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PI3K

Phosphoinositide 3-kinases (PI3Ks), also called phosphatidylinositol 3-kinases, are a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer.PI3Ks are a family of related intracellular signal transducer enzymes capable of phosphorylating the 3 position hydroxyl group of the inositol ring of phosphatidylinositol (PtdIns). The pathway, with oncogene PIK3CA and tumor suppressor PTEN, is implicated in the sensitivity of cancer tumors to insulin and IGF1, and in calorie restriction.

Inavolisib
RG6114, GDC-0077
T153752060571-02-8
Inavolisib (GDC-0077) is an orally available selective PI3Kα inhibitor with an IC50 value of 0.038 nM.It exerts its activity by binding to the ATP-binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3.
  • $80
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D-GsMTx4 TFA
T37697L
D-GsMTx4 TFA, a selective spider venom peptide, is a TRPC1/6 and Piezo2 inhibitor that inhibits cation-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families, blocks cation-selective stretch-activated channels (SACs), and attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglia reactivity. toxicity and microglia reactivity.D-GsMTx4 TFA prevented myocardial infarction in a mouse model of ischemia/reperfusion and can be used to characterize the role of excitatory MSCs in normal physiology and pathology.
  • $438
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LY294002
SF 1101, NSC 697286, LY 294002
T2008154447-36-6
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.
  • $34
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3-Methyladenine
NSC 66389, 3-MA
T18795142-23-4
3-Methyladenine (3-MA) is a PI3K inhibitor that selectively inhibits class IB PI3Kγ (IC50 = 60 μM) and class III VPS34 (IC50 = 25 μM). 3-Methyladenine inhibits autophagy.
  • $35
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STX-478
T782112883540-92-7
STX-478 is an orally active and selective PI3Kα inhibitor that penetrates the blood-brain barrier and has anticancer activity to inhibit tumor growth.STX-478 is indicated for the study of breast cancer and other cancers.
  • $81
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RLY-2608
Zovegalisib, RLY2608, RLY 2608
T812642733573-94-7In house
RLY-2608 is a selective mutant PI3Kα inhibitor that inhibits tumor growth in a PIK3CA mutant xenograft model.
  • $538
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Taurocholic acid
N-Choloyltaurine
TN225981-24-3
Taurocholic acid (N-Choloyltaurine) is a bile acid involved in fat emulsification, possessing notable biological and immunomodulatory activities. It can inhibit bile duct injury induced by hepatic artery ligation by upregulating VEGF-A expression and protect cholangiocytes from TNF-α-induced damage via a PI3K-mediated pathway, and is commonly used to induce pancreatitis models.
  • $55
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AZD-7648
T71222230820-11-6
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.
  • $34
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Quercetin
Sophoretin
T2174117-39-5
Quercetin, a flavonoid natural product, is a SIRT1 activator. It is also a PI3K inhibitor, inhibiting PI3Kγ, PI3Kδ, and PI3Kβ with IC50 values of 2.4, 3.0, and 5.4 μM, respectively. Recognized as a heat shock protein inhibitor, Quercetin can significantly reduce exosome release in TII models by downregulating Hsp70 or Hsp90.
  • $42
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Alpelisib
BYL-719
T19211217486-61-7
Alpelisib (BYL-719) is a PI3Kα inhibitor (IC50=5 nM) with selective, potent, and oral activity, inhibiting PI3Kβ/γ/δ with low activity (IC50=250/290/1200 nM). Alpelisib demonstrates antitumor activity and specifically targets PIK3CA mutant tumors.
  • $33
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Protectin D1
NPD1, Neuroprotectin D1
T37379660430-03-5In house
Protectin D1 (Neuroprotectin D1) is a neuroprotectin produced by neuronal cells and is a potential cardioprotective agent.Protectin D1 attenuates myocardial ischemia/reperfusion injury and inhibits imiquimod-induced psoriasis-like skin inflammation by modulating the PI3K/AKT signaling pathway.
  • $245
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740 Y-P
PDGFR 740Y-P, 740YPDGFR
TQ00031236188-16-1
740 Y-P (740YPDGFR) is a PI3K activator with cell permeability. 740 Y-P binds GST fusion proteins containing the N-and C-terminal SH2 domains of p85.
  • $89
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GSK251
T395732125968-05-8
GSK251 is a novel, orally bioavailable inhibitor of PI3Kδ, exhibiting high potency and selectivity, with a unique binding mode.
  • $166
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Cytochalasin D
T322922144-77-0
Cytochalasin D is an actin inhibitor, the removal of actin stress fibers is crucial for the chondrogenic differentiation. It may be an inhibitor of some fertilization processes such as sperm penetration or sperm head decondensation. Cytochalasin D inhibit
  • $70
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Wortmannin
SL-2052, KY-12420
T628319545-26-7
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.
  • $32
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Apilimod
STA 5326
T2018541550-19-0
Apilimod (STA 5326) inhibits the production of IL-12 and IL-23 and reduces dendritic cell infiltration in psoriasis.
  • $43
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PIK-75
T2667372196-67-3
PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).
  • $38
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Torin 1
T60451222998-36-8
Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.
  • $30
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iMDK
T9460881970-80-5In house
iMDK quarterhydrate is a potent PI3K inhibitor that inhibits the growth factor MDK (also known as midkine or MK). iMDK quarterhydrate synergistically inhibits non-small cell lung cancer (NSCLC) with MEK inhibitors without harming normal cells and mice.
  • $54
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Copanlisib dihydrochloride
BAY 80-6946 dihydrochloride
T149981402152-13-9
Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is an ATP-competitive pan-class I PI3K inhibitor, with IC50 values of 0.5 nM for PI3Kα, 0.7 nM for PI3Kδ, 3.7 nM for PI3Kβ, and 6.4 nM for PI3Kγ. It exhibits superior antitumor activity and demonstrates more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR.
  • $47
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hSMG-1 inhibitor 11e
T355291402452-10-1In house
hSMG-1 inhibitor 11e is an effective and selective inhibitor of hSMG-1 (IC50 <0.05 nM) and can be used in studies about cancer treatment.
  • $157
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Solenopsin HCl(137038-57-4 Free base)
Solenopsin HCl(137038-57-4 Free base), (-)-Solenopsin A HCl
T12972L137119-46-1
Solenopsin HCl is an alkaloid extracted from fire ants, inhibiting phosphoinositide 3-kinase signaling and angiogenesis in a dose-dependent manner, affecting cardiovascular function, and used in cardiovascular disease research.
  • $195
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Resibufogenin
Recibufogenin, Bufogenin
T4A2458465-39-4
1. Resibufogenin (Bufogenin) is a cytotoxic steroid isolated from the Chinese drug ChanSu. 2. Resibufogenin can inhibit rectifier potassium current ( I K ) and transient potassium current ( I A ), it has pathological effects on central nervous system. 3. Resibufogenin corrects hypertension in a rat model of human preeclampsia, it not only prevents the advent of hypertension and proteinuria, but also the development of intrauterine growth restriction.4. Resibufogenina's major metabolic pathway in the human liver is CYP3A4 dominantly mediated 5β-hydroxylation .
  • $48
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Micheliolide
T568868370-47-8
Micheliolide(MCL) is a sesquiterpene lactone which inhibits various inflammatory response.
  • $39
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