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MedKoo Cat#: 471044 | Name: SGC-iMLLT
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Description:

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

SGC-iMLLT, a chemical probe, is a selective inhibitor of the YEATS domain-containing proteins MLLT1 and MLLT3.

Chemical Structure

SGC-iMLLT
SGC-iMLLT
CAS#2255338-25-9

Theoretical Analysis

MedKoo Cat#: 471044

Name: SGC-iMLLT

CAS#: 2255338-25-9

Chemical Formula: C22H24N6O

Exact Mass: 388.2012

Molecular Weight: 388.48

Elemental Analysis: C, 68.02; H, 6.23; N, 21.63; O, 4.12

Price and Availability

Size Price Availability Quantity
1mg USD 300.00 2 weeks
5mg USD 500.00 2 weeks
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Related CAS #
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Synonym
SGCiMLLT, SGC-iMLLT, SGC iMLLT
IUPAC/Chemical Name
6'-amino-N-(2-morpholinooxazolo[4,5-b]pyridin-6-yl)-[2,3'-bipyridine]-6-carboxamide
InChi Key
RWIMETUXCNDSLE-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H19N7O3/c22-18-5-4-13(11-23-18)15-2-1-3-16(26-15)20(29)25-14-10-17-19(24-12-14)27-21(31-17)28-6-8-30-9-7-28/h1-5,10-12H,6-9H2,(H2,22,23)(H,25,29)
SMILES Code
O=C(C1=CC=CC(C2=CC=C(N)N=C2)=N1)NC3=CN=C4C(OC(N5CCOCC5)=N4)=C3
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
>3 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:
SGC-iMLLT is a selective inhibitor of MLLT1/3-histone interactions with an IC50 of 0.26 μM. SGC-iMLLT shows high binding activity towards MLLT1 YEATS domain (YD) and MLLT3 YD (AF9/YEATS3) with Kds of 0.129 and 0.077 μM, respectively.
In vitro activity:
SGC-iMLLT can be used to understand MLLT1/3-associated biology and the therapeutic potential of small-molecule YEATS domain (YD) inhibitors. SGC-iMLLT has excellent selectivity over other human YD proteins (YEATS2/4) and bromodomains. SGC-iMLLT displays cellular target engagement of MLLT1 and MLLT3. Reference: Angew Chem Int Ed Engl. 2018 Dec 10;57(50):16302-16307. https://pubmed.ncbi.nlm.nih.gov/30288907/
In vivo activity:
To be determined
Solvent mg/mL mM comments
Solubility
DMSO 83.3 214.51
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 388.48 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. Hu H, Saha N, Yang Y, Ahmad E, Lachowski L, Shrestha U, Premkumar V, Ropa J, Chen L, Teahan B, Grigsby S, Marschalek R, Nikolovska-Coleska Z, Muntean AG. The ENL YEATS epigenetic reader domain critically links MLL-ENL to leukemic stem cell frequency in t(11;19) Leukemia. Leukemia. 2023 Jan;37(1):190-201. doi: 10.1038/s41375-022-01765-0. Epub 2022 Nov 26. PMID: 36435883. 2. Moustakim M, Christott T, Monteiro OP, Bennett J, Giroud C, Ward J, Rogers CM, Smith P, Panagakou I, Díaz-Sáez L, Felce SL, Gamble V, Gileadi C, Halidi N, Heidenreich D, Chaikuad A, Knapp S, Huber KVM, Farnie G, Heer J, Manevski N, Poda G, Al-Awar R, Dixon DJ, Brennan PE, Fedorov O. Discovery of an MLLT1/3 YEATS Domain Chemical Probe. Angew Chem Int Ed Engl. 2018 Dec 10;57(50):16302-16307. doi: 10.1002/anie.201810617. Epub 2018 Nov 16. PMID: 30288907; PMCID: PMC6348381.
In vitro protocol:
1. Hu H, Saha N, Yang Y, Ahmad E, Lachowski L, Shrestha U, Premkumar V, Ropa J, Chen L, Teahan B, Grigsby S, Marschalek R, Nikolovska-Coleska Z, Muntean AG. The ENL YEATS epigenetic reader domain critically links MLL-ENL to leukemic stem cell frequency in t(11;19) Leukemia. Leukemia. 2023 Jan;37(1):190-201. doi: 10.1038/s41375-022-01765-0. Epub 2022 Nov 26. PMID: 36435883. 2. Moustakim M, Christott T, Monteiro OP, Bennett J, Giroud C, Ward J, Rogers CM, Smith P, Panagakou I, Díaz-Sáez L, Felce SL, Gamble V, Gileadi C, Halidi N, Heidenreich D, Chaikuad A, Knapp S, Huber KVM, Farnie G, Heer J, Manevski N, Poda G, Al-Awar R, Dixon DJ, Brennan PE, Fedorov O. Discovery of an MLLT1/3 YEATS Domain Chemical Probe. Angew Chem Int Ed Engl. 2018 Dec 10;57(50):16302-16307. doi: 10.1002/anie.201810617. Epub 2018 Nov 16. PMID: 30288907; PMCID: PMC6348381.
In vivo protocol:
To be determined
1. Moustakim M, et al. Discovery of an MLLT1/3 YEATS Domain Chemical Probe. Angew Chem Int Ed Engl. 2018 Dec 10;57(50):16302-16307. 2: Hu H, Saha N, Yang Y, Ahmad E, Lachowski L, Shrestha U, Premkumar V, Ropa J, Chen L, Teahan B, Grigsby S, Marschalek R, Nikolovska-Coleska Z, Muntean AG. The ENL YEATS epigenetic reader domain critically links MLL-ENL to leukemic stem cell frequency in t(11;19) Leukemia. Leukemia. 2023 Jan;37(1):190-201. doi: 10.1038/s41375-022-01765-0. Epub 2022 Nov 26. PMID: 36435883; PMCID: PMC11246743. 3: Guo S, Jia T, Xu X, Yang F, Xiao S, Hou Z, Xu H, Ma S, Liu X, Luo C, Jiang H, Chen H, Chen S. Design, synthesis of novel benzimidazole derivatives as ENL inhibitors suppressing leukemia cells viability via downregulating the expression of MYC. Eur J Med Chem. 2023 Feb 15;248:115093. doi: 10.1016/j.ejmech.2023.115093. Epub 2023 Jan 10. PMID: 36645983.