Catalog

PI3K Phosphoinositide 3-kinases

Inhibitors

Cat.No.	Name	Information
M9017	Bimiralisib	Bimiralisib (PQR309) is an orally bioavailable inhibitor of PI3K and mTOR, with potential antineoplastic activity.
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.

Signaling Pathways

Product Type

PI3K Phosphoinositide 3-kinases

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