PI3K
Catalog No. | Inhibitor Name | PI3K | p110α | p110β | p110δ | p110γ | C2α | C2β | Vps34 | Other Targets |
---|---|---|---|---|---|---|---|---|---|---|
A10133 | Dactolisib (BEZ235, NVP-BEZ235) | **** | ** | *** | *** | mTOR (p70S6K),ATR | ||||
A10421 | Pictilisib (GDC-0941) | **** | ** | **** | ** | * | mTOR | |||
A10547 | LY294002 | * | * | * | ||||||
A10172 | Idelalisib (CAL-101, GS-1101) | * | * | **** | ** | * | DNA-PK | |||
A11016 | Buparlisib (BKM120, NVP-BKM120) | ** | * | ** | * | * | mTOR | |||
A10726 | PI-103 | **** | **** | **** | *** | DNA-PK,mTOR | ||||
A10923 | TGX-221 | * | **** | ** | ||||||
A10463 | IC-87114 | * | ** | * | ||||||
A11161 | Wortmannin | **** | DNA-PK,ATM,MLCK | |||||||
A10995 | XL147 analogue | *** | ** | *** | *** | |||||
A11014 | ZSTK474 | *** | *** | *** | **** | ** | ||||
A11328 | Alpelisib (BYL719) | **** | ||||||||
A10088 | AS-605240 | ** | * | * | *** | |||||
A10729 | PIK-75 HCl | *** | * | ** | DNA-PK | |||||
A11151 | 3-Methyladenine (3-MA) | * | * | |||||||
A11202 | A66 | *** | * | * | PI4Kβ | |||||
A10731 | PIK-93 | *** | * | ** | *** | * | ** | * | PI4KIIIβ,DNA-PK,ATM | |
A11035 | Omipalisib (GSK2126458, GSK458) | **** | **** | **** | **** | mTORC1,mTORC2 | ||||
A10730 | PIK-90 | *** | * | ** | *** | |||||
A11024 | PF-04691502 | **** | **** | **** | **** | P-Akt (S473),P-Akt (T308),mTOR | ||||
A10112 | AZD6482 | * | *** | ** | * | DNA-PK | ||||
A11023 | Apitolisib (GDC-0980, RG7422) | **** | *** | *** | *** | mTOR | ||||
A10438 | GSK1059615 | **** | **** | **** | **** | mTOR | ||||
A12422 | Duvelisib (IPI-145, INK1197) | *** | **** | **** | **** | |||||
A11079 | Gedatolisib (PF-05212384, PKI-587) | **** | **** | mTOR | ||||||
A10922 | TG100-115 | * | * | ** | ** | |||||
A11099 | AS-252424 | * | *** | Casein Kinase 2 | ||||||
A11162 | BGT226 (NVP-BGT226) | **** | ** | *** | mTOR | |||||
A11153 | CUDC-907 | *** | ** | *** | * | HDAC1,HDAC3,HDAC10 | ||||
A10728 | PIK-294 | * | *** | ** | ||||||
A11197 | AS-604850 | * | ** | |||||||
A11766 | Copanlisib (BAY 80-6946) | **** | **** | **** | *** | |||||
A11064 | YM201636 | * | PIKfyve | |||||||
A11169 | CH5132799 | *** | ** | * | *** | |||||
A10727 | PIK-293 | * | * | ** | * | |||||
A11089 | PKI-402 | **** | *** | *** | *** | mTOR | ||||
A11956 | TG100713 | ** | ** | *** | ** | |||||
A12480 | VS-5584 (SB2343) | **** | *** | **** | **** | mTOR | ||||
A12831 | Taselisib (GDC 0032) | **** | *** | **** | **** | * | * | |||
A11363 | CZC24832 | * | * | *** | ||||||
A16332 | IPI-549 | * | * | * | *** | |||||
A16277 | TGR-1202 | *** | ||||||||
A16272 | GDC-0084 | **** | ** | **** | *** | mTOR | ||||
A16352 | AZD8835 | *** | * | **** | ** | |||||
A15868 | PIK-III | * | * | * | *** | |||||
A15874 | VPS34-IN1 | *** | ||||||||
A16276 | Voxtalisib (XL765, SAR245409) | *** | ** | ** | *** | DNA-PK,mTOR | ||||
A15901 | AMG319 | * | * | *** | * | |||||
A15759 | AZD8186 | *** | **** | *** | * | |||||
A12889 | PF-4989216 | **** | ** | **** | ** | |||||
A15283 | Pilaralisib (XL147) | ** | *** | *** | *** | |||||
A14338 | PI-3065 | * | * | *** | * | |||||
A13021 | HS-173 | **** | ||||||||
A10766 | Quercetin | * | * | * | PKC,Src,Sirtuin | |||||
A11784 | GSK2636771 | |||||||||
A11196 | CAY10505 | |||||||||
A16126 | LY3023414 | DNA-PK,mTOR kinase | ||||||||
A13992 | GNE-317 | |||||||||
A14441 | Acalisib (GS-9820) | |||||||||
A16273 | NVP-QAV-572 | |||||||||
A16266 | ON 146040 | *** | *** | |||||||
A15992 | PQR309 | |||||||||
A15529 | MLN1117 (Serabelisib) | *** | ||||||||
A15030 | CAL-130 | |||||||||
A14379 | Panulisib (P7170, AK151761) | ALK1, mTOR, DNA-PK | ||||||||
A13879 | CNX-1351 | **** | ||||||||
A11198 | D-106669 | **** | ||||||||
A11261 | PX-866 (Sonolisib) | **** | * | **** | *** | |||||
A11511 | NVP-BAG956 | *** | * | *** | ** | PDK1 | ||||
A12935 | PF-04979064 | **** | **** | **** | **** | mTOR | ||||
A13328 | ETP-46464 | * | mTOR, DNA-PK, ATR, ATM | |||||||
A14432 | GNE-493 | **** | *** | *** | *** | mTOR |
Notes:
1.Hover mouse over " " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
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Parsaclisib
Catalog No. A13561 PI3Kδ inhibitorParsaclisib is a potent and selective PI3Kδ inhibitor, with an IC50 of 1 nM at 1 mM ATP, and shows appr 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases. 了解更多 -
CAL-130 Racemate
Catalog No. A20942 PI3Kδ inhibitorCAL-130 Racemate is the racemate of CAL-130. CAL-130 Racemate is a PI3Kδ inhibitor. 了解更多 -
Alpelisib hydrochloride
Catalog No. A21794 PI3Kα inhibitorAlpelisib hydrochloride (BYL-719 hydrochloride) is a potent, orally active, and selective PI3Kα inhibitor with IC50s of 5 nM, 250 nM, 290 nM and 1200 nM for p110α, p110γ, p110δ, and p110β, respectively. 了解更多 -
Umbralisib R-enantiomer
Catalog No. A21993 PI3Kδ inhibitorUmbralisib R-enantiomer (TGR-1202 R-enantiomer) is a PI3Kδ inhibitor, which is the less active enantiomer of TGR-1202. 了解更多 -
GSK2292767
Catalog No. A16564 PI3Kδ inhibitorGSK2292767 is a potent and selective inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ; Ki = 79 pM). GSK2292767 is >100-fold selective for PI3Kδ over a panel of 250 kinases. 了解更多 -
PI3Kdelta inhibitor 1
Catalog No. A19249 PI3Kδ inhibitorPI3Kdelta inhibitor 1 (Compound 5d) is a potent, selective and orally available PI3Kδ inhibitor with an IC50 of 1.3 nM. 了解更多 -
CHMFL-PI3KD-317
Catalog No. A19990 PI3Kδ inhibitorCHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM. 了解更多 -
BEZ235 (NVP-BEZ235, Dactolisib)
Catalog No. A10133 PI3K/mTOR 抑制剂BEZ235 (NVP-BEZ235,Dactolisib)是通过与这些酶的ATP结合裂隙结合来抑制PI3K和mTOR激酶活性。 了解更多 -
BKM120 (NVP-BKM120, Buparlisib)
Catalog No. A11016 PI3K 抑制剂?BKM120 (NVP-BKM120,Buparlisib)是生物可利用的口服泛I类磷脂酰肌醇3激酶(PI3K)激酶抑制剂,在无细胞试验中作用于p110α/β/δ/γ的。对VPS34,mTOR,DNAPK的作用效果下降,而对 PI4Kβ几乎没有活性。 了解更多 -
GDC-0941 (Pictilisib)
Catalog No. A10421 PI3K 抑制剂GDC-0941 (Pictilisib)是一种强效、选择性、口服生物可利用的I类PI3激酶(PI3K)抑制剂,p110 α、β、δ和γ亚型、DNA-PK和mTOR的IC50值分别为3、33、3、75、1230和580 nM。 了解更多 -
ZSTK474
Catalog No. A11014 -
XL147 analogue
Catalog No. A10995 PI3K 抑制剂XL147 analogue是一种有效的,选择性的,口服可生物利用的I类磷脂酰肌醇3激酶(PI3K)小分子抑制剂,作用于PI3Kα/δ/γ,对PI3Kβ作用效果稍弱。具有潜在的抗肿瘤活性。 了解更多 -
CAL-101 (GS-1101, Idelalisib)
Catalog No. A10172 PI3K 抑制剂CAL-101 (GS-1101,Idelalisib)是PI3K的同种型选择性抑制剂,可诱导慢性淋巴细胞性白血病(CLL)细胞凋亡。 了解更多 -
GSK1059615
Catalog No. A10438 mTOR/PI3K 抑制剂GSK1059615是PI3Kα (IC50 = 2 nM)的强效、可逆、ATP竞争性噻唑烷二酮抑制剂。 了解更多 -
TGX-221
Catalog No. A10923 -
NU-7441 (KU-57788)
Catalog No. A11098 DNA-PK 抑制剂NU-7441 (KU-57788)是一种有效的选择性DNA依赖性蛋白激酶(DNA-PK)抑制剂。对于DNA-PK,mTOR,PI 3-K,ATM和ATR,IC50值分别为14、1700、5000,> 100000和> 100000 nM。 了解更多 -
CUDC-907 (Fimepinostat)
Catalog No. A11153 PI3K/HDAC 抑制剂CUDC-907 (Fimepinostat)是针对PI3K和HDAC的单一小分子抑制剂,作用于PI3Kα和HDAC1/2/3/10,IC50分别为19 nM和1.7 nM/5 nM/1.8 nM/2.8 nM。 了解更多 -
Wortmannin
Catalog No. A11161 PI3K 抑制剂Wortmannin是一种有效的,选择性的,可透过细胞的且不可逆的磷脂酰肌醇3-激酶(PI 3-激酶)(IC50 = 2-4 nM)抑制剂,它也有效抑制polo-like激酶1(PLK1)(IC50 = 5.8 nM)。 了解更多 -
PIK-75 hydrochloride
Catalog No. A10729 PI3K 抑制剂PIK-75是一种p110α抑制剂,IC50值为5.8nM。在p110γ和p110β的效果较差,IC50值为0.076 ?M和1.3 ?M。 了解更多 -
BYL719 (Alpelisib)
Catalog No. A11328 PI3K 抑制剂BYL719 (Alpelisib)是一种口服生物可利用的磷脂酰肌醇3-激酶(PI3K)抑制剂,抑制 p110α/p110γ/p110δ/p110β 的 IC50 分别为 5 nM,250 nM,290 nM,1200 nM 。具有潜在的抗肿瘤活性。 了解更多 -
BAY 80-6946 (Copanlisib)
Catalog No. A11766 PI3K 抑制剂BAY 80-6946 (Copanlisib)是具有潜在抗肿瘤活性的磷酸肌醇3激酶(PI3K)抑制剂。 了解更多 -
GSK2636771
Catalog No. A11784 -
VS-5584
Catalog No. A12480 -
Panulisib (P7170, AK151761)
Catalog No. A14379 -
AZD8186
Catalog No. A14164 -
CAL-130
Catalog No. A15030 -
CAL-130 Hydrochloride
Catalog No. A15031 PI3K 抑制剂CAL-130 Hydrochloride是一种新型的磷酸肌醇3激酶(PI3K)抑制剂。据报道,PI3Kδ/γ的联合抑制可作为T细胞急性淋巴细胞白血病(T-ALL)的疗法。 了解更多 -
LY 303511
Catalog No. A15147 -
NVP-BKM120 Hydrochloride
Catalog No. A15195 PI3K 抑制剂?NVP-BKM120 Hydrochloride是p110α/β/δ/γ的选择性PI3K抑制剂,IC50分别为52 nM/166 nM/116 nM/262 nM。对VPS34,mTOR,DNA-PK的效力降低,对PI4Kβ几乎没有活性。 了解更多 -
PI-103 Hydrochloride
Catalog No. A15212 PI3K 抑制剂PI-103 Hydrochloride是对重组PI3K亚型p110alpha(IC50 = 2 nM),p110beta(IC50 = 3 nM),p110delta(IC50 = 3 nM)和p110gamma(IC50 = 15 nM)具有低IC50值的有效抑制剂,对mTOR的效力较低/DNA-PK,IC50为30 nM/23 nM。 了解更多 -
XL-147 (Pilaralisib)
Catalog No. A15283