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SRPK inhibitor

Product Name
SRPK inhibitor
CAS No.
218156-96-8
Chemical Name
SRPK inhibitor
Synonyms
CS-910;SRPIN340;SRPIN 340;SRPIN-340;SRPK inhibitor;SRPIN340, >=98%;SRPIN340 >=98% (HPLC);SRPIN340, 10 mM in DMSO;SRPK Inhibitor(SRPIN340);SRPIN340 (SRPK inhibitor)
CBNumber
CB22668305
Molecular Formula
C18H18F3N3O
Formula Weight
349.35
MOL File
218156-96-8.mol
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SRPK inhibitor Property

Boiling point:
395.9±42.0 °C(Predicted)
Density 
1.306±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMSO: soluble20mg/mL, clear
form 
powder
pka
11.09±0.70(Predicted)
color 
white to beige
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
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Safety

Hazard Codes 
Xn
Risk Statements 
22
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1088
Product name
SRPIN340
Purity
≥98% (HPLC)
Packaging
5mg
Price
$121
Updated
2025/07/31
Sigma-Aldrich
Product number
SML1088
Product name
SRPIN340
Purity
≥98% (HPLC)
Packaging
25mg
Price
$489
Updated
2025/07/31
Sigma-Aldrich
Product number
5.04293
Product name
SRPK Inhibitor, SRPIN340 - CAS 281856-96-8 - Calbiochem
Packaging
10mg
Price
$204
Updated
2023/01/07
Cayman Chemical
Product number
16284
Product name
SRPIN340
Purity
≥95%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
16284
Product name
SRPIN340
Purity
≥95%
Packaging
5mg
Price
$86
Updated
2024/03/01
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SRPK inhibitor Chemical Properties,Usage,Production

Description

Serine/arginine-rich protein kinase 1 (SRPK1) targets proteins that contain multiple serine/arginine (SR) dipeptides, including SR-rich splicing factor 1, SRSF1. SRPIN340 is an isonicotinamide compound that inhibits SRPK1 (Ki = 0.89 μM). It is about 10-fold less effective against SRPK2 and does not inhibit the related SRPKs, Clk1 and Clk4. SRPIN340 suppresses the propagation of Sindbis virus in Vero cells and the replication of hepatitis C virus in Huh7/Rep-Feo-2a cells. By blocking SRPK1-mediated phosphorylation of SRSF1, SRPIN340 modulates alternative splicing of VEGF, reducing neovascularization both in cells and in animals.

Uses

SRPIN340 is a SRPK1 kinase inhibitor, which shows potential novel targeted therapeutic strategy in prostate cancer.

Synthesis

1496-40-8

39178-35-3

218156-96-8

The general procedure for the synthesis of N-(2-(1-piperidinyl)-5-(trifluoromethyl)phenyl)isonicotinamide from 2-piperidin-1-yl-5-(trifluoromethyl)aniline and isocyanidinium chloride is as follows: isonicotinic acid chloride hydrochloride (6.48 g, 36.4 mmol, commercially available) and triethylamine (5.57 ml, 54.6 mmol) are sequentially added at 0°C to the 2-(1-piperidinyl)-5-(trifluoromethyl)aniline (4.45 g, 18.2 mmol, prepared as described in Reference Examples 1-2B) to a solution of methylene chloride (10 ml). The reaction mixture was stirred for 30 minutes. Subsequently, water was added to the mixture and extracted three times with ethyl acetate. The organic layers were combined, washed with saturated sodium chloride solution, dried over anhydrous sodium sulfate, filtered and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (200 g silica gel, eluent ratio hexane/ethyl acetate = 1/1) and recrystallized. The final N-[2-(1-piperidinyl)-5-(trifluoromethyl)phenyl]isonicotinamide (SRPIN-1, GIF-0340) (5.49 g, 86.3% yield) was obtained as a colorless solid.

References

[1] TAKESHI FUKUHARA. Utilization of host SR protein kinases and RNA-splicing machinery during viral replication.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2006: 11329-11333. DOI:10.1073/pnas.0604616103
[2] MELISSA V R GAMMONS. SRPK1 inhibition modulates VEGF splicing to reduce pathological neovascularization in a rat model of retinopathy of prematurity.[J]. ACS Applied Materials & Interfaces, 2013: 5797-5806. DOI:10.1167/iovs.13-11634
[3] M V GAMMONS. Targeting SRPK1 to control VEGF-mediated tumour angiogenesis in metastatic melanoma[J]. British Journal of Cancer, 2014, 111 3: 477-485. DOI:10.1038/bjc.2014.342

SRPK inhibitor Preparation Products And Raw materials

Raw materials

Preparation Products

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SRPK inhibitor Suppliers

MedChemexpress LLC
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021-58955995
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sales@cckinase.com
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View Lastest Price from SRPK inhibitor manufacturers

Career Henan Chemical Co
Product
SRPK inhibitor 218156-96-8
Price
US $1.00/KG
Min. Order
1KG
Purity
98%
Supply Ability
20kg
Release date
2019-09-05

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