WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H565549
CAS#: 2304465-89-0
Description: F5446 is a SUV39H1 inhibitor. F5446 has an EC50 of 0.496 μmol/L for SUV39H1 enzymatic activity. H3K9me3 was enriched in the promoters of GZMB, PRF1, FASLG, and IFNG in quiescent T cells. F5446 inhibited H3K9me3, thereby upregulating expression of these effectors in tumor-infiltrating CTLs and suppressing colon carcinoma growth in a CD8+ CTL-dependent manner in vivo. Our data indicate that SUV39H1 represses CTL effector gene expression and, in doing so, confers colon cancer immune escape.
Hodoodo Cat#: H565549
Name: F5446
CAS#: 2304465-89-0
Chemical Formula: C26H17ClN2O8S
Exact Mass: 552.04
Molecular Weight: 552.938
Elemental Analysis: C, 56.48; H, 3.10; Cl, 6.41; N, 5.07; O, 23.15; S, 5.80
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Synonym: F5446; F 5446; F-5446
IUPAC/Chemical Name: 1-Benzyl 7-methyl 6-((4-chlorophenyl)sulfonyl)-4,5-dioxo-3,4,5,6-tetrahydropyrrolo[3,2-e]indole-1,7-dicarboxylate
InChi Key: MLPQCOLPRPRADV-UHFFFAOYSA-N
InChi Code: InChI=1S/C26H17ClN2O8S/c1-36-26(33)19-11-17-20-18(25(32)37-13-14-5-3-2-4-6-14)12-28-21(20)23(30)24(31)22(17)29(19)38(34,35)16-9-7-15(27)8-10-16/h2-12,28H,13H2,1H3
SMILES Code: O=C(C1=CNC2=C1C3=C(N(S(=O)(C4=CC=C(Cl)C=C4)=O)C(C(OC)=O)=C3)C(C2=O)=O)OCC5=CC=CC=C5
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: F5446 decreased H3K9me3 deposition at the FAS promoter, increased Fas expression, and increased CRC cell sensitivity to FasL-induced apoptosis in vitro. Furthermore, inhibition of SUV39H1 altered the expression of genes with known functions in DNA replication and cell cycle in the metastatic colon carcinoma cells, which is associated with cell cycle arrest at S phase in the metastatic human colon carcinoma cells, resulting in tumor cell apoptosis and growth inhibition in a concentration-dependent manner in vitro. Moreover, F5446 increased 5-FU-resistant human CRC sensitivity to both 5-FU- and FasL-induced apoptosis and inhibited tumor cell growth in vitro. More importantly, F5446 suppressed human colon tumor xenograft growth in vivo.
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The following data is based on the product molecular weight 552.94 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: Lu C, Klement JD, Yang D, Albers T, Lebedyeva IO, Waller JL, Liu K. SUV39H1 regulates human colon carcinoma apoptosis and cell cycle to promote tumor growth. Cancer Lett. 2020 Apr 28;476:87-96. doi: 10.1016/j.canlet.2020.02.004. Epub 2020 Feb 12. PMID: 32061753; PMCID: PMC7138631.
2: Lu C, Yang D, Klement JD, Oh IK, Savage NM, Waller JL, Colby AH, Grinstaff MW, Oberlies NH, Pearce CJ, Xie Z, Kulp SK, Coss CC, Phelps MA, Albers T, Lebedyeva IO, Liu K. SUV39H1 Represses the Expression of Cytotoxic T-Lymphocyte Effector Genes to Promote Colon Tumor Immune Evasion. Cancer Immunol Res. 2019 Mar;7(3):414-427. doi: 10.1158/2326-6066.CIR-18-0126. Epub 2019 Jan 4. PMID: 30610059; PMCID: PMC6397681.
3: Chen Y, Copeland WK, Vedanthan R, Grant E, Lee JE, Gu D, Gupta PC, Ramadas K, Inoue M, Tsugane S, Tamakoshi A, Gao YT, Yuan JM, Shu XO, Ozasa K, Tsuji I, Kakizaki M, Tanaka H, Nishino Y, Chen CJ, Wang R, Yoo KY, Ahn YO, Ahsan H, Pan WH, Chen CS, Pednekar MS, Sauvaget C, Sasazuki S, Yang G, Koh WP, Xiang YB, Ohishi W, Watanabe T, Sugawara Y, Matsuo K, You SL, Park SK, Kim DH, Parvez F, Chuang SY, Ge W, Rolland B, McLerran D, Sinha R, Thornquist M, Kang D, Feng Z, Boffetta P, Zheng W, He J, Potter JD. Association between body mass index and cardiovascular disease mortality in east Asians and south Asians: pooled analysis of prospective data from the Asia Cohort Consortium. BMJ. 2013 Oct 1;347:f5446. doi: 10.1136/bmj.f5446. PMID: 24473060; PMCID: PMC3788174.