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MedKoo Cat#: 564182 | Name: SGC3027
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Description:

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

SGC3027 is a prodrug form of the protein arginine methyltransferase 7 (PRMT7) inhibitor SGC8158. It is converted by intracellular reductases to SGC8158, which inhibits PRMT7 with an IC50 value of less than 2.5 nM for inhibition of histone H2B (23-37) methylation. SGC3027 inhibits methylation of heat shock protein 70 (Hsp70) in vitro (IC50 = 2.4 µM).

Chemical Structure

SGC3027
SGC3027
CAS# 2624313-13-7

Theoretical Analysis

MedKoo Cat#: 564182

Name: SGC3027

CAS#: 2624313-13-7

Chemical Formula: C41H47ClN6O6S

Exact Mass: 786.2966

Molecular Weight: 787.37

Elemental Analysis: C, 62.54; H, 6.02; Cl, 4.50; N, 10.67; O, 12.19; S, 4.07

Price and Availability

Size Price Availability Quantity
1mg USD 350.00
5mg USD 650.00
10mg USD 1,000.00
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Related CAS #
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Synonym
SGC-3027; SGC 3027; SGC3027
IUPAC/Chemical Name
N-(4-((((2S,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)thio)butyl)-N-((4'-chloro-[1,1'-biphenyl]-3-yl)methyl)-3-methyl-3-(2,4,5-trimethyl-3,6-dioxocyclohexa-1,4-dien-1-yl)butanamide
InChi Key
MLJVGAYSVYMPSB-MSUKGTQXSA-N
InChi Code
InChI=1S/C41H47ClN6O6S/c1-23-24(2)35(51)32(25(3)34(23)50)41(4,5)18-31(49)47(19-26-9-8-10-28(17-26)27-11-13-29(42)14-12-27)15-6-7-16-55-20-30-36(52)37(53)40(54-30)48-22-46-33-38(43)44-21-45-39(33)48/h8-14,17,21-22,30,36-37,40,52-53H,6-7,15-16,18-20H2,1-5H3,(H2,43,44,45)/t30-,36-,37-,40-/m1/s1
SMILES Code
O=C1C(C)=C(C)C(C(C(C)(C)CC(N(CC2=CC(C3=CC=C(Cl)C=C3)=CC=C2)CCCCSC[C@@H]4[C@@H](O)[C@@H](O)[C@H](N5C(N=CN=C6N)=C6N=C5)O4)=O)=C1C)=O
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
To be determined
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
2934.99.03.00
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
SGC3027 is converted by intracellular reductases to SGC8158, which inhibits PRMT7 with an IC50 value of less than 2.5 nM for inhibition of histone H2B (23-37) methylation. SGC3027 inhibits methylation of Hsp70 in vitro (IC50 = 2.4 µM).
In vitro activity:
In cells, SGC3027 inhibits methylation of both constitutive and inducible forms of HSP70, and leads to decreased tolerance for perturbations of proteostasis including heat shock and proteasome inhibitors. SGC3027 is a cell permeable prodrug, which in cells is converted to SGC8158, a potent, SAM-competitive PRMT7 inhibitor. Reference: Erratum in: Nat Commun. 2020 May 26;11(1):2683. https://pubmed.ncbi.nlm.nih.gov/32409666/
In vivo activity:
To be determined

Preparing Stock Solutions

The following data is based on the product molecular weight 787.37 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. Zhang M, Chen C, Lu Z, Cai Y, Li Y, Zhang F, Liu Y, Chen S, Zhang H, Yang S, Gen H, Jiang Y, Ning C, Huang J, Wang W, Fan L, Zhang Y, Jin M, Han J, Xiong Z, Cai M, Liu J, Huang C, Yang X, Xu B, Li H, Li B, Zhu X, Wei Y, Zhu Y, Tian J, Miao X. Genetic Control of Alternative Splicing and its Distinct Role in Colorectal Cancer Mechanisms. Gastroenterology. 2023 Nov;165(5):1151-1167. doi: 10.1053/j.gastro.2023.07.019. Epub 2023 Aug 3. PMID: 37541527. 2. Szewczyk MM, Ishikawa Y, Organ S, Sakai N, Li F, Halabelian L, Ackloo S, Couzens AL, Eram M, Dilworth D, Fukushi H, Harding R, Dela Seña CC, Sugo T, Hayashi K, McLeod D, Zepeda C, Aman A, Sánchez-Osuna M, Bonneil E, Takagi S, Al-Awar R, Tyers M, Richard S, Takizawa M, Gingras AC, Arrowsmith CH, Vedadi M, Brown PJ, Nara H, Barsyte-Lovejoy D. Pharmacological inhibition of PRMT7 links arginine monomethylation to the cellular stress response. Nat Commun. 2020 May 14;11(1):2396. doi: 10.1038/s41467-020-16271-z. Erratum in: Nat Commun. 2020 May 26;11(1):2683. PMID: 32409666; PMCID: PMC7224190.
In vitro protocol:
1. Zhang M, Chen C, Lu Z, Cai Y, Li Y, Zhang F, Liu Y, Chen S, Zhang H, Yang S, Gen H, Jiang Y, Ning C, Huang J, Wang W, Fan L, Zhang Y, Jin M, Han J, Xiong Z, Cai M, Liu J, Huang C, Yang X, Xu B, Li H, Li B, Zhu X, Wei Y, Zhu Y, Tian J, Miao X. Genetic Control of Alternative Splicing and its Distinct Role in Colorectal Cancer Mechanisms. Gastroenterology. 2023 Nov;165(5):1151-1167. doi: 10.1053/j.gastro.2023.07.019. Epub 2023 Aug 3. PMID: 37541527. 2. Szewczyk MM, Ishikawa Y, Organ S, Sakai N, Li F, Halabelian L, Ackloo S, Couzens AL, Eram M, Dilworth D, Fukushi H, Harding R, Dela Seña CC, Sugo T, Hayashi K, McLeod D, Zepeda C, Aman A, Sánchez-Osuna M, Bonneil E, Takagi S, Al-Awar R, Tyers M, Richard S, Takizawa M, Gingras AC, Arrowsmith CH, Vedadi M, Brown PJ, Nara H, Barsyte-Lovejoy D. Pharmacological inhibition of PRMT7 links arginine monomethylation to the cellular stress response. Nat Commun. 2020 May 14;11(1):2396. doi: 10.1038/s41467-020-16271-z. Erratum in: Nat Commun. 2020 May 26;11(1):2683. PMID: 32409666; PMCID: PMC7224190.
In vivo protocol:
To be determined
Zhang M, Chen C, Lu Z, Cai Y, Li Y, Zhang F, Liu Y, Chen S, Zhang H, Yang S, Gen H, Jiang Y, Ning C, Huang J, Wang W, Fan L, Zhang Y, Jin M, Han J, Xiong Z, Cai M, Liu J, Huang C, Yang X, Xu B, Li H, Li B, Zhu X, Wei Y, Zhu Y, Tian J, Miao X. Genetic Control of Alternative Splicing and its Distinct Role in Colorectal Cancer Mechanisms. Gastroenterology. 2023 Nov;165(5):1151-1167. doi: 10.1053/j.gastro.2023.07.019. Epub 2023 Aug 3. PMID: 37541527. Srour N, Villarreal OD, Hardikar S, Yu Z, Preston S, Miller WH Jr, Szewczyk MM, Barsyte-Lovejoy D, Xu H, Chen T, Del Rincón SV, Richard S. PRMT7 ablation stimulates anti-tumor immunity and sensitizes melanoma to immune checkpoint blockade. Cell Rep. 2022 Mar 29;38(13):110582. doi: 10.1016/j.celrep.2022.110582. PMID: 35354055; PMCID: PMC9838175. Szewczyk MM, Ishikawa Y, Organ S, Sakai N, Li F, Halabelian L, Ackloo S, Couzens AL, Eram M, Dilworth D, Fukushi H, Harding R, Dela Seña CC, Sugo T, Hayashi K, McLeod D, Zepeda C, Aman A, Sánchez-Osuna M, Bonneil E, Takagi S, Al-Awar R, Tyers M, Richard S, Takizawa M, Gingras AC, Arrowsmith CH, Vedadi M, Brown PJ, Nara H, Barsyte-Lovejoy D. Pharmacological inhibition of PRMT7 links arginine monomethylation to the cellular stress response. Nat Commun. 2020 May 14;11(1):2396. doi: 10.1038/s41467-020-16271-z. Erratum in: Nat Commun. 2020 May 26;11(1):2683. doi: 10.1038/s41467-020-16613-x. PMID: 32409666; PMCID: PMC7224190.