General Information of the Drug (ID: M6APDG00307)
Name
SB-747651A
Synonyms
SB-747651A; CHEMBL188434; compound 26; SCHEMBL4719834; GTPL8130; BDBM24996; oxadiazole-containing compound, 9; MBCJUIJWPYUEBX-UHFFFAOYSA-N; ZINC13998530; NCGC00273984-05; NCGC00273984-03; SB-747651; 4-{1-ethyl-7-[(piperidin-4-ylamino)methyl]-1H-imidazo[4,5-c]pyridin-2-yl}-1,2,5-oxadiazol-3-amine; [2-(4-Amino-furazan-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-7-ylmethyl]-piperidin-4-yl-amine
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Status
Investigative
Structure
Formula
C16H22N8O
InChI
1S/C16H22N8O/c1-2-24-14-10(8-20-11-3-5-18-6-4-11)7-19-9-12(14)21-16(24)13-15(17)23-25-22-13/h7,9,11,18,20H,2-6,8H2,1H3,(H2,17,23)
InChIKey
MBCJUIJWPYUEBX-UHFFFAOYSA-N
PubChem CID
11393719
TTD Drug ID
D0I1FJ
Target Gene(s) and Their Upstream m6A Regulator, Together with the Effect of Target Gene(s) in Drug Response
The target genes involved in drug-target interaction (such as drug-metabolizing enzymes, drug transporters and therapeutic targets) and drug-mediated cell death signaling (including modulating DNA damage and repair capacity, escaping from drug-induced apoptosis, autophagy, cellular metabolic reprogramming, oncogenic bypass signaling, cell microenvironment, cell stemness, etc.) could be regulated by m6A regulator(s) and affected their corresponding drug response. You can browse detailed information on drug-related target gene(s) mediated by m6A regulators.
RAC-alpha serine/threonine-protein kinase (AKT1)
Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1)
In total 1 mechanisms lead to this potential drug response
Response Summary RAC-alpha serine/threonine-protein kinase (AKT1) is a therapeutic target for SB-747651A. The Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) has potential in affecting the response of SB-747651A through regulating the expression of RAC-alpha serine/threonine-protein kinase (AKT1). [1], [2]
Insulin-like growth factor 2 mRNA-binding protein 2 (IGF2BP2)
In total 1 mechanisms lead to this potential drug response
Response Summary RAC-alpha serine/threonine-protein kinase (AKT1) is a therapeutic target for SB-747651A. The Insulin-like growth factor 2 mRNA-binding protein 2 (IGF2BP2) has potential in affecting the response of SB-747651A through regulating the expression of RAC-alpha serine/threonine-protein kinase (AKT1). [2], [3]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
Response Summary RAC-alpha serine/threonine-protein kinase (AKT1) is a therapeutic target for SB-747651A. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of SB-747651A through regulating the expression of RAC-alpha serine/threonine-protein kinase (AKT1). [2], [4]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary RAC-alpha serine/threonine-protein kinase (AKT1) is a therapeutic target for SB-747651A. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of SB-747651A through regulating the expression of RAC-alpha serine/threonine-protein kinase (AKT1). [2], [5]
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
Response Summary RAC-alpha serine/threonine-protein kinase (AKT1) is a therapeutic target for SB-747651A. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of SB-747651A through regulating the expression of RAC-alpha serine/threonine-protein kinase (AKT1). [2], [6]
YTH domain-containing family protein 1 (YTHDF1)
In total 1 mechanisms lead to this potential drug response
Response Summary RAC-alpha serine/threonine-protein kinase (AKT1) is a therapeutic target for SB-747651A. The YTH domain-containing family protein 1 (YTHDF1) has potential in affecting the response of SB-747651A through regulating the expression of RAC-alpha serine/threonine-protein kinase (AKT1). [2], [7]
YTH domain-containing family protein 2 (YTHDF2)
In total 1 mechanisms lead to this potential drug response
Response Summary RAC-alpha serine/threonine-protein kinase (AKT1) is a therapeutic target for SB-747651A. The YTH domain-containing family protein 2 (YTHDF2) has potential in affecting the response of SB-747651A through regulating the expression of RAC-alpha serine/threonine-protein kinase (AKT1). [2], [8]
YTH domain-containing family protein 3 (YTHDF3)
In total 1 mechanisms lead to this potential drug response
Response Summary RAC-alpha serine/threonine-protein kinase (AKT1) is a therapeutic target for SB-747651A. The YTH domain-containing family protein 3 (YTHDF3) has potential in affecting the response of SB-747651A through regulating the expression of RAC-alpha serine/threonine-protein kinase (AKT1). [2], [3]
YTH domain-containing protein 2 (YTHDC2)
In total 1 mechanisms lead to this potential drug response
Response Summary RAC-alpha serine/threonine-protein kinase (AKT1) is a therapeutic target for SB-747651A. The YTH domain-containing protein 2 (YTHDC2) has potential in affecting the response of SB-747651A through regulating the expression of RAC-alpha serine/threonine-protein kinase (AKT1). [2], [9]
RAC-gamma serine/threonine-protein kinase (AKT3)
Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1)
In total 1 mechanisms lead to this potential drug response
Response Summary RAC-gamma serine/threonine-protein kinase (AKT3) is a therapeutic target for SB-747651A. The Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) has potential in affecting the response of SB-747651A through regulating the expression of RAC-gamma serine/threonine-protein kinase (AKT3). [10], [11]
Ribosomal protein S6 kinase beta-1 (S6K1)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Ribosomal protein S6 kinase beta-1 (S6K1) is a therapeutic target for SB-747651A. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of SB-747651A through regulating the expression of Ribosomal protein S6 kinase beta-1 (S6K1). [12], [13]
References
Ref 1 HNRNPA2B1 regulates tamoxifen- and fulvestrant-sensitivity and hallmarks of endocrine resistance in breast cancer cells. Cancer Lett. 2021 Oct 10;518:152-168. doi: 10.1016/j.canlet.2021.07.015. Epub 2021 Jul 14.
Ref 2 Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. J Med Chem. 2005 Sep 8;48(18):5639-43. doi: 10.1021/jm050392q.
Ref 3 N6-methyladenosine reader YTH N6-methyladenosine RNA binding protein 3 or insulin like growth factor 2 mRNA binding protein 2 knockdown protects human bronchial epithelial cells from hypoxia/reoxygenation injury by inactivating p38 MAPK, AKT, ERK1/2, and NF-KappaB pathways. Bioengineered. 2022 May;13(5):11973-11986. doi: 10.1080/21655979.2021.1999550.
Ref 4 METTL14 Inhibits Hepatocellular Carcinoma Metastasis Through Regulating EGFR/PI3K/AKT Signaling Pathway in an m6A-Dependent Manner. Cancer Manag Res. 2020 Dec 23;12:13173-13184. doi: 10.2147/CMAR.S286275. eCollection 2020.
Ref 5 Methyltransferase-like 3 promotes the progression of lung cancer via activating PI3K/AKT/mTOR pathway. Clin Exp Pharmacol Physiol. 2022 Jul;49(7):748-758. doi: 10.1111/1440-1681.13647. Epub 2022 May 23.
Ref 6 ALKBH5-mediated m(6)A demethylation of KCNK15-AS1 inhibits pancreatic cancer progression via regulating KCNK15 and PTEN/AKT signaling. Cell Death Dis. 2021 Dec 1;12(12):1121. doi: 10.1038/s41419-021-04401-4.
Ref 7 YTHDF1 promotes hepatocellular carcinoma progression via activating PI3K/AKT/mTOR signaling pathway and inducing epithelial-mesenchymal transition. Exp Hematol Oncol. 2021 Jun 4;10(1):35. doi: 10.1186/s40164-021-00227-0.
Ref 8 YTHDF2 mediates the mRNA degradation of the tumor suppressors to induce AKT phosphorylation in N6-methyladenosine-dependent way in prostate cancer. Mol Cancer. 2020 Oct 29;19(1):152. doi: 10.1186/s12943-020-01267-6.
Ref 9 m(6)A Reader YTHDC2 Promotes Radiotherapy Resistance of Nasopharyngeal Carcinoma via Activating IGF1R/AKT/S6 Signaling Axis. Front Oncol. 2020 Jul 31;10:1166. doi: 10.3389/fonc.2020.01166. eCollection 2020.
Ref 10 HNRNPA2B1 promotes multiple myeloma progression by increasing AKT3 expression via m6A-dependent stabilization of ILF3 mRNA. J Hematol Oncol. 2021 Apr 1;14(1):54. doi: 10.1186/s13045-021-01066-6.
Ref 11 US patent application no. 6,395,545, Antisense modulation of inhibitor-kappa B kinase-alpha expression.
Ref 12 m(6)A methyltransferase METTL3 promotes retinoblastoma progression via PI3K/AKT/mTOR pathway. J Cell Mol Med. 2020 Oct 8;24(21):12368-78. doi: 10.1111/jcmm.15736. Online ahead of print.
Ref 13 3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3). Bioorg Med Chem Lett. 2001 Mar 12;11(5):635-9. doi: 10.1016/s0960-894x(00)00721-6.