pk-3

PK-3 is a cancer cell growth inhibitor. It also has microtubule-binding activity.

CLK1/2-IN-3 (Cpd-3) is a potent and selective CLK1 and CLK2 inhibitor with antiproliferative activity and inhibits the activities of CLK1, CLK2, SRPK1, SRPK2, and SRPK3.CLK1/2-IN-3 induces nuclear speckle enlargement, which induces S6K pre-mRNA-selective splicing and subsequent inhibition of cell growth of multiple cancer cell types. cancer cell types cell growth.

TC-DAPK 6 is an ATP-competitive inhibitor of Death-associated protein kinase (DAPK) with IC50s of 69 and 225 nM for DAPK1 and DAPK3.

RIPK3-IN-5 (compound 32) is a potent RIPK3 inhibitor with an IC50 of 27 nM. Additionally, it inhibits necroptosis with an EC50 of 0.45 μM.

RIPK3-IN-6 (compound 1) is a type I RIPK3 inhibitor with low selectivity within the RIPK family, particularly in relation to RIPK2 activity.

Ro3280 (Ro5203280) is an effective, specific inhibitor of PLK1(IC50=3, Kd=0.09 nM).

TBB (NSC-231634)(NSC-231634) is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2).

SM1-71 is a potent multi-targeted acrylamide-modified TAK1 inhibitor that inhibits MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2.SM1-71 can be used as a kinase probe with anticancer activity and inhibits the proliferation of various cancer cell lines.

RIPK3-IN-2, a RIP3 inhibitor, is utilized in studies of diseases caused by or associated with activated necrotic pathways.

GSK-690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.

RIPK3-IN-1 is a selective and potent RIPK3 inhibitor (IC50: 9.1 nM) that inhibits the activities of c-Met kinase, RIPK1 and RIPK2.RIPK3-IN-1 has potential tumorigenic activity and can be used to study apoptosis.

SZM-1209 is a potent and specific RIPK1 inhibitor with oral activity, displaying a dissociation constant (Kd) of 85 nM. It demonstrates substantial anti-necroptotic efficacy with an EC50 of 22.4 ± 8.1 nM and possesses therapeutic effects against systemic inflammatory response syndrome (SIRS) and acute lung injury (ALI) [1].

SZM679 is an orally active, selective RIPK1 inhibitor displaying potent affinity with a dissociation constant (Kd) of 8.6 nM for RIPK1, while exhibiting minimal activity towards RIPK3, with a Kd of >5000 nM. It effectively counteracts tumor necrosis factor-induced systemic inflammation, reduces Tau hyperphosphorylation, diminishes neuroinflammation, and lowers RIPK1 phosphorylation in the hippocampus and cortex. SZM679 is utilized in Alzheimer's disease (AD) research [1].

DMAT (Casein kinase II Inhibitor) is a potent and specific inhibitor of CK2(IC50 value of 130 nM).

HS148 is a selective inhibitor of DAPK3 (death-associated protein kinase 3), with a Ki value of 119 nM. Inhibition of DAPK3 by HS148 has been shown to reduce the progression of gastric cancer by activating the ULK1-dependent pathway, which is implicated in cellular autophagy and tumor suppression mechanisms.

HS94 (DAPK3 inhibitor HS94) is a selective and potent DAPK3 inhibitor with a Ki value of 126 nM for Pim kinase inhibition and can be used to study hypertension.

RIPK3-IN-3 (compound 20) is a selective RIPK3 inhibitor with a potent IC50 value of 10 nM, effectively blocking RIPK3-mediated phosphorylation of MLKL, preventing oligomerization and necroptosis induction. Moreover, RIPK3-IN-3 suppresses CXCL5 secretion and impedes AsPC-1 cell migration and invasion [1].

RIPK3-IN-4 (Compound 42) is a RIPK3 inhibitor that mitigates necroptosis, inflammatory responses, and HK-2 cell damage. It alleviates acute kidney injury by attenuating Cisplatin- and I/R-induced kidney damage, along with associated inflammatory responses and necroptosis [1].

UH15-38 is a potent and selective RIPK3 inhibitor that blocks necroptosis in alveolar epithelial cells triggered by IAV, useful for studying lung inflammation.

LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5/0.57/0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC50=1.4 μM) and an inhibitor of CK2 (IC50=98 nM). LY294002 activates apoptosis and autophagy.

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6/15/2/3/3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.

AZD-7648 is an inhibitor of DNA-dependent protein kinase (DNA-PK) with the IC50 of 0.63 nM in an enzyme assay,has anti-tumor activity.

STL127705 (Compound L) is a potent inhibitor of the Ku 70/80 heterodimer protein, disrupting Ku70/80-DNA interaction with an IC50 of 3.5 μM, and inhibiting Ku-dependent DNA-PKCS kinase activation with an IC50 of 2.5 μM.