research use only

Senexin A CDK inhibitor

Name: Senexin A
Brand: Selleck Chemicals
SKU: S8520
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S8520

Senexin A is a potent and selective inhibitor of CDK8 and its nearest relative, CDK19 with Kd values of 0.83 μM and 0.31 μM for CDK8 and CDK19 ATP site binding, respectively.

Chemical Structure

Molecular Weight: 274.32

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S852001 DMSO]54 mg/mL]false]Ethanol]54 mg/mL]false]Water]Insoluble]false Purity: 99.89%

99.89

Related Targets	DNA/RNA Synthesis Microtubule Associated Ras HSP (HSP90) PD-1/PD-L1 Aurora Kinase Casein Kinase Rho Serine/threonin kinase eIF Chk ROCK Myc Kinesin PLK DHFR PAK PERK DYRK RUNX PP2A PFKFB AP-1 MPS1 Wee1 p21 BMI-1 LIM kinase Nur77 APC
Related Products	Ro-3306 Dinaciclib Roscovitine Flavopiridol (Alvocidib) SNS-032 (BMS-387032) Flavopiridol (Alvocidib) HCl AT7519 LDC000067 PHA-767491 HCl THZ1 2HCl XL413 JNJ-7706621 AZD5438 Purvalanol A Milciclib BS-181 HCl K03861 (AUZ454) PHA-793887 BMS-265246 AT7519 HCl AZD4573 MSC2530818 Riviciclib hydrochloride (P276-00) CVT-313 (E/Z)-TG003 Kenpaullone R547 Atuveciclib (BAY-1143572) YKL-5-124 LDC4297

Chemical Information, Storage & Stability

Molecular Weight	274.32	Formula	C₁₇H₁₄N₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1366002-50-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC=C(C=C1)CCNC2=NC=NC3=C2C=C(C=C3)C#N

Solubility

In vitro
Batch:

DMSO : 54 mg/mL ( (196.85 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 54 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.700mg/ml (9.84mM)	Taking the 1 mL working solution as an example, add 50 μL of 54 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.675mg/ml (2.46mM)	Taking the 1 mL working solution as an example, add 50 μL of 13.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	CDK19 ^[1] (Cell-free assay) 0.31 μM(Kd) CDK8 ^[1] (Cell-free assay) 0.83 μM(Kd)
In vitro	p21 is shown to activate NF-κB–dependent transcription, and Senexin A inhibits p21-stimulated activity of the consensus NF-κB–dependent promoter. This compound has no effect on p21 induction by IPTG, on cell growth with or without p21, or on p21-induced senescent phenotype. It does not affect the inhibition of gene expression by p21 and does not interfere with p21-mediated inhibition of large sets of genes belonging to Gene Ontology (GO) categories of mitosis and DNA replication. This chemical inhibits only p21-induced transcription but not other biological effects of p21. It inhibits CDK8 and CDK19 ATP site binding with Kd50 of 0.83 μM and 0.31 μM, respectively and CDK8 kinase activity with IC50 of 0.28 μM. It inhibits β-catenin–dependent transcription in HCT116 colon carcinoma cells. It does not inhibit ROCK and did not share cortistatin A's strong antiendothelial cell activity^[1].
In vivo	The CDK8/19 inhibitor Senexin A reverses chemotherapy-induced paracrine tumor-promoting activities in vivo and does not inhibit reporter cell growth and showed no detectable toxicity in a mouse study^[1].
References	https://pubmed.ncbi.nlm.nih.gov/22869755/

Applications

Methods	Biomarkers	Images	PMID
Western blot	GLUT1 / GLUT3 / HK1 / HIF1A / CDK8		29117556

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):