| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
BRD6989 is an analog of the naturally occurng cortistatin A (dCA), acting as a novel, potent and selective CDK8 inhibitor with an IC50 of ~200 nM. BRD6989 requires an intact cyclin C-CDK8 complex in order to upregulate IL-10, a function that is recapitulated by several structurally distinct CDK8 and CDK19 inhibitors. BRD6989 showed a strong preference for CDK8 over CDK19. BRD6989 increased IL-10 production and inhibited STAT1 phosphorylation at S727 in bone marrow-derived dendritic cells, indicating that CDK8 functions as a negative regulator of IL-10 production during innate immune activation. For inflammatory conditions, BRD6989 might be helpful.
| Targets |
CDK8 (IC50 ~200 nM); recombinant CDK8 (IC50 ~0.5 μM); recombinant CDK19 (IC50 >30 μM); IL-10
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| ln Vitro |
Using BRD6989 (0-100 μM; 48 hours) to ablate BMDCs results in an EC50 trajectory of 1 μM for IL-10 production [1]. IFNγ-stimulated BMDCs are inhibited at Ser727 by BRD6989 (0.6, 1.7, 5, 15 μM). After stimulating BMDMs, BRD6989 (5 μM; ~2 hours) differentially suppresses STAT1–STAT2 activity and phosphorylation of the NF-κB activation domain [1]. BRD6989 (^2 hours; 5 µM). 24 hours) increases the synthesis of IL-10 and activator in mouse dendritic cells and macrophages [1].
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| References |
[1]. Johannessen L, et al. Small-molecule studies identify CDK8 as a regulator of IL-10 in myeloid cells. Nat Chem Biol. 2017 Oct;13(10):1102-1108
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| Molecular Formula |
C16H16N4
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|---|---|
| Molecular Weight |
264.332
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| Exact Mass |
264.1375
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| Elemental Analysis |
C, 72.70; H, 6.10; N, 21.20
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| CAS # |
642008-81-9
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| Related CAS # |
642008-81-9
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| Appearance |
Solid powder
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| SMILES |
CC1CCC2=C(C1)C(=C(C(=N2)N)C#N)C3=CN=CC=C3
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| InChi Key |
QSYBDNXNOJIKML-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H16N4/c1-10-4-5-14-12(7-10)15(11-3-2-6-19-9-11)13(8-17)16(18)20-14/h2-3,6,9-10H,4-5,7H2,1H3,(H2,18,20)
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| Chemical Name |
2-amino-6-methyl-4-pyridin-3-yl-5,6,7,8-tetrahydroquinoline-3-carbonitrile
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| Synonyms |
BRD-6989; BRD6989; BRD 6989
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 25~30 mg/mL (94.6~113.5 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7831 mL | 18.9157 mL | 37.8315 mL | |
| 5 mM | 0.7566 mL | 3.7831 mL | 7.5663 mL | |
| 10 mM | 0.3783 mL | 1.8916 mL | 3.7831 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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