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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| M8998 | PIK-III | PIK-III (also known as VPS34-IN2) is a potent and selective inhibitor of VPS34 enzymatic activity, with IC50s of 18 nM and 1.2 μM for VPS34 and PI(3)Kδ, respectively. |
| M8925 | LY3023414 | LY3023414 is a selective ATP-competitive inhibitor of PI3Kα and mTOR, DNA-PK, and other class I PI3K family members. |
| M7555 | SAR405 | SAR405 is a PIK3C3/Vps34 inhibitor with an IC50 of 1.2 nM. SAR405 also is a proximal inhibitor of the autophagy machinery. |
| M7538 | Tenalisib | Tenalisib (RP6530) is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively. |
| M7139 | PI 828 | PI 828 is a pI 3-kinase inhibitor, more potent than LY 294002. |
| M6307 | IPI3063 | IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5 ± 1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher. |
| M6304 | GDC-0084 | GDC-0084 is a brain penetrant inhibitor of PI3K and mTOR. |
| M6225 | GNE-317 | GNE-317 is a potent, brain-penetrant PI3K inhibitor. |
| M6175 | Serabelisib | Serabelisib (INK-1117,MLN-1117,TAK-117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase. |
| M6152 | SF2523 | SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively. |
| M6084 | IPI549 | IPI549 is a potent and selective PI3Kγ Inhibitor with IC50 of 16 nM. |
| M5344 | VPS34-IN1 | Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks. |
| M5343 | Voxtalisib Analogue | Voxtalisib (SAR245409, XL765) Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2. |
| M5337 | PI-3065 | PI-3065 is a novel potent and selective PI3K p110δ inhibitor with IC50 of 15 nM; exhibits > 100 fold selectivity against p110α, p110β, p110γ, DNA-PK and mTOR |
| M5335 | PF-4989216 | PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively. |
| M5314 | AZD-8835 | AZD8835 ia a novel mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity against PI3Kβ (IC50=431 nM) and PI3Kγ (IC50=90 nM). |
| M5268 | TGR-1202 | TGR-1202, a novel, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 & 24.3 nM, respectively. |
| M5255 | GDC-0326 | GDC-0326 is Inhibitor of the class I phosphoinositide 3-kinase (PI3K) isoform PI3Kα which has received substantial attention for their potential use in cancer therapy. |
| M5231 | GSK2269557 | Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9). |
| M4803 | AZD8186 | AZD8186 is a novel potent small molecule that targets the lipid kinase PI3Kβ with selectivity vs PI3Kα. |
| M3902 | Quercetin | Quercetin is a PI3K inhibitor with IC50 of 2.4-5.4 μM that has been shown to cause potent reversible inhibition of fatty-acid synthase. |
| M3880 | Acalisib | Acalisib (GS-9820) is an inhibitor of the beta and delta isoforms of the 110 kDa catalytic subunit of class IA phosphoinositide-3 kinases (PI3K) with potential immunomodulating and antineoplastic activities. |
| M3765 | NVP-QAV-572 | NVP-QAV-572 is a potent PI3K kianse inhibitor with IC50 of 10 nM. |
| M3730 | CNX-1351 | CNX-1351 is a selective covalent Inhibitor of PI3Kα. |
| M3679 | AMG 511 | AMG 511, a potent and selective pan class I PI3K inhibitor exhibiting IC50 values of 8, 11, 2, and 6 nM against the PI3K α, β, δ, and γ isoforms respectively. |
| M3531 | PIK-294 | PIK-294 is a highly selective p110δ inhibitor with IC50 of 10 nM, 1000-, 49- and 16-fold less potent to PI3Kα/β/γ, respectively. |
| M3474 | PIK-93 | PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM; shown to inhibit PI3Kα with IC50 of 39 nM. |
| M3450 | PIK-293 | PIK-293 is a PI3K inhibitor, mostly for PI3Kδ with IC50 of 0.24 μM, 500-, 100- and 50-fold less potent to PI3Kα/β/γ, respectively. |
| M3368 | AS-604850 | AS-604850 is a selective, ATP-competitive PI3Kγ inhibitor with IC50 of 250 nM, over 80-fold selectivity for PI3Kγ than PI3Kδ/β, and 18-fold more selective for PI3Kγ than PI3Kα. |
| M3367 | CAY10505 | CAY10505 is dehydroxyl of AS-252424, which is a PI3Kγ inhibitor with IC50 of 33 nM. |
| M3304 | YM201636 | YM201636 is a selective PIKfyve inhibitor with IC50 of 33 nM, less potent to p110α and insensitive to Fabl (yeast orthologue). |
| M3230 | D-87503 | D-87503 inhibits PI3K and Erk2 with IC50 of 62 nM and 760 nM, respectively. |
| M3218 | PKI-402 | PKI-402 is a potent dual pan-PI3K/mTOR inhibitor targeting PI3Kα/β/γ/δ and mTOR with IC50 of 2 nM/7 nM/16 nM/14 nM and 3 nM, respectively; also potent to PI3Kα mutants E545K and H1047R. |
| M3063 | TG100713 | TG100713 is a pan-PI3K inhibitor against PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ with IC50 of 50 nM, 24 nM, 165 nM and 215 nM, respectively. |
| M3007 | SF1126 | SF1126 is a soluble, vascular targeted pan-PI3K inhibitor. |
| M2609 | CZC24832 | CZC24832 is the first selective PI3Kγ inhibitor with IC50 of 27 nM, with 10-fold selectivity over PI3Kβ and >100-fold selectivity over PI3Kα and PI3Kδ. |
| M2567 | VS-5584 | VS-5584 (SB2343) is a potent and selective dual PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively. |
| M2436 | BAY 80-6946 | BAY 80-6946 is a potent and highly selective reversible PI3K inhibitor for PI3Kα/β with IC50 of 0.469 nM/3.72 nM. |
| M2296 | 3-Methyladenine | 3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM, respectively. |
| M2295 | AZD6482 | AZD6482 is an inhibitor of PI3Kβ with IC50 of 21 nM. |
| M2220 | GDC-0941 Bimesylate | GDC-0941 Bimesylate is the orally bioavailable bismesylate salt of a potent inhibitor of the class I phosphatidylinositol 3 kinase (PI3K). |
| M2135 | GDC-0032 | GDC-0032 is a potent, next generation PI3-kinase inhibitor. |
| M2104 | BYL719 | BYL719 is the first oral PI3K inhibitor that strongly and selectively inhibits the PI3K alpha isoform of PI3K. |
| M2073 | IPI-145 | IPI-145 is a potent, oral inhibitor of phosphoinositide-3-kinase (PI3K)-delta and PI3K-gamma. |
| M2053 | Wortmannin | Wortmannin is a specific, covalent inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) with IC50 of 3 nM. |
| M2050 | GSK2636771 | GSK2636771 is a potent, orally available and specific PI3K p110β (PI3K beta, PI3Kβ) inhibitor. |
| M1984 | PF-04691502 | PF-04691502 is a potent and selective, ATP-competitive PI3K/mTOR inhibitor with IC50 of 7.5 nM and 3.8 nM of AKT T308 and AKT S473, respectively. |
| M1978 | GSK1059615 | GSK1059615 is a potent, ATP-competitive inhibitor of PI 3-kinase alpha (PI3Kα) with IC50 of 2 nM. |
| M1945 | CAL-101 | CAL-101 (GS-1101) is an oral PI3Kδ-specific inhibitor that has shown preclinical and clinical activity in non-Hodgkin lymphoma and chronic lymphocytic leukemia. |
| M1933 | GNE-493 | GNE-493 is a potent, selective and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitor for the treatment of cancer. |
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