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MedKoo Cat#: 555348 | Name: HS-1371
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Description:

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

HS-1371 is a novel kinase inhibitor of RIP3-mediated necroptosis. HS-1371 directly binds to RIP3 in an ATP-competitive and time-independent manner, providing a mechanism of action. Moreover, the compound inhibited TNF-induced necroptosis but did not inhibit TNF-induced apoptosis, indicating that this novel inhibitor has a specific inhibitory effect on RIP3-mediated necroptosis via the suppression of RIP3 kinase activity. HS-1371 could serve as a potential preventive or therapeutic agent for diseases involving RIP3 hyperactivation.

Chemical Structure

HS-1371
HS-1371
CAS#2158197-70-5

Theoretical Analysis

MedKoo Cat#: 555348

Name: HS-1371

CAS#: 2158197-70-5

Chemical Formula: C24H24N4O

Exact Mass: 384.1950

Molecular Weight: 384.48

Elemental Analysis: C, 74.97; H, 6.29; N, 14.57; O, 4.16

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 Ready to Ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,350.00 Ready to ship
500mg USD 2,950.00 Ready to ship
1g USD 4,650.00 2 Weeks
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Related CAS #
No Data
Synonym
HS-1371; HS 1371; HS1371;
IUPAC/Chemical Name
7-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)-4-(p-tolyloxy)quinoline
InChi Key
VPVLPCIBKVWFDT-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H24N4O/c1-17-2-5-21(6-3-17)29-24-10-13-26-23-14-18(4-7-22(23)24)19-15-27-28(16-19)20-8-11-25-12-9-20/h2-7,10,13-16,20,25H,8-9,11-12H2,1H3
SMILES Code
CC1=CC=C(OC2=CC=NC3=CC(C4=CN(C5CCNCC5)N=C4)=CC=C23)C=C1
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
>3 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
Necroptosis is a type of programmed cell death that usually occurs under apoptosis-deficient conditions. Receptor-interacting protein kinase-3 (RIP3, or RIPK3) is a central player in necroptosis, and its kinase activity is essential for downstream necroptotic signaling events. Since RIP3 kinase activity has been associated with various diseases, the development of specific RIP3 inhibitors is an attractive strategy for therapeutic application.
Biological target:
HS-1371 is a potent and ATP-competitive receptor-interacting protein kinase 3 (RIP3) inhibitor with an IC50 of 20.8 nM.
In vitro activity:
Only HS-1371 rescued TSZ-induced cell death, similar to DAB, and the reduced cytotoxicity was consistent with western blot data showing that HS-1371 effectively blocked RIP3 kinase activity (Fig. 3a). The effect of HS-1371 on TNF-induced cell death was similar to other necroptosis inhibitors, Nec-1, DAB, and NSA (Fig. 3b, left panel). Reference: Exp Mol Med. 2018 Sep 20;50(9):1-15. https://pubmed.ncbi.nlm.nih.gov/30237400/
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMF 30.0 78.03
DMF:PBS (pH 7.2) (1:4) 0.2 0.52
DMSO 11.6 30.06
Ethanol 4.5 11.70
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 384.48 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
Formulation protocol:
1. Park HH, Park SY, Mah S, Park JH, Hong SS, Hong S, Kim YS. HS-1371, a novel kinase inhibitor of RIP3-mediated necroptosis. Exp Mol Med. 2018 Sep 20;50(9):1-15. doi: 10.1038/s12276-018-0152-8. PMID: 30237400; PMCID: PMC6148246.
In vitro protocol:
1. Park HH, Park SY, Mah S, Park JH, Hong SS, Hong S, Kim YS. HS-1371, a novel kinase inhibitor of RIP3-mediated necroptosis. Exp Mol Med. 2018 Sep 20;50(9):1-15. doi: 10.1038/s12276-018-0152-8. PMID: 30237400; PMCID: PMC6148246.
In vivo protocol:
TBD
Park HH, Park SY, Mah S, Park JH, Hong SS, Hong S, Kim YS. HS-1371, a novel kinase inhibitor of RIP3-mediated necroptosis. Exp Mol Med. 2018 Sep 20;50(9):1-15. doi: 10.1038/s12276-018-0152-8. PMID: 30237400; PMCID: PMC6148246.