Molecular structure of BI-D1870, CAS Number: 501437-28-1
BI-D1870 (CAS 501437-28-1)
See product citations (12)
Alternate Names:
BI-D1870 is known as an inhibitor of RSK1-4.
Application:
BI-D1870 is a cell permeable, ATP-competitive inhibitor of the four isoforms of ribosomal S6 kinase (p90 RSK).
CAS Number:
501437-28-1
Purity:
≥98%
Molecular Weight:
391.41
Molecular Formula:
C19H23F2N5O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
BI-D1870 is a cell permeable, ATP-competitive inhibitor of the four isoforms of ribosomal S6 kinase (p90 RSK) (IC50′s at 100muM ATP: Rsk-1 = 31nM, Rsk-2 = 24nM, Rsk-3 = 18nM, Rsk-4 = 15nM). BI-D1870 does not significantly inhibit 10 other AGC kinases, and over 40 other protein kinases at 100X concentrations. BI-D1870 acts on the N-terminal AGC kinase domain and completely prevents PMA-induced TSC2 phosphorylation.
BI-D1870 (CAS 501437-28-1) References
- BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. | Sapkota, GP., et al. 2007. Biochem J. 401: 29-38. PMID: 17040210
- Differential regulation of NHE1 phosphorylation and glucose uptake by inhibitors of the ERK pathway and p90RSK in 3T3-L1 adipocytes. | Chen, S. and Mackintosh, C. 2009. Cell Signal. 21: 1984-93. PMID: 19765648
- Overcoming resistance to Sonic Hedgehog inhibition by targeting p90 ribosomal S6 kinase in pediatric medulloblastoma. | Pambid, MR., et al. 2014. Pediatr Blood Cancer. 61: 107-15. PMID: 23940083
- The p90 ribosomal S6 kinase (RSK) inhibitor BI-D1870 prevents gamma irradiation-induced apoptosis and mediates senescence via RSK- and p53-independent accumulation of p21WAF1/CIP1. | Neise, D., et al. 2013. Cell Death Dis. 4: e859. PMID: 24136223
- Antitumor effects of BI-D1870 on human oral squamous cell carcinoma. | Chiu, CF., et al. 2014. Cancer Chemother Pharmacol. 73: 237-47. PMID: 24241211
- Two widely used RSK inhibitors, BI-D1870 and SL0101, alter mTORC1 signaling in a RSK-independent manner. | Roffé, M., et al. 2015. Cell Signal. 27: 1630-42. PMID: 25889895
- The ribosomal S6 kinase inhibitor BI-D1870 ameliorated experimental autoimmune encephalomyelitis in mice. | Takada, I., et al. 2016. Immunobiology. 221: 188-92. PMID: 26386981
- A combination of SILAC and nucleotide acyl phosphate labelling reveals unexpected targets of the Rsk inhibitor BI-D1870. | Edgar, AJ., et al. 2014. Biosci Rep. 34: PMID: 27919044
- Serine-227 in the N-terminal kinase domain of RSK2 is a potential therapeutic target for mantle cell lymphoma. | Matsumura-Kimoto, Y., et al. 2020. Cancer Med. 9: 5185-5199. PMID: 32420699
- RSK inhibitor BI-D1870 inhibits acute myeloid leukemia cell proliferation by targeting mitotic exit. | Chae, HD., et al. 2020. Oncotarget. 11: 2387-2403. PMID: 32637030
- Inhibition of p90 ribosomal S6 kinase potentiates cisplatin activity in A549 human lung adenocarcinoma cells. | Abdulrahman, N., et al. 2020. J Pharm Pharmacol. 72: 1536-1545. PMID: 32667058
- RSK Inhibition Induces Apoptosis by Downregulating Protein Synthesis in a Variety of Acute Myeloid Leukemia Cell Lines. | Katayama, K. and Nishihata, A. 2021. Biol Pharm Bull. 44: 1843-1850. PMID: 34602526
- BI-D1870 Induces Mitotic Dysfunction and Apoptosis in Neuroblastoma by Regulating the PI3K-Akt-mTORC1 Signal Axis. | Jin, L., et al. 2023. Cancers (Basel). 15: PMID: 37046682
Inhibitor of:
ACBD6, ANKLE2, AP-2β, CCDC64B, DSCP1, EG432879, FAM200B, FMIP, LHFPL4, Melanocortin receptor (MC-R), p70 S6 kinase α, Pim-3, Prickle1, RasGRP1, RIA1, Ribosomal Protein S6, RIOK1, Rsk, Rsk-1, Rsk-2, Rsk-3, Rsk-4, Rsk3, SAP-1, SGK3, SPATA19, SSTK-IP, TGN38B, ubiquitous kinesin heavy chain, and VRK3.Activator of:
ARP-1, eIF4B, HOOK1, HVEM, Krs-2, MAD1, Rsk-3, and TORC2.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
BI-D1870, 1 mg | sc-397022 | 1 mg | $90.00 | |||
BI-D1870, 5 mg | sc-397022A | 5 mg | $275.00 |