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.

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.

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.

Pictilisib (GDC-0941) (GDC-0941) is a potent pan inhibitor of class I catalytic subunits of PI3K (IC50s: 3 33 3 75 nM for p110α β δ γ).

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

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.

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).

PI-3065 is a novel potent and selective PI3K p110δ inhibitor.

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).

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.

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).

URAT1&XO Inhibitor 3 (compound 27) is an orally effective anti-gout agent targeting XO (IC50: 35 nM) and URAT1 (IC50: 31 nM). This compound exhibits favorable pharmacological and pharmacokinetic (PK) characteristics, as well as in vivo safety.

Imarikiren (also known as TAK-272) is a potent, highly selective, orally bioavailable direct renin inhibitor primarily used for treating diabetic nephropathy. In hPRA assays, TAK-272 exhibits strong inhibitory activity against human renin (IC50 = 2.1 nM) and demonstrates excellent selectivity over other aspartic proteases such as pepsin (IC50 > 10 μM) and cathepsin D (IC50 > 10 μM). In rats, TAK-272 shows significantly improved pharmacokinetic properties (F = 25.2%) and, upon oral administration (3 and 10 mg kg), exhibits a dose-dependent, potent, and sustained antihypertensive effect. Currently, TAK-272 HCl is undergoing human clinical trials.

Pilaralisib analogue (XL147 analogue) is a selective and reversible class I PI3K inhibitor targeting PI3Kα δ γ.

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

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

PIK-93, the first potent synthetic PI4K inhibitor, exhibits an IC50 of 19 nM and also inhibits PI3Kα with an IC50 of 39 nM.

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

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