NU6027|CDK Inhibitor|DC Chemicals

Cas No.:	220036-08-8
Chemical Name:	4-Cyclohexylmethoxy-2,6-diamino-5-nitrosopyrimidine
Synonyms:	NU6027，NU-6027，NU 6027
SMILES:	NC1=NC(OCC2CCCCC2)=C(N=O)C(N)=N1
Formula:	C₁₁H₁₇N₅O₂
M.Wt:	251.28
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with Kis of 2.5 µM and 1.3 µM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner[1][2].
Target:	CDK1:2.5 μM (Ki) CDK2:1.3 μM (Ki) ATR
In Vitro:	NU6027 (1 nM-100 µM; 48 h) inhibits the growth of human tumor cells with a GI50 of 10±6 µM[1]. NU6027 (0.1-25 µM; 24 h) inhibits ATR activity with an IC50 of 2.8 µM in GM847KD cells. NU6027 (1-10 µM; 24 h) inhibits ATR activity with an IC50 of 6.7±2.3 µM in MCF7 cells[2]. NU6027 (4 or 10 µM; 24 h) attenuates G2/M arrest following DNA damage in MCF7 cells[2]. NU6027 (10 µM; 24 h) significantly reduces RAD51 foci in both control and PF-01367338-treated V-C8 B2 cells[2]. NU6027 (4 µM; 24 h) causes 82% suppression of the increase in RAD51 foci-positive cells treated by PF-01367338[2]. Western Blot Analysis[2] Cell Line: MCF7 cells Concentration: 0, 1, 5, 10 μM Incubation Time: 24 h Result: Inhibited CDK2-mediated pRbT821 by 42±27% compared with 70±12% inhibition of pCHK1S345 with the concentration of 10 µM.
References:	[1]. Arris CE, et, al. Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. J Med Chem. 2000 Jul 27; 43(15): 2797-804. [2]. Peasland A, et, al. Identification and evaluation of a potent novel ATR inhibitor, NU6027, in breast and ovarian cancer cell lines. Br J Cancer. 2011 Jul 26;105(3):372-81.

Cat. No.	Product name	Field of application
DC27001	SR-4835	SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13.
DC70595	MFH290	MFH290 (MFH-290) is a potent, highly selective, covalent inhibitor of CDK12/13 with IC50 of 25/49 nM.MFH290 forms a covalent bond with Cys-1039 of CDK12, and CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290.MFH290 exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes.MFH290 restored Pol II CTD phosphorylation and DNA damage repair gene expression AND augments the antiproliferative effect of the PARP inhibitor olaparib.
DC49082	CDK5-IN-2	CDK5-IN-2 (compound 15) is a highly selective CDK5 inhibitor with IC50s of 0.2 and 23 for CDK5/p25 and CDK2/CycA, respectively.
DC44518	SY-5609 (CDK7-IN-3)	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.
DC28661	Cdc7-IN-7	Cdc7-IN-7 (compound I-E) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-E. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
DC28660	Cdc7-IN-6	Cdc7-IN-6 (compound I-D) is a potent Cdc7 kinase inhibitor (IC50=4 nM), extracted from patent WO2019165473A1, compound I- D, has anti-tumor activity.
DC28659	Cdc7-IN-5	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.
DC7493	SB1317(TG-02)	SB1317(TG-02) is a novel small molecule potent CDK2/JAK2/FLT3 inhibitor with IC50s of 13/73/56 nM respectively.
DC11282	THZ2	THZ2 is a potent and selective CDK7 inhibitor with IC50 of 13.9 nM.
DC8068	WHI-P180(Janex 3)	WHI-P180(Janex 3) is a potent inhibitor of IgE-mediated mast cell responses to allergens in vitro and in vivo. Also inhibits cyclin-dependent kinase 2 (CDK2; IC50 = 1µM) by blocking the ATP site