CDK9-IN-1|cas 1415559-43-1|DC Chemicals

Cas No.:	1415559-43-1
SMILES:	CC1=C(NS(C)(=O)=O)C=C(NC2=NC=NC(C3=CC=CC(N4C(C5=C(C=CC=C5)C4=O)=O)=C3)=C2)C=C1
Formula:	C₂₆H₂₁N₅O₄S
M.Wt:	499.541
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection. Among CDKs, CDK9 is a validated pathological target in HIV infection, inflammation and cardiac hypertrophy; however selective CDK9 inhibitors are still not available. We present a selective inhibitor family of CDK9 based on the 4-phenylamino-6- phenylpyrimidine nucleus. We show a convenient synthetic method to prepare a useful intermediate and its derivatisation resulting in novel compounds. The CDK9 inhibitory activity of the derivatives was measured in specific kinase assay and the CDK inhibitory profile of the best ones (IC50 > 100nM) was determined. The most selective compounds had high selectivity over CDK1, 2, 3, 5, 6, 7 and showed at least one order of magnitude higher inhibitory activity over CDK4 inhibition. The most selective molecules were examined in cytotoxicity assays and their ability to inhibit HIV-1 replication was determined in cellular assays.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC47707	CDK/HDAC-IN-1	CDK/HDAC-IN-1 shows remarkable CDK2/4/6 and HDAC6 inhibitory activity of IC50 = 60.9 ± 2.9, 276 ± 22.3, 27.2 ± 4.2, and 128.6 ± 0.4 nM, respectively.
DC47706	CDK2-IN-7	CDK2-IN-7 is a CDK2 inhibitor for treating cancer (IC50 < 50 nM).
DC47705	JH-XVI-178	JH-XVI-178 is a highly potent and selective inhibitor of CDK8/19 that displays low clearance and moderate oral pharmacokinetic properties.
DC47704	CDK9-IN-12	CDK9-IN-12 displays the optimal CDK9 inhibitory activity with an IC50 value of 5.41 nM.
DC47236	Cirtuvivint	Cirtuvivint (SM08502) is a potent and orally active CDC-like kinase (CLK) inhibitor. Cirtuvivint can be used for solid tumors research.
DC47205	Eltenac	Eltenac, a non-steroidal anti-inflammatory drug (NSAID), is a COX inhibitor. Eltenac shows IC50 of 0.03 μM for both COX-1 and COX-2 in isolated human whole blood.
DC47130	CDK5-IN-1	CDK5-IN-1, a potent CDK5 inhibitor, is against CDK5 activity less than 10 nM. CDK5-IN-1 is used for kidney diseases research.
DC47109	Cimpuciclib	Cimpuciclib is a cyclin-dependent kinase(CDK) inhibitor and antineoplastic.
DC47043	Ocarocoxib	Ocarocoxib, a potent COX-2 (cyclooxygenase-2) inhibitor, is a non-steroidal anti-inflammatory for veterinary use.
DC46945	Avotaciclib	Avotaciclib (BEY1107) is an orally active cyclin dependent kinase 1 (CDK1) inhibitor. Avotaciclib can be used for the research of cancer.