for Chk1 and Chk2 respectively). Abrogates cell cycle arrest at S and G2-M checkpoints; sensitizes cells to DNA damage. Group: Biochemicals. Grades: Highly Purified. CAS No. 952021-60-2. Pack Sizes: 10mg. Molecular Formula: C??H??N?O?. US Biological Life Sciences.
Worldwide
Poloxipan
Poloxipan is a potent and pan-specific PLK1 inhibitor. In vitro, Poloxipan has IC50 3.2 uM (Plk1); 1.7 uM (Plk2); and 3 uM (Plk3). Poloxipan showed minor inhibition over FHA dommain of Chk2, S2 domian of STAT1, STAT5b, Lck, etc. Synonyms: (Z)-2-(5-bromo-2-methoxybenzylidene)-6-methyl-2H-thiazolo[3,2-b][1,2,4]triazine-3,7-dione; 2-(5-Bromo-2-methoxybenzylidene)-6-methyl-2H-thiazolo[3,2-b][1,2,4]triazine-3,7-dione. Grades: 98%. CAS No. 1239513-63-3. Molecular formula: C14H10BrN3O3S. Mole weight: 380.22.
Prexasertib
Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a K i of 0.9 nM and an IC 50 of <1 nM. Prexasertib inhibits CHK2 (IC 50 =8 nM) and RSK1 (IC 50 =9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: LY2606368. CAS No. 1234015-52-1. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-18174.
Prexasertib dihydrochloride
Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a K i of 0.9 nM and an IC 50 of <1 nM. Prexasertib dihydrochloride inhibits CHK2 (IC 50 =8 nM) and RSK1 (IC 50 =9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: LY2606368 dihydrochloride. CAS No. 1234015-54-3. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-18174A.
Prexasertib mesylate
Prexasertib, also known as LY2606368, is an ATP-competitive CHK1 inhibitor (Ki= 0.9 nmol/L), with minor activity against CHK2 and RSK with IC50= 8 nM and 9 nM respectively in cell-free assay. 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. Synonyms: 2-Pyrazinecarbonitrile, 5-((5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)-, methanesulfonate; Prexasertib mesylate; LY2606368; LY-2606368; LY 2606368. CAS No. 1234015-55-4. Molecular formula: C19H23N7O5S. Mole weight: 461.49.
SCH900776
SCH900776 (MK-8776) is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. SCH900776 shows 50- and 500-fold selectivity over CDK2 and Chk2, respectively[1][2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: MK-8776. CAS No. 891494-63-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-15532.
An inhibitor of CHK1 and CHK2. Synonyms: Thieno[2,?3-d]?pyridazine-7-carboxamide, 2-(3-fluorophenyl)?-4-[(3S)?-3-piperidinylamino]?-, hydrochloride (1:1). CAS No. 1278405-51-8. Molecular formula: C18H19ClFN5OS. Mole weight: 407.89.
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