pk 3

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

DNA-PK-IN-3 is a highly potent inhibitor of DNA-PK that exerts a synergistic effect with radiotherapy and chemotherapy, enhancing therapeutic outcomes and significantly inhibiting tumor growth. Additionally, it demonstrates remarkable efficacy in reducing damage to normal cells, thereby minimizing adverse side effects, making it a compound of great potential for cancer research applications[1].

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.

LY-294002 hydrochloride (NSC 697286) is a synthetic molecule inhibitor of PI3Kα δ β (IC50: 0.5 0.57 0.97 μM, in cell-free assays); more stable than Wortmannin in solution, and also is a blocker of autophagosome formation.

PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).

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.

PK11000 is a p53 targeting compound, has anti-tumor activities through activation of unstable p53.

Wortmannin (SL-2052) is a PI3K inhibitor (IC50=3 nM) that is covalent and irreversible. Wortmannin is also an inhibitor of PlK1 and PlK3 (IC50=5.8 48 nM) that blocks autophagy.

KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 values of 8.6 nM, 4 nM, 0.5 nM, and 0.1 nM respectively, and demonstrates less inhibition of PI3Kγ with an IC50 of 0.59 μM.

Samotolisib (LY3023414) is an oral ATP competitive inhibitor of the class I PI3K isoforms, DNA-PK, and mTOR. Samotolisib (LY3023414) has been used in trials studying the treatment of Neoplasm, Solid Tumor, COLON CANCER, BREAST CANCER, and Advanced Cancer, among others.

Pictilisib dimethanesulfonate (GDC-0941 2 MeSO3H salt) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

SF2523 is a highly selective and potent inhibitor (SF2523) with improved physicochemical properties, excellent aqueous solubility, and biological efficacy. It is typically used in genome editing [CRISPR Cas Solution] technology and can effectively enhance the efficiency of this process.

ETP-45658 (ETP45658) is a PI 3-kinase inhibitor (IC50 values are 22, 30, 129 and 710 nM for PI 3-Kα, PI 3-Kδ, PI 3-Kβ and PI 3-Kγ respectively). Also inhibits DNA-PK and mTOR (IC50 values are 70.6 and 152 nM respectively).

PP487 is a dual tyrosine kinase PI(3)K inhibitor, exhibiting IC50 values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. It is applicable in cancer research [1].

IDO1-IN-22 (Compound 3) is an inhibitor of IDO1 with potent activity, showing a biochemical hIDO1 IC50 of 67.4 nM and HeLa hIDO1 IC50 of 17.6 nM. It demonstrates excellent antitumor efficacy in an LLC xenograft model and has a desirable pharmacokinetic (PK) profile [1].

PIK-90, a DNA-PK and PI3K inhibitor, suppresses p110α( IC50=11 nM), p110γ(IC50=18 nM) and DNA-PK(IC50=13 nM) .

ATR-IN-20, a potent ATM/ATR inhibitor, showcases an IC50 value of 3 nM. It also exhibits inhibitory activity against mTOR with an IC50 of 18 nM, while maintaining selectivity over PI3Kα (100 nM), ATM (100 nM), and DNA-PK (662 nM). Additionally, ATR-IN-20 has an excellent pharmacokinetic profile with an oral bioavailability (F) of 30%, and demonstrates anticancer effects.

GR 94800 TFA is a potent, selective antagonist of the NK 2 receptor peptide, demonstrating pK B values of 9.6 for NK 2, 6.4 for NK 1, and 6.0 for NK 3 receptors, respectively [1] [2].

QLT0267 is an inhibitor targeting integrin-linked kinase (ILK; IC50= 26 nM), showing over 10-fold selectivity against cyclin-dependent kinases 1, 2, and 5 (Cdk1, Cdk2, and Cdk5), and over 1,000-fold selectivity against C-terminal Src kinase (CSK), DNA-PK, Pim-1, Akt, PKC, and casein kinase 2 (CK2) at a concentration of 10 mg/ml. This compound effectively inhibits the proliferation of NPA187 papillary thyroid cancer cells with an IC50 of approximately 3 µM and induces apoptosis in NPA187, DRO, and K4 cancer cell lines. In vivo studies reveal that QLT0267, administered at 100 mg/kg, significantly reduces tumor growth in a DRO mouse xenograft model and diminishes both tumor volume and intratumoral vascularization in a U87MG glioblastoma mouse xenograft model, showcasing its potential for therapeutic applications in cancer treatment.

PF-06455943, a leucine rich repeat kinase 2 (LRRK2) inhibitor, exhibits an inhibition concentration (IC50) value of 3 nM and also functions as a PET radioligand. It is utilized in the research of ADME/neuro PK characterization and Parkinson's disease (PD).

MF-592 is a potent and selective antagonists of the EP4 receptor. MF-592 demonstrated good functional potency (hEP4 IC50 = 3 nM) and potent inhibition of PGE2 modulated TNFa release in LPS stimulated human whole blood (hWB) (IC50 = 78nM). In addition, it showed an excellent oral pharmacokinetic (PK) profile and in vivo efficacy in a rat chronic adjuvant-induced-arthritis model (ED50 = 0.1 mg/kg/day).. MF-592 has a desirable overall preclinical profile that suggests it is suitable for further development.

Canfosfamide (TLK-286, TER286), a glutathione analogue prodrug, becomes activated by glutathione S-transferase P1-1 to induce apoptosis and inhibit DNA-dependent protein kinase's (DNA-PK) catalytic kinase activity. Upon activation, it generates an anticancer alkylating agent and a glutathione derivative, making it useful in researching malignancies [1] [2] [3].

Pasireotide diaspartate (SOM230), a long-acting cyclohexapeptide and somatostatin analog, enhances agonist activity across somatostatin receptor subtypes (sst1/2/3/4/5, with pK i values of 8.2, 9.0, 9.1, <7.0, and 9.9, respectively). This compound demonstrates antisecretory, antiproliferative, and proapoptotic activities [1] [2].

GSK172981 is a non-peptide tachykinin NK3 receptor antagonist with a high affinity for the recombinant human (PK (I) value 7.7) and native guinea pig (PK (I) value 7.8) tachykinin NK3 receptor. In vitro, the functional evaluation showed that GSK172981 was

PK-THPP is a channel blocker of TASK-3.

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.

PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of PI3K family members (IC50s: 2/3/3/15/30/23 nM for p110α/β/δ/γ, mTOR, and DNA-PK).

GR 83074 is a potent and selective antagonist of the NK-2 (Neurokinin Receptor) with a 340-fold selectivity over NK-1 and a pK_B value of 8.23. It does not act as an antagonist for NK-3, affirming its specificity [1].

Tuberculosis inhibitor 3 (compound 2i) exhibits potent anti-TB properties (MIC < 0.016 μg mL) against both drug-sensitive and resistant MTB strains, with acceptable pharmacokinetic profiles and oral bioavailability[1].

PIK-75 hydrochloride (PIK-75 HCl) is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM in cell-free assays.

Sp-5,6-DCl-cBIMPS is a potent and specific activator of cAMP-dependent protein kinases (cAMP-PK) that enhances insulin release and inhibits U46619-induced activation of Rho, Gq, and G12 G13 in platelets.

ATM Inhibitor-1 is a highly potent, selective, and orally active ATM inhibitor (IC50: 0.7 nM) with anti-tumor activity. It exhibits weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM), and PI3Kδ (IC50, 0.73 μM).

GSK256471 is a potent selective NK(3) antagonist that shows a high affinity for recombinant human (PK (I) value 8.9) and native guinea pig (PK (I) value 8.4) tachykinin NK(3) receptors. In vitro functional assessment showed that GSK256471 reduced the E(Ma

PI-103 Hydrochloride is a potent dual inhibitor of PI3K and mTOR, demonstrating inhibitory IC50 values of 8 nM for p110α, 88 nM for p110β, 48 nM for p110δ, 150 nM for p110γ, 20 nM for mTORC1, and 83 nM for mTORC2, respectively. Additionally, it inhibits DNA-PK with an IC50 of 2 nM and induces autophagy [1] [2] [3] [4].