HIPK2 Inhibitors
HIPK2, or Homeodomain-Interacting Protein Kinase 2, is a multifaceted protein kinase known for its pivotal role in cellular homeostasis, DNA damage response, and transcriptional regulation. As a nuclear kinase, HIPK2 is intricately involved in various signaling pathways, including p53, Wnt, and TGF-β, exerting its effects through phosphorylation of key substrates and interaction with diverse transcriptional regulators. Within the intricate network of cellular processes, HIPK2 plays a crucial role in modulating gene expression, apoptosis, and DNA repair. Its ability to phosphorylate and regulate the stability of transcription factors, such as p53, provides a direct link between HIPK2 and fundamental cellular responses to stress and damage. Additionally, HIPK2's involvement in Wnt and TGF-β pathways highlights its regulatory impact on cell fate determination and tissue development.
Inhibition of HIPK2 represents a complex interplay within the cellular signaling network. Numerous chemical inhibitors, acting either directly on HIPK2 or indirectly through modulation of upstream or parallel pathways, offer insights into strategies for controlling HIPK2 activity. For instance, compounds like SB203580 and SP600125 exert their inhibitory effects on HIPK2 indirectly by targeting upstream kinases, such as p38 MAP kinase and JNK, disrupting the signaling cascades that converge on HIPK2. Furthermore, compounds like U0126 and Ruxolitinib intervene in pathways associated with HIPK2, exemplifying the interconnected nature of cellular signaling. The intricate dance of chemical inhibitors, influencing diverse pathways and molecular players, showcases the challenge and opportunity in precisely modulating HIPK2 function. Understanding these inhibitors' specific mechanisms provides a foundation for unraveling the nuanced regulatory roles of HIPK2 within the intricate tapestry of cellular signaling networks.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
SB 203580 | 152121-47-6 | sc-3533 sc-3533A | 1 mg 5 mg | $90.00 $349.00 | 284 | |
Pyridinyl imidazole compound. Selective inhibitor of p38 MAP kinase, a pathway upstream of HIPK2. Inhibition of p38 MAP kinase disrupts the downstream signaling, indirectly modulating HIPK2 function. | ||||||
SP600125 | 129-56-6 | sc-200635 sc-200635A | 10 mg 50 mg | $40.00 $150.00 | 257 | |
Anthrapyrazolone compound. Inhibitor of c-Jun N-terminal kinase (JNK), a kinase involved in various cellular processes. By blocking JNK activity, SP600125 indirectly affects HIPK2, as JNK can regulate HIPK2 expression and activity in specific cellular contexts. | ||||||
Tyrphostin B42 | 133550-30-8 | sc-3556 | 5 mg | $26.00 | 4 | |
Tyrosine kinase inhibitor. Blocks JAK2, upstream of the JAK/STAT pathway, which regulates HIPK2 expression. Inhibition of JAK2 alters the downstream signaling cascade, indirectly influencing HIPK2 levels and activity. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $123.00 $400.00 | 148 | |
Synthetic quercetin analog. Inhibitor of phosphatidylinositol 3-kinase (PI3K), a pathway interconnected with HIPK2 signaling. Modulating PI3K activity indirectly affects HIPK2 function by disrupting the crosstalk between these pathways. | ||||||
Wortmannin | 19545-26-7 | sc-3505 sc-3505A sc-3505B | 1 mg 5 mg 20 mg | $67.00 $223.00 $425.00 | 97 | |
Fungal metabolite. Irreversible PI3K inhibitor. Blocks the PI3K/Akt pathway, which cross-talks with HIPK2 signaling. Indirectly influences HIPK2 function by disrupting the balance between pro-survival and pro-apoptotic signals within the cell. | ||||||
SP2509 | 1423715-09-6 | sc-492604 | 5 mg | $284.00 | ||
Quinoline compound. Inhibitor of histone methyltransferase G9a, involved in epigenetic regulation. G9a inhibition can alter the epigenetic landscape, indirectly influencing HIPK2 expression and chromatin accessibility, impacting its transcriptional regulation. | ||||||
KU 60019 | 925701-46-8 | sc-363284 sc-363284A | 10 mg 50 mg | $248.00 $1035.00 | 1 | |
Highly selective inhibitor of ataxia telangiectasia mutated (ATM) kinase. ATM is involved in DNA damage response pathways, and its inhibition indirectly affects HIPK2, as both proteins participate in cellular processes related to DNA damage and repair. | ||||||
GDC-0879 | 905281-76-7 | sc-364497 | 5 mg | $225.00 | ||
Inhibitor of RAF kinase, part of the RAS/RAF/MEK/ERK pathway. By blocking RAF kinase, GDC-0879 disrupts the downstream signaling cascade, indirectly modulating HIPK2 expression and activity in cellular contexts where these pathways intersect. | ||||||
BX 795 | 702675-74-9 | sc-281689 sc-281689A sc-281689C sc-281689B sc-281689D sc-281689E | 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg | $219.00 $273.00 $331.00 $495.00 $882.00 $1489.00 | 5 | |
Thienopyrimidine compound. Inhibitor of TBK1/IKKε kinases, associated with the NF-κB pathway. By blocking TBK1/IKKε, BX-795 influences the NF-κB pathway, which cross-talks with HIPK2 signaling, indirectly affecting HIPK2 expression and activity. | ||||||
JIB 04 | 199596-05-9 | sc-397040 | 20 mg | $177.00 | ||
Thiazole derivative. Inhibitor of Jumonji histone demethylases (JHDMs). JIB-04 indirectly modulates HIPK2 expression by altering the histone methylation status, impacting the epigenetic regulation of the gene encoding HIPK2 in specific cellular contexts. | ||||||