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Staurosporine - 98%, high purity , CAS No.62996-74-1, Inhibitor of calcium/calmodulin-dependent protein kinase II beta subunit;Inhibitor of death associated protein kinase 1;Inhibitor of homeodomain interacting protein kinase 1;Inhibitor of mitogen-activated protein kinase kinase 4;Inhibitor of mitogen-activ

Moligand™
≥98%

CAS#: 62996-74-1
Formula: C₂₈H₂₆N₄O₃
Molecular Weight: 466.53
Beilstein Registry Number: 1060573
MDL number: MFCD00077402
PubChem CID: 44259

Item Number

S102392

Grouped product items
SKU	Size	Availability	Price	Qty
S102392-1mg	1mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$31.90
S102392-5mg	5mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$129.90

Protein kinase inhibitor

View related series

calcium/calmodulin-dependent protein kinase II beta subunit Inhibitor death associated protein kinase 1 Inhibitor homeodomain interacting protein kinase 1 Inhibitor M1 receptor Allosteric modulator M2 receptor Allosteric modulator M4 receptor Allosteric modulator mitogen-activated protein kinase kinase 4 Inhibitor mitogen-activated protein kinase kinase 6 Inhibitor p21 (RAC1) activated kinase 2 Inhibitor phosphorylase kinase catalytic subunit gamma 2 Inhibitor protein kinase C iota Inhibitor protein kinase N1 Inhibitor protein kinase，cAMP-dependent，catalytic，beta subunit Inhibitor serine/threonine kinase 3 Inhibitor TRAF2 and NCK interacting kinase Inhibitor

Basic Description

Synonyms	staurosporine\|Staurosporin\|62996-74-1\|(+)-Staurosporine\|Antibiotic 230\|Antibiotic AM 2282\|AM-2282\|CCRIS 3272\|Antibiotic AM-2282\|Alkaloid AM-2282 from Streptomyces\|(5S,6R,7R,9R)-6-methoxy-5-methyl-7-(methylamino)-6,7,8,9,15,16-hexahydro-5H,14H-17-oxa-4b,9a
Specifications & Purity	Moligand™, ≥98%
Biochemical and Physiological Mechanisms	Staurosporine (Stsp) is potent inhibitor of protein kinase C (PKC) from rat brain, exhibiting an IC50 value of 2.7 nM. It inhibits rat recombinant PKC-α approximately 100- and 1,000-fold better than PKC-δ and PKC-ζ, respectively.2 However, Stsp is non-sel
Storage Temp	Store at 2-8°C
Shipped In	Wet ice
Grade	Moligand™
Action Type	ALLOSTERIC MODULATOR, INHIBITOR
Mechanism of action	Inhibitor of calcium/calmodulin-dependent protein kinase II beta subunit;Inhibitor of death associated protein kinase 1;Inhibitor of homeodomain interacting protein kinase 1;Inhibitor of mitogen-activated protein kinase kinase 4;Inhibitor of mitogen-activ
Note	This product is supplied in one (or more) pack size which is freeze dried. Therefore the contents may not be readily visible, as they can coat the bottom or walls of the vial. Please see our FAQs and information page for more details on handling. Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description	Staurosporine is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM). Phase 3.

Associated Targets

CDK1 Tchem Cyclin-dependent kinase 1 4 Activities

Discover Target: CDK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ERBB4 Tclin Receptor tyrosine-protein kinase erbB-4 2 Activities

Discover Target: ERBB4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EPHB6 Tchem Ephrin type-B receptor 6 0 Activities

Discover Target: EPHB6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ERBB2 Tclin Receptor tyrosine-protein kinase erbB-2 1 Activities

Discover Target: ERBB2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EGFR Tclin Epidermal growth factor receptor 12 Activities

Discover Target: EGFR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK9 Tchem Cyclin-dependent kinase 9 0 Activities

Discover Target: CDK9

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDKL5 Tchem Cyclin-dependent kinase-like 5 0 Activities

Discover Target: CDKL5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK18 Tchem Cyclin-dependent kinase 18 0 Activities

Discover Target: CDK18

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 8 Activities

Discover Target: CDK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT4 Tclin Vascular endothelial growth factor receptor 3 9 Activities

Discover Target: FLT4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

YES1 Tclin Tyrosine-protein kinase Yes 4 Activities

Discover Target: YES1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TYK2 Tclin Non-receptor tyrosine-protein kinase TYK2 4 Activities

Discover Target: TYK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 32 Activities

Discover Target: FLT3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR2 Tclin Fibroblast growth factor receptor 2 6 Activities

Discover Target: FGFR2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 8 Activities

Discover Target: FGFR3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MET Tclin Hepatocyte growth factor receptor 0 Activities

Discover Target: MET

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

IGF1R Tclin Insulin-like growth factor 1 receptor 1 Activities

Discover Target: IGF1R

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PRKACG Tchem cAMP-dependent protein kinase catalytic subunit gamma 2 Activities

Discover Target: PRKACG

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TERT Tchem Telomerase reverse transcriptase 0 Activities

Discover Target: TERT

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PLK4 Tchem Serine/threonine-protein kinase PLK4 5 Activities

Discover Target: PLK4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PIM1 Tchem Serine/threonine-protein kinase pim-1 15 Activities

Discover Target: PIM1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PIK3CG Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 0 Activities

Discover Target: PIK3CG

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDGFRA Tclin Platelet-derived growth factor receptor alpha 8 Activities

Discover Target: PDGFRA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PIM2 Tchem Serine/threonine-protein kinase pim-2 7 Activities

Discover Target: PIM2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PIK3CB Tchem Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform 0 Activities

Discover Target: PIK3CB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PIM3 Tchem Serine/threonine-protein kinase pim-3 5 Activities

Discover Target: PIM3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PRKG2 Tchem cGMP-dependent protein kinase 2 4 Activities

Discover Target: PRKG2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RPS6KA2 Tchem Ribosomal protein S6 kinase alpha-2 5 Activities

Discover Target: RPS6KA2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PRKCH Tchem Protein kinase C eta type 6 Activities

Discover Target: PRKCH

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PRKD1 Tchem Serine/threonine-protein kinase D1 4 Activities

Discover Target: PRKD1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BTK Tclin Tyrosine-protein kinase BTK 5 Activities

Discover Target: BTK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKA Tchem Aurora kinase A 19 Activities

Discover Target: AURKA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKB Tchem Aurora kinase B 13 Activities

Discover Target: AURKB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AAK1 Tchem AP2-associated protein kinase 1 3 Activities

Discover Target: AAK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TNK2 Tclin Activated CDC42 kinase 1 4 Activities

Discover Target: TNK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHRM4 Tclin Muscarinic acetylcholine receptor M4 1 Activities

Discover Target: CHRM4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ACHE Tclin Acetylcholinesterase 0 Activities

Discover Target: ACHE

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 10 Activities

Discover Target: ABL1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AKT2 Tchem RAC-beta serine/threonine-protein kinase 5 Activities

Discover Target: AKT2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AKT1 Tchem RAC-alpha serine/threonine-protein kinase 18 Activities

Discover Target: AKT1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CLK3 Tchem Dual specificity protein kinase CLK3 0 Activities

Discover Target: CLK3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BCHE Tclin Cholinesterase 0 Activities

Discover Target: BCHE

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 18 Activities

Discover Target: GSK3B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KIT Tclin Mast/stem cell growth factor receptor Kit 18 Activities

Discover Target: KIT

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 0 Activities

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NTRK1 Tclin High affinity nerve growth factor receptor 10 Activities

Discover Target: NTRK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MTOR Tclin Serine/threonine-protein kinase mTOR 0 Activities

Discover Target: MTOR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one
INCHI	InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
InChi Key	HKSZLNNOFSGOKW-FYTWVXJKSA-N
Canonical SMILES	CC12C(C(CC(O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)NC)OC
Isomeric SMILES	C[C@@]12[C@@H]([C@@H](C[C@@H](O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)NC)OC
WGK Germany	3
PubChem CID	44259
Molecular Weight	466.53
Beilstein	1060573

Database links

PubChem CID	44259
ChEBI	CHEBI:15738
CAS Registry No.	62996-74-1
ChEMBL Ligand	CHEMBL388978
BindingDB Ligand	2579
Wikipedia	Staurosporine
DrugBank Ligand	DB02010
DiscoveRx TREEspot	Staurosporine\|
RCSB PDB Ligand	STU
GPCRdb Ligand	staurosporine

Certificates

Certificate of Analysis(COA)

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2 results found

Lot Number	Certificate Type	Date	Item
H1815136	Certificate of Analysis	Mar 06, 2024	S102392
H1815135	Certificate of Analysis	Mar 06, 2024	S102392

Safety and Hazards(GHS)

Pictogram(s)	GHS06, GHS08, GHS09, GHS07
Signal	Danger
Hazard Statements	H351:Suspected of causing cancer H373:Causes damage to organs through prolonged or repeated exposure H413:May cause long lasting harmful effects to aquatic life H302:Harmful if swallowed H228:Flammable solid H400:Very toxic to aquatic life H410:Very toxic to aquatic life with long lasting effects H300:Fatal if swallowed H310:Fatal in contact with skin H340:May cause genetic defects H350:May cause cancer H361:Suspected of damaging fertility or the unborn child H361d:Suspected of damaging the unborn child
Precautionary Statements	P273:Avoid release to the environment. P280:Wear protective gloves/protective clothing/eye protection/face protection. P370+P378:In case of fire: Use ... to extinguish. P210:Keep away from heat, hot surface, sparks, open flames and other ignition sources. - No smoking. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P240:Ground/bond container and receiving equipment. P264:Wash hands [and …] thoroughly after handling. P260:Do not breathe dust/fume/gas/mist/vapors/spray. P281:Use personal protective equipment as required. P241:Use explosion-proof [electrical/ventilating/lighting/.../] equipment. P270:Do not eat, drink or smoke when using this product. P391:Collect spillage. P330:Rinse mouth. P262:Do not get in eyes, on skin, or on clothing. P361+P364:Take off immediately all contaminated clothing and wash it before reuse. P203:Obtain, read and follow all safety instructions before use. P301+P316:IF SWALLOWED: Get emergency medical help immediately. P301+P317:IF SWALLOWED: Get medical help. P318:if exposed or concerned, get medical advice. P316:Get emergency medical help immediately. P319:Get medical help if you feel unwell.
WGK Germany	3

References

1. Omura S, Iwai Y, Hirano A, Nakagawa A, Awaya J, Tsuchya H, Takahashi Y, Masuma R. (1977) A new alkaloid AM-2282 OF Streptomyces origin. Taxonomy, fermentation, isolation and preliminary characterization.. J Antibiot, 30 (4): (275-82). [PMID:863788]
2. Rüegg UT, Burgess GM. (1989) Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases.. Trends Pharmacol Sci, 10 (6): (218-20). [PMID:2672462]
3. Devaiah BN, Lewis BA, Cherman N, Hewitt MC, Albrecht BK, Robey PG, Ozato K, Sims 3rd RJ, Singer DS. (2012) BRD4 is an atypical kinase that phosphorylates serine2 of the RNA polymerase II carboxy-terminal domain.. Proc Natl Acad Sci USA, 109 (18): (6927-32). [PMID:22509028]
4. Sanders DW, Jumper CC, Ackerman PJ, Bracha D, Donlic A, Kim H, Kenney D, Castello-Serrano I, Suzuki S, Tamura T et al.. (2021) SARS-CoV-2 requires cholesterol for viral entry and pathological syncytia formation.. Elife, 10 (3): (589-97). [PMID:33890572]
5. Budworth J, Gescher A. (1995) Differential inhibition of cytosolic and membrane-derived protein kinase C activity by staurosporine and other kinase inhibitors.. FEBS Lett, 362 (2): (139-42). [PMID:7536688]
6. McKenzie BA et al.. (2020) Activation of the executioner caspases-3 and -7 promotes microglial pyroptosis in models of multiple sclerosis.. J Neuroinflammation, 17 (253). [PMID:32861242]
7. Lotsberg ML et al.. (2020) AXL Targeting Abrogates Autophagic Flux and Induces Immunogenic Cell Death in Drug-Resistant Cancer Cells.. J Thorac Oncol, 15 (6): (973-999). [PMID:32018052]
8. Wu N et al.. (2021) Berberine ameliorates neuronal AD-like change via activating Pi3k/PGCε pathway.. Biofactors, 47 (4): (587-599). [PMID:33740285]
9. Hofmann L et al.. (2018) Characterization of small fiber pathology in a mouse model of Fabry disease.. Elife, 7 [PMID:30328411]
10. Tomasek T et al.. (2021) Cell-free hemoglobin-mediated human lung microvascular endothelial barrier dysfunction is not mediated by cell death.. Biochem Biophys Res Commun, 556 (199-206). [PMID:33848934]
11. Pacitto R et al.. (2017) CXCL12-induced macropinocytosis modulates two distinct pathways to activate mTORC1 in macrophages.. J Leukoc Biol, 101 (3): (683-692). [PMID:28250113]
12. Toth K et al.. (2019) Encoding the ß-Arrestin Trafficking Fate of Ghrelin Receptor GHSR1a: C-Tail-Independent Molecular Determinants in GPCRs.. ACS Pharmacol Transl Sci, 2 (4): (230-246). [PMID:32259059]
13. Bhattacharyya M et al.. (2020) Flexible linkers in CaMKII control the balance between activating and inhibitory autophosphorylation.. Elife, 9 [PMID:32149607]
14. Le TM et al.. (2021) Ex vivo Induction of Apoptotic Mesenchymal Stem Cell by High Hydrostatic Pressure.. Stem Cell Rev Rep, 17 (2): (662-672). [PMID:33128169]
15. Bukong TN et al.. (2014) Exosomes from hepatitis C infected patients transmit HCV infection and contain replication competent viral RNA in complex with Ago2-miR122-HSP90.. PLoS Pathog, 10 (10): (e1004424). [PMID:25275643]
16. Qian L et al.. (2016) Grb7 and Hax1 may colocalize partially to mitochondria in EGF-treated SKBR3 cells and their interaction can affect Caspase3 cleavage of Hax1.. J Mol Recognit, 29 (7): (318-33). [PMID:26869103]
17. Le TM et al.. (2020) Hydrostatic pressure can induce apoptosis of the skin.. Sci Rep, 10 (17594). [PMID:33077833]
18. Avril M et al.. (2019) Interplay of Plasmodium falciparum and thrombin in brain endothelial barrier disruption.. Sci Rep, 9 (13142). [PMID:31511575]
19. Park YH et al.. (2016) Involvement of AMPA Receptor and Its Flip and Flop Isoforms in Retinal Ganglion Cell Death Following Oxygen/Glucose Deprivation.. Invest Ophthalmol Vis Sci, 57 (2): (508-26). [PMID:26868754]
20. Magerus-Chatinet A & Rieux-Laucat F. (2017) In Vitro Evaluation of the Apoptosis Function in Human Activated T Cells.. Methods Mol Biol, 1557 (33-40). [PMID:28078580]
21. Nicholls SB et al.. (2011) Mechanism of a genetically encoded dark-to-bright reporter for caspase activity.. J Biol Chem, 286 (28): (24977-86). [PMID:21558267]
22. Hansel CS et al.. (2019) Nanoneedle-Mediated Stimulation of Cell Mechanotransduction Machinery.. ACS Nano, 13 (3): (2913-2926). [PMID:30829469]
23. Anderson CJ et al.. (2021) Microbes exploit death-induced nutrient release by gut epithelial cells.. Nature, 596 (7871): (262-267). [PMID:34349263]
24. Vasilevich AS et al.. (2020) On the correlation between material-induced cell shape and phenotypical response of human mesenchymal stem cells.. Sci Rep, 10 (18988). [PMID:33149200]
25. Le Vasseur M et al.. (2019) Pannexin 2 Localizes at ER-Mitochondria Contact Sites.. Cancers (Basel), 11 (3): [PMID:30862038]
26. Jabbari K et al.. (2021) Protein Ligands in the Secretome of CD36+ Fibroblasts Induce Growth Suppression in a Subset of Breast Cancer Cell Lines.. Cancers (Basel), 13 (18): [PMID:34572749]
27. Yadikar H et al.. (2020) Screening of tau protein kinase inhibitors in a tauopathy-relevant cell-based model of tau hyperphosphorylation and oligomerization.. PLoS One, 15 (7): (e0224952). [PMID:32692785]
28. Langsfeld ES et al.. (2015) The Deacetylase Sirtuin 1 Regulates Human Papillomavirus Replication by Modulating Histone Acetylation and Recruitment of DNA Damage Factors NBS1 and Rad51 to Viral Genomes.. PLoS Pathog, 11 (9): (e1005181). [PMID:26405826]

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