JP-11646

JP-11646 is a pan-PIM inhibitor with increased potency against PIM2 (IC50 = 0.5 nM) . JP11646 is freely reversible and ATP non-competitive. JP-11646 results in a decrease of PIM1, 2, and 3 mRNA. JP-11646 can effectively inhibit cell viability in small cell lung cancer (SCLC) and large cell neuroendocrine carcinomas of the lung (LCNEC) . JP-11646 can cause a decrease in p-4EBP-1 protein, increasing the cleavage of caspases while decreasing caspase-3. JP-11646 induces apoptosis or necroptosis in cells. JP-11646 leads to reductions in MYC paralogs. JP-11646 can be used for the study of SCLC, LCNEC, human acute leukemia (AML), multiple myeloma (MM), and triple-negative breast cancer (TNBC) [1][2][3][4][5].

Product Specifications

CAS Number

[1902983-63-4]

UNSPSC

12352100

Target

Apoptosis; Caspase; Necroptosis; NF-κB; PARP; Pim

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics; JAK/STAT Signaling; NF-κB

Field of Research

Cancer

Smiles

O=C1NC(/C(S1)=C/C2=CC=NC(N[C@H]3CC[C@@H](CC3)NCC4=CC=CC5=C4C=CC=C5)=N2)=O

Molecular Formula

C25H25N5O2S

Molecular Weight

459.56

References & Citations

[1]Minton K, et al. P3. 02G. 04 JP11646-mediated PIM2 Inhibition Has Potent Antitumor Effects in Small Cell Lung Cancer and Large Cell Neuroendocrine Carcinoma of the Lung[J]. Journal of Thoracic Oncology, 2024, 19 (10) : S305-S306.|[2]Krista E. et al. Translational pharmacology approaches to explore the novel mechanism of a pan-PIM kinase inhibitor, JP-11646, in acute myeloid leukemia. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA) : AACR; Cancer Res 2015;75 (15 Suppl) :Abstract nr 681.|[3]Katsuta E, et al. Targeting PIM2 by JP11646 results in significant antitumor effects in solid tumors[J]. International journal of oncology, 2022, 61 (4) : 114.|[4]Nair JR, et al. Novel inhibition of PIM2 kinase has significant anti-tumor efficacy in multiple myeloma. Leukemia. 2017 Aug;31 (8) :1715-1726.|[5]Mehta R, et al. Preclinical efficacy of the novel PIM2 kinase inhibitor, JP11646 in triple negative breast cancer models [abstract]. In: Proceedings of the 2016 San Antonio Breast Cancer Symposium; 2016 Dec 6-10; San Antonio, TX. Philadelphia (PA) : AACR; Cancer Res 2017;77 (4 Suppl) :Abstract nr P6-11-10.