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MedKoo Cat#: 555260 | Name: MLS-2052
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

MLS-2052, aso known as BIO and GSK3 Inhibitor IX, is a cell-permeable bis-indolo (indirubin) compound that acts as a highly potent, selective, reversible, and ATP-competitive inhibitor of GSK3α/β (IC50 = 5 nM).

Chemical Structure

MLS-2052
CAS#667463-62-9

Theoretical Analysis

MedKoo Cat#: 555260

Name: MLS-2052

CAS#: 667463-62-9

Chemical Formula: C16H10BrN3O2

Exact Mass: 354.9956

Molecular Weight: 356.18

Elemental Analysis: C, 53.95; H, 2.83; Br, 22.43; N, 11.80; O, 8.98

Price and Availability

Size Price Availability Quantity
5mg USD 255.00 2 weeks
10mg USD 450.00 2 weeks
25mg USD 850.00 2 weeks
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Related CAS #
No Data
Synonym
BIO; ​GSK3 Inhibitor IX; MLS 2052; MLS-2052; MLS2052.
IUPAC/Chemical Name
6-Bromoindirubin-3'-oxime
InChi Key
DDLZLOKCJHBUHD-WAVHTBQISA-N
InChi Code
InChI=1S/C16H10BrN3O2/c17-8-5-6-9-12(7-8)19-16(21)13(9)15-14(20-22)10-3-1-2-4-11(10)18-15/h1-7,18,22H,(H,19,21)/b15-13-,20-14+
SMILES Code
O=C(/C1=C2NC3=C(C\2=N/O)C=CC=C3)NC4=C1C=CC(Br)=C4
Appearance
Solid powder
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
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5.
In vitro activity:
To determine whether a molecule that can maintain stem cell properties can also participate in controlling the proliferative capability of the highly differentiated cardiomyocytes, this study examines the effect of BIO (6-bromoindirubin-3'-oxime) in postmitotic cardiac cells. Here, this study shows that BIO promotes proliferation in mammalian cardiomyocytes. Reference: Chem Biol. 2006 Sep;13(9):957-63. https://pubmed.ncbi.nlm.nih.gov/16984885/
In vivo activity:
Anti-cancer activity of 6BIO (6-Bromoindirubin-3'-oxime) in vivo was studied with an A2058 human melanoma xenograft mouse model. 6BIO at the dose of 100 mg/kg was found safe to the mice (Fig. 5A). Then this study used a dose of 50 mg/kg for 6BIO therapy study in NSG mouse xenograft model by oral administration once daily for 2 weeks. As shown in Figure 5B, the tumor growth was significantly suppressed. Reference: Cancer Res. 2011 Jun 1;71(11):3972-9. https://pubmed.ncbi.nlm.nih.gov/21610112/
Solvent mg/mL mM comments
Solubility
DMF 10.0 28.08
DMSO 26.9 75.50
DMSO:PBS (pH 7.2) (1:2) 0.3 0.84
Ethanol 8.4 23.45
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 356.18 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.

Recalculate based on batch purity %
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:
1. Park JS, Jung IA, Choi HS, Kim DH, Choi HI, Bae EH, Ma SK, Kim SW. Anti-fibrotic effect of 6-bromo-indirubin-3'-oxime (6-BIO) via regulation of activator protein-1 (AP-1) and specificity protein-1 (SP-1) transcription factors in kidney cells. Biomed Pharmacother. 2022 Jan;145:112402. doi: 10.1016/j.biopha.2021.112402. Epub 2021 Nov 10. PMID: 34773763. 2. Tseng AS, Engel FB, Keating MT. The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes. Chem Biol. 2006 Sep;13(9):957-63. doi: 10.1016/j.chembiol.2006.08.004. PMID: 16984885. 3. Verma V, Kumar MJV, Sharma K, Rajaram S, Muddashetty R, Manjithaya R, Behnisch T, Clement JP. Pharmacological intervention in young adolescents rescues synaptic physiology and behavioural deficits in Syngap1+/- mice. Exp Brain Res. 2022 Jan;240(1):289-309. doi: 10.1007/s00221-021-06254-x. Epub 2021 Nov 5. PMID: 34739555. 4. Liu L, Nam S, Tian Y, Yang F, Wu J, Wang Y, Scuto A, Polychronopoulos P, Magiatis P, Skaltsounis L, Jove R. 6-Bromoindirubin-3'-oxime inhibits JAK/STAT3 signaling and induces apoptosis of human melanoma cells. Cancer Res. 2011 Jun 1;71(11):3972-9. doi: 10.1158/0008-5472.CAN-10-3852. Epub 2011 May 24. PMID: 21610112; PMCID: PMC3107399.
In vitro protocol:
1. Park JS, Jung IA, Choi HS, Kim DH, Choi HI, Bae EH, Ma SK, Kim SW. Anti-fibrotic effect of 6-bromo-indirubin-3'-oxime (6-BIO) via regulation of activator protein-1 (AP-1) and specificity protein-1 (SP-1) transcription factors in kidney cells. Biomed Pharmacother. 2022 Jan;145:112402. doi: 10.1016/j.biopha.2021.112402. Epub 2021 Nov 10. PMID: 34773763. 2. Tseng AS, Engel FB, Keating MT. The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes. Chem Biol. 2006 Sep;13(9):957-63. doi: 10.1016/j.chembiol.2006.08.004. PMID: 16984885.
In vivo protocol:
1. Verma V, Kumar MJV, Sharma K, Rajaram S, Muddashetty R, Manjithaya R, Behnisch T, Clement JP. Pharmacological intervention in young adolescents rescues synaptic physiology and behavioural deficits in Syngap1+/- mice. Exp Brain Res. 2022 Jan;240(1):289-309. doi: 10.1007/s00221-021-06254-x. Epub 2021 Nov 5. PMID: 34739555. 2. Liu L, Nam S, Tian Y, Yang F, Wu J, Wang Y, Scuto A, Polychronopoulos P, Magiatis P, Skaltsounis L, Jove R. 6-Bromoindirubin-3'-oxime inhibits JAK/STAT3 signaling and induces apoptosis of human melanoma cells. Cancer Res. 2011 Jun 1;71(11):3972-9. doi: 10.1158/0008-5472.CAN-10-3852. Epub 2011 May 24. PMID: 21610112; PMCID: PMC3107399.
1. Meijer, L., Skaltsounis, A.L., Magiatis, P., et al. GSK-3-selective inhibitors derived from tyrian purple indirubins. Chem. Biol. 10(12), 1255-1266 (2003). 2. Polychronopoulos, P., Magiatis, P., Skaltsounis, A.L., et al. Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases. J. Med. Chem. 47(4), 935-946 (2004). 3. Sato, N., Meijer, L., Skaltsounis, L., et al. Maintenance of pluripotency in human and mouse embryonic stem cells through activation of Wnt signaling by a pharmacological GSK-3-specific inhibitor. Nature Medicine 10(1), 55-63 (2004). 4. Tseng, A.S., Engel, F.B., and Keating, M.T. The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes. Chemistry & Biology 13, 957-963 (2006).