WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H130252
CAS#: 2271348-04-8 (free acid)
Description: MK256 is a novel CDK8 inhibitor with potent antitumor activity in AML through downregulation of the STAT pathway. MK256 induced differentiation and maturation. Treatment of MK256 inhibited proliferation of AML cell lines. MK256 not only downregulated phosphorylated STAT1(S727) and STAT5(S726), but also lowered mRNA expressions of MCL-1 and CCL2 in AML cell lines. Efficacy of MK256 was shown in MOLM-14 xenograft models, and the inhibitory effect on phosphorylated STAT1(S727) and STAT5(S726) with treatment of MK256 was observed in vivo. Pharmacologic dynamics study of MK256 in MOLM-14 xenograft models showed dose-dependent inhibition of the STAT pathway. Both in vitro and in vivo studies suggested that MK256 could effectively downregulate the STAT pathway.
Hodoodo Cat#: H130252
Name: MK256
CAS#: 2271348-04-8 (free acid)
Chemical Formula: C14H9BrN2O2
Exact Mass: 315.98
Molecular Weight: 317.140
Elemental Analysis: C, 53.02; H, 2.86; Br, 25.20; N, 8.83; O, 10.09
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Related CAS #: 2271348-04-8 (free acid) 2271348-72-0 (sodium)
Synonym: MK256; MK 256; MK-256
IUPAC/Chemical Name: 1-amino-5-bromobenzo[h]isoquinoline-8-carboxylic acid
InChi Key: SNTFBMJZDZCZRU-UHFFFAOYSA-N
InChi Code: InChI=1S/C14H9BrN2O2/c15-11-6-8-5-7(14(18)19)1-2-9(8)12-10(11)3-4-17-13(12)16/h1-6H,(H2,16,17)(H,18,19)
SMILES Code: NC1=NC=CC2=C1C3=C(C=C2Br)C=C(C=C3)C(O)=O
Appearance: To be determined
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info: Acute myeloid leukemia (AML) is the most lethal form of AML due to disease relapse. Cyclin dependent kinase 8 (CDK8) is a serine/threonine kinase that belongs to the family of Cyclin-dependent kinases and is an emerging target for the treatment of AML. MK256, a potent, selective, and orally available CDK8 inhibitor was developed to target AML. We sought to examine the anticancer effect of MK256 on AML. In CD34+/CD38- leukemia stem cells,
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The following data is based on the product molecular weight 317.14 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1. Lee JC, Liu S, Wang Y, Liang Y, Jablons DM. MK256 is a novel CDK8 inhibitor with potent antitumor activity in AML through downregulation of the STAT pathway. Oncotarget. 2022 Nov 2;13:1217-1236. doi: 10.18632/oncotarget.28305. PMID: 36342456; PMCID: PMC9629815.
