MedKoo Cat#: 407908 | Name: SRPKIN-1

Description:

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

SRPKIN-1 is a Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenic Isoform. SRPKIN-1 is also the first kinase inhibitor that forms a covalent bond with a tyrosine phenol group in the ATP-binding pocket. Kinome-wide profiling demonstrates its selectivity for SRPK1/2, and SRPKIN-1 attenuates SR protein phosphorylation at submicromolar concentrations.

Chemical Structure

SRPKIN-1
CAS#2089226-94-6

Theoretical Analysis

MedKoo Cat#: 407908

Name: SRPKIN-1

CAS#: 2089226-94-6

Chemical Formula: C27H21FN2O3S

Exact Mass: 472.1257

Molecular Weight: 472.53

Elemental Analysis: C, 68.63; H, 4.48; F, 4.02; N, 5.93; O, 10.16; S, 6.78

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
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Synonym
SRPKIN-1; SRPKIN1; SRPKIN 1.
IUPAC/Chemical Name
3-(3-Cyano-9-ethyl-6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazol-8-yl)benzenesulfonyl fluoride
InChi Key
TWKWEBMGDALHPN-UHFFFAOYSA-N
InChi Code
InChI=1S/C27H21FN2O3S/c1-4-16-12-21-22(13-20(16)17-6-5-7-18(11-17)34(28,32)33)27(2,3)26-24(25(21)31)19-9-8-15(14-29)10-23(19)30-26/h5-13,30H,4H2,1-3H3
SMILES Code
O=S(C1=CC=CC(C2=C(CC)C=C3C(C(C)(C)C(NC4=C5C=CC(C#N)=C4)=C5C3=O)=C2)=C1)(F)=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
Soluble in DMSO
Shelf Life
>2 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
Vascular endothelial growth factor (VEGF) is a known target for SRPK-regulated splicing and, relative to the first-generation SRPK inhibitor SRPIN340 or small interfering RNA-mediated SRPK knockdown, SRPKIN-1 is more potent in converting the pro-angiogenic VEGF-A165a to the anti-angiogenic VEGF-A165b isoform and in blocking laser-induced neovascularization in a murine retinal model. These findings encourage further development of SRPK inhibitors for treatment of age-related macular degeneration.

Preparing Stock Solutions

The following data is based on the product molecular weight 472.53 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
1: Hatcher JM, Wu G, Zeng C, Zhu J, Meng F, Patel S, Wang W, Ficarro SB, Leggett AL, Powell CE, Marto JA, Zhang K, Ki Ngo JC, Fu XD, Zhang T, Gray NS. SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenic Isoform. Cell Chem Biol. 2018 Apr 19;25(4):460-470.e6. doi: 10.1016/j.chembiol.2018.01.013. Epub 2018 Feb 22. PubMed PMID: 29478907.