NU2058|NU-2058|cas 161058-83-9

Cas No.:	161058-83-9
Synonyms:	NU 2058,NU-2058,NU2058
SMILES:	C1(COC2N=C(N)N=C3C=2N=CN3)CCCCC1
Formula:	C₁₂H₁₇N₅O
M.Wt:	247.3
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	NU2058 is a guanine-based CDK inhibitor with IC50 of 17 μM and 26 μM for CDK2 and CDK1.
Target:	CDK2:17 μM (IC50) CDK1:26 μM (IC50)
In Vitro:	NU2058 is a competitive inhibitor of CDK2 with respect to ATP (Ki value CDK2, 12 3 μM) that binds in the ATP binding pocket in a different orientation from other purine-based inhibitors, including olomoucine and roscovotine. NU2058 is the lead compound in a structure-based drug discovery program to develop more potent and selective CDK inhibitors.
References:	[1]. Rigas AC, et al. Therapeutic potential of CDK inhibitor NU2058 in androgen-independent prostate cancer. Oncogene. 2007 Dec 6;26(55):7611-7619.

Cat. No.	Product name	Field of application
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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