| S7938 |
GSK2292767 |
GSK2292767 is a potent and selective PI3Kδ inhibitor. |
Selective |
|
| S7937 |
Nemiralisib |
Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9). |
Selective |
PI3Kδ, pKi: 9.9 |
| S8917 |
P110δ-IN-1 |
P110δ-IN-1 is an oral, potent and selective inhibitor of Phosphatidylinositol 3-Kinase (PI3K) P110δ with IC50 of 0.6 nM in cellular assay. |
Selective |
P110δ, IC50: 0.6 nM |
| S8693 |
Selective PI3Kδ Inhibitor 1 (compound 7n) |
Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM]. |
Selective |
PI3Kδ, IC50: 0.9 nM |
| S7335 |
IPI-3063 |
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. |
Selective |
p110δ, IC50: 2.5 nM |
| S2226 |
Idelalisib (CAL-101) |
Idelalisib (CAL-101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Idelalisib also stimulates autophagy. |
Selective |
p110δ, IC50: 2.5 nM |
| S2227 |
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. |
Selective |
p110δ, IC50: 10 nM |
| S8752 |
leniolisib (CDZ 173) |
Leniolisib (CDZ 173) is a potent PI3Kδ selective inhibitor with biochemical IC50 values of 0.244, 0.424, 2.23 and 0.011 μM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. |
Selective |
PI3Kδ, IC50: 0.011 μM |
| S8560 |
Seletalisib (UCB-5857) |
Seletalisib (UCB-5857) is a novel small-molecule inhibitor of PI3Kδ with an IC50 value of 12 nM and shows significant selectivity to PI3Kδ with respect to the other class I PI3K isoforms (between 24- and 303-fold). |
Selective |
PI3Kδ, IC50: 12 nM |
| S5818 |
acalisib (GS-9820) |
Acalisib (GS-9820, CAL-120) is a highly selective and potent p110δ inhibitor (IC50 = 14 nM) with 114- to 400-fold selectivity over the other class I PI3K enzymes and no activity against Class II and III PI3K family members or other PI3K-related proteins including mTOR and DNA-PK. |
Selective |
p110δ, IC50: 14 nM |
| S7623 |
PI-3065 |
PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members.
|
Selective |
p110δ, IC50: 15 nM |
| S7813 |
AMG319 |
AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.
|
Selective |
PI3Kδ, IC50: 18 nM |
| S8194 |
umbralisib (TGR-1202) |
Umbralisib (TGR-1202, Rp-5264), 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. |
Selective |
PI3Kδ, IC50: 22.2 nM |
| S2207 |
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. |
Selective |
p110δ, IC50: 0.24 μM |
| S1268 |
IC-87114 |
IC-87114 is a selective PI3Kδ inhibitor with IC50 of 0.5 μM in a cell-free assay, 58-fold more selective for PI3Kδ than PI3Kγ, and over 100-fold more selective than PI3Kα/β. |
Selective |
PI3Kδ, IC50: 0.5 μM |
| S2658 |
Omipalisib (GSK2126458) |
Omipalisib (GSK2126458, GSK458) is a highly selective and potent inhibitor of p110α/β/δ/γ, mTORC1/2 with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM in cell-free assays, respectively. Omipalisib induces autophagy. Phase 1. |
Pan |
p110δ, Ki: 0.024 nM |
| S8045 |
KU-0060648 |
KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM. |
Pan |
PI3Kδ, IC50: 0.1 nM |
| S7103 |
Taselisib (GDC 0032) |
Taselisib (GDC 0032, RG7604) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ. |
Pan |
PI3Kδ, Ki: 0.12 nM |
| S2802 |
Copanlisib |
Copanlisib is a potent pan-class I PI3K with IC50 of 0.5, 3.7, 6.4, and 0.7 nM in cell-free assays for PI3Kα/β/γ/δ , respectively. Phase 3.This product has poor solubility, animal experiments are available, cell experiments please choose carefully! |
Pan |
PI3Kδ, IC50: 0.7 nM |
| S7675 |
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.
|
Pan |
p110δ, IC50: 1 nM |
| S7028 |
Duvelisib (IPI-145) |
Duvelisib (IPI-145, INK1197) is a novel and selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM in cell-free assays, highly selective for PI3K δ/γ than other protein kinases. Phase 3. |
Pan |
PI3Kδ, Ki: 23 pM |
| S2743 |
PF-04691502 |
PF-04691502 (PF4691502) is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM in cell-free assays, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. PF-04691502 induces apoptosis. Phase 2. |
Pan |
PI3Kδ, Ki: 1.6 nM |
| S1360 |
GSK1059615 |
GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively. Phase 1. |
Pan |
PI3Kδ, IC50: 2 nM |
| S7016 |
VS-5584 (SB2343) |
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. Phase 1. |
Pan |
PI3Kδ, IC50: 2.7 nM |
| S1038 |
PI-103 |
PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma. |
Pan |
p110δ, IC50: 3 nM |
| S8163 |
Paxalisib (GDC-0084) |
Paxalisib (GDC-0084, RG7666) is a brain penetrant inhibitor of PI3K and mTOR with Kiapp values of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR. |
Pan |
PI3Kδ, Ki app: 3 nM |
| S1065 |
Pictilisib (GDC-0941) |
Pictilisib (GDC-0941, RG7321) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2. |
Pan |
p110δ, IC50: 3 nM |
| S8157 |
GDC-0326 |
GDC-0326 is a potent and selective inhibitor of PI3Kα with Ki value of 0.2 nM; remarkably selective over the other class I isoforms in enzymatic assays. |
Pan |
PI3Kδ, Ki: 4 nM |
| S1072 |
ZSTK474 |
ZSTK474 inhibits class I PI3K isoforms with IC50 of 37 nM in a cell-free assay, mostly PI3Kδ. Phase1/2. |
Pan |
PI3Kδ, IC50: 4.6 nM |
| S7966 |
AZD8835 |
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). |
Pan |
PI3Kδ, IC50: 5.7 nM |
| S1009 |
Dactolisib (BEZ235) |
Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2. |
Pan |
p110δ, IC50: 7 nM |
| S2696 |
Apitolisib (GDC-0980) |
Apitolisib (GDC-0980, RG7422, GNE 390) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Apitolisib activates autophagy and apoptosis simultaneously in pancreatic cancer cells. Phase 2. |
Pan |
p110δ, IC50: 7 nM |
| S7694 |
AZD8186 |
AZD8186 is a potent and selective inhibitor of PI3Kβ and PI3Kδ with IC50 of 4 nM and 12 nM, respectively. Phase 1.
|
Pan |
PI3Kδ, IC50: 12 nM |
| S2739 |
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. |
Pan |
PI3Kδ, IC50: 14 nM |
| S2870 |
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. |
Pan |
PI3Kδ, IC50: 24 nM |
| S8672 |
Tenalisib (RP6530) |
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. |
Pan |
PI3Kδ, IC50: 24.5 nM |
| S8738 |
Bimiralisib (PQR309) |
Bimiralisib (PQR309) is a novel brain-penetrant dual PI3K/mTOR inhibitor with in vitro and in vivo antilymphoma activity. It displays excellent selectivity versus PI3K-related lipid kinases, protein kinases and unrelated targets. |
Pan |
PI3Kδ, Kd: 25 nM |
| S1118 |
XL147 analogue |
XL147 analogue (SAR245408) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. XL147 analogue induces apoptosis. Phase 1/2. |
Pan |
PI3Kδ, IC50: 36 nM |
| S7645 |
Pilaralisib (XL147) |
Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.
|
Pan |
PI3Kδ, IC50: 36 nM |
| S2759 |
Fimepinostat (CUDC-907) |
CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. CUDC-907 induces cell cycle arrest and apoptosis in breast cancer cells. Phase 1. |
Pan |
PI3Kδ, IC50: 39 nM |
| S1523 |
Voxtalisib (XL765) 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. |
Pan |
PI3Kδ, IC50: 43 nM |
| S7646 |
Voxtalisib (XL765) |
Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
|
Pan |
PI3Kδ, IC50: 43 nM |
| S1187 |
PIK-90 |
PIK-90 is a PI3Kα/γ/δ inhibitor with IC50 of 11 nM/18 nM/58 nM, respectively, less potent to PI3Kβ. |
Pan |
PI3Kδ, IC50: 58 nM |
| S1462 |
AZD6482 |
AZD6482 (KIN-193) is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ in cell-free assays. Phase 1. |
Pan |
PI3Kδ, IC50: 80 nM |
| S1169 |
TGX-221 |
TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM in a cell-free assay, 1000-fold more selective for p110β than p110α. |
Pan |
p110δ, IC50: 0.1 μM |
| S2247 |
Buparlisib (BKM120) |
Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Buparlisib induces apoptosis. Phase 2. |
Pan |
p110δ, IC50: 116 nM |
| S1352 |
TG100-115 |
TG100-115 is a PI3Kγ/δ inhibitor with IC50 of 83 nM/235 nM, with little effect on PI3Kα/β. Phase 1/2. |
Pan |
PI3Kδ, IC50: 235 nM |
| S1410 |
AS-605240 |
AS-605240 selectively inhibits PI3Kγ with IC50 of 8 nM, over 30-fold and 7.5-fold more selective for PI3Kγ than PI3Kδ/β and PI3Kα in cell-free assays, respectively. |
Pan |
PI3Kδ, IC50: 300 nM |
| S8948 |
SRX3207 |
SRX3207 is an orally active dual inhibitor of Syk-PI3K with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 blocks tumor immunosuppression and increases anti-tumor immunity. |
Pan |
PI3K delta, IC50: 388 nM |
| S2699 |
CH5132799 |
CH5132799 (MEN1611, PA799) inhibits class I PI3Ks, particularly PI3Kα with IC50 of 14 nM; less potent to PI3Kβδγ, while sensitive in PIK3CA mutations cell lines. Phase 1. |
Pan |
PI3Kδ, IC50: 0.50 μM |
| S1205 |
PIK-75 HCl |
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. |
Pan |
p110δ, IC50: 0.51 μM |
| S1105 |
LY294002 |
LY294002 (SF 1101, NSC 697286) is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autoph |
Pan |
p110δ, IC50: 0.57 μM |
| S7683 |
PIK-III |
PIK-III (VPS34-IN2), which is a selective inhibitor of VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates. The IC50 values for VPS34 and PI(3)Kδ are 0.018 μM and 1.2 μM respectively. |
Pan |
PI3Kδ, IC50: 1.2μM |
| S2347 |
Quercetin Dihydrate |
Quercetin (Sophoretin), a polyphenolic flavonoid found in a wide variety of plant-based foods, such as apples, onions, berries, and red wine, is utilized in many different cultures for their nervous system and anticancer effects. Quercetin (dihydrate), a natural flavonoid, is a stimulator of recombinant SIRT1 and a PI3K inhibitor with IC50s of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively. |
Pan |
PI3Kδ, IC50: 3.0 μM |
| S2391 |
Quercetin |
Quercetin, a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4. |
Pan |
PI3Kδ, IC50: 3.0 μM |
