Search Result
| Isoforms Recommended: |
PI3Kγ
|
Results for "
PI3Kγ
" in MedChemExpress (MCE) Product Catalog:
5
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-18085
-
-
-
- HY-10681
-
|
PKI-587; PF-05212384
|
PI3K
mTOR
|
Cancer
|
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Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively . Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2 .
|
-
-
- HY-N0451
-
|
5,7-Dihydroxy-4'-methoxyflavone
|
Apoptosis
Autophagy
|
Neurological Disease
Inflammation/Immunology
Cancer
|
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Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an orally active flavonoid derived from Dendranthema morifolium. Acacetin docks in the ATP binding pocket of PI3Kγ. Acacetin causes cell cycle arrest and induces apoptosis and autophagy in cancer cells. Acacetin has potent anti-cancer and anti-inflammatory activity and has the potential for pain-related diseases research .
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-
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- HY-100716
-
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IPI-549
|
PI3K
|
Cancer
|
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Eganelisib (IPI549) is a potent and selective PI3Kγ inhibitor with an IC50 of 16 nM. Eganelisib shows >100-fold selectivity over other lipid and protein kinases .
|
-
-
- HY-D0254
-
|
Pyrogallol phthalein
|
PI3K
|
Cancer
|
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Gallein is a Gβγ subunit signaling inhibitor that can interfere with the interaction between Gβγ subunit and PI3Kγ, regulate platelet function, and exhibit anti-tumor activity [1][3].
|
-
-
- HY-18085A
-
-
-
- HY-15346
-
|
BAY 80-6946
|
PI3K
Apoptosis
|
Cancer
|
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Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity .
|
-
-
- HY-15346A
-
|
BAY 80-6946 dihydrochloride
|
PI3K
Apoptosis
|
Cancer
|
|
Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity .
|
-
-
- HY-19962
-
|
GDC-0084
|
PI3K
mTOR
|
Cancer
|
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Paxalisib (GDC-0084) is a brain penetrant inhibitor of PI3K and mTOR, with Kis of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively .
|
-
-
- HY-13898
-
|
GDC-0032; RG-7604
|
PI3K
|
Cancer
|
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Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
|
-
-
- HY-12868
-
|
PQR309
|
PI3K
mTOR
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.
|
-
-
- HY-13246
-
|
GDC-0980; GNE 390; RG 7422
|
PI3K
mTOR
Apoptosis
|
Cancer
|
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Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a?Ki?of 17 nM for mTOR.
|
-
-
- HY-13532
-
|
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PI3K
|
Cancer
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AS-252424 is a potent and selective PI3Kγ inhibitor with an IC50 of 30±10 nM.
|
-
-
- HY-N0146
-
|
|
PI3K
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
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 .
|
-
-
- HY-18085R
-
-
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- HY-12513
-
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LY3023414
|
PI3K
DNA-PK
mTOR
Autophagy
|
Cancer
|
|
Samotolisib (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. Samotolisib potently inhibits mTORC1/2 at low nanomolar concentrations .
|
-
-
- HY-10109
-
|
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PI3K
Autophagy
|
Cancer
|
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AS-605240 is a specific and orally active inhibitor of the PI3Kγ, with an IC50 of 8 nM, and a Ki of 7.8 nM.
|
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- HY-12046
-
|
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PI4K
PI3K
Virus Protease
|
Cancer
|
|
PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM, and also inhibits PI3Kγ and PI3Kα with IC50 of 16 nM and 39 nM, respectively.
|
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- HY-50847
-
|
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PI3K
Autophagy
|
Cancer
|
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ZSTK474 is an ATP-competitive pan-class I PI3K inhibitor with IC50s of 16 nM, 44 nM, 4.6 nM and 49 nM for PΙ3Κα, PI3Kβ, PI3Kδ and PI3Kγ, respectively.
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- HY-12330
-
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PI3K
|
Cancer
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AZD8186 is a PI3K inhibitor, which potently inhibits PI3Kβ (IC50=4 nM) and PI3Kδ (IC5050=12 nM) with selectivity over PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM).
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-
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- HY-111570
-
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PI3K
|
Inflammation/Immunology
|
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PI3Kγ inhibitor AZ2 is a highly selective PI3Kγ inhibitor (The pIC50 value for PI3Kγ is 9.3). PI3Kγ inhibitor AZ2 can be used for the research of inflammatory and immune diseases .
|
-
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- HY-101146
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SF2523
2 Publications Verification
|
PI3K
Epigenetic Reader Domain
DNA-PK
|
Cancer
|
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SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
|
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- HY-16526
-
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XL-147; SAR245408
|
PI3K
|
Cancer
|
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Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.
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-
- HY-10683
-
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PI3K
mTOR
|
Cancer
|
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PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC50=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).
|
-
-
- HY-16585
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VS-5584
5 Publications Verification
SB2343
|
PI3K
mTOR
|
Cancer
|
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VS-5584 is a pan-PI3K/mTOR kinase inhibitor with IC50s of 16 nM, 68 nM, 42 nM, 25 nM, and 37 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively. VS-5584 simultaneously blocks mTORC2 as well as mTORC1.
|
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- HY-111508
-
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PI3K
mTOR
|
Cancer
|
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PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/34/16/1 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR . Antitumor activity .
|
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- HY-144806
-
|
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PI3K
Akt
Apoptosis
|
Cancer
|
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PI3K/AKT-IN-1 is an effective PI3K/AKT dual inhibitor (IC50 of 6.99, 4.01 and 3.36 μM for PI3Kγ, PI3Kδ and AKT, respectively). PI3K/AKT-IN-1 has anticancer activity and acts by inhibiting PI3K/AKT axis and inducing caspase 3 dependent apoptosis .
|
-
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- HY-15294
-
-
-
- HY-112897
-
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Autophagy
PI3K
Apoptosis
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Cancer
|
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IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.
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- HY-13531
-
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PI3K
|
Cancer
|
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AS-604850 is a potent, selective and ATP-competitive PI3Kγ inhibitor with an IC50 value of 0.25 μM and a Ki value of 0.18 μM. AS-604850 shows isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα, respectively .
|
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- HY-17645
-
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RP6530
|
PI3K
|
Cancer
|
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Tenalisib (RP6530) is a novel, potent, and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively.
|
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- HY-13431
-
|
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DNA-PK
PI3K
mTOR
|
Cancer
|
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KU-0060648 is a dual inhibitor of PI3K and DNA-PK with IC50s of 4 nM, 0.5 nM, 0.1 nM, 0.594 nM and 8.6 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and DNA-PK, respectively .
|
-
-
- HY-10811
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GNE-493
2 Publications Verification
|
PI3K
mTOR
|
Cancer
|
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GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
|
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-
- HY-13334
-
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NVP-BGT226 maleate
|
PI3K
mTOR
Autophagy
Apoptosis
|
Cancer
|
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BGT226 (NVP-BGT226 maleate) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ) /mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells .
|
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- HY-12034
-
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mTOR
Autophagy
Apoptosis
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Cancer
|
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WYE-354 is an ATP-competitive mTOR inhibitor with an IC50 of 5 nM. WYE-354 also inhibits PI3Kα and PI3Kγ with IC50s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits both mTORC1 and mTORC2. WYE-354 induces autophagy activation in vitro [3].
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- HY-13530
-
|
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PI3K
Apoptosis
|
Cancer
|
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CAY10505 is a potent and selective PI3Kγ inhibitor with an IC50 of 30 nM in neurons.
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-
-
- HY-13333
-
|
BAG 956
|
PI3K
|
Cancer
|
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NVP-BAG956 is an ATP-competitive PI3K inhibitor with IC50s of 34, 56, 112 and 444 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
|
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- HY-15271
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WYE-687
3 Publications Verification
|
mTOR
PI3K
|
Cancer
|
|
WYE-687 is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
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-
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- HY-19798
-
|
|
PI4K
PI3K
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Cancer
|
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PI4KIIIbeta-IN-9 is a potent PI4KIIIβ inhibitor with an IC50 of 7 nM. PI4KIIIbeta-IN-9 also inhibits PI3Kδ and PI3Kγ with IC50s of 152 nM and 1046 nM, respectively.
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-
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- HY-18085S1
-
-
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- HY-162713
-
|
|
EGFR
PI3K
PPAR
|
Cancer
|
|
MTX-531 is an oral drug that inhibits EGFR (with an IC50 of 14.7 nM) and PI3K (with IC50 values of 6.4, 233, 8.3, and 1.1 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ respectively), and it has anti-tumor effects. MTX-531 also acts as a weak agonist of PPARγ, with an IC50 of 2.5 µM, helping to alleviate hyperglycemia induced by PI3K inhibitors .
|
-
-
- HY-115870
-
|
|
PI3K
|
Inflammation/Immunology
|
|
AZD8154 is a selective PI3Kγδ dual inhibitor. AZD8154 can suppress PI3Kγ and PI3Kδ signaling pathway activation. AZD8154 can be used for the researches of inflammation and immunology, such as asthma .
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-
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- HY-143404
-
|
|
PI3K
|
Cancer
|
|
PI3K-IN-30 (compound 6d) is a potent PI3K inhibitor with IC50s of 5.1, 136, 30.7 and 8.9 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively .
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-
-
- HY-112443
-
-
-
- HY-110109
-
|
|
PI3K
DNA-PK
mTOR
|
Cancer
|
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ETP-45658 is a potent PI3K inhibitor, with IC50s of 22.0 nM, 39.8 nM, 129.0 nM and 717.3 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. ETP-45658 also can inhibit DNA-PK (IC50=70.6 nM) and mTOR (IC50=152.0 nM). ETP-45658 can be used for the research of cancer .
|
-
-
- HY-148317
-
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|
PI3K
|
Inflammation/Immunology
|
|
PI3Kγ inhibitor 6 (compound 9) is a PI3Kγ inhibitor. PI3Kγ inhibitor 6 can be used for the research of inflammatory and autoimmune diseases .
|
-
-
- HY-147419
-
|
|
PI3K
|
Cancer
|
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Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. Antiproliferative and antineoplastic activity .
|
-
-
- HY-128333
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-4 is an orally active pan-class I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC50 values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer .
|
-
-
- HY-10812
-
|
|
PI3K
mTOR
|
Cancer
|
|
GNE-490, a (thienopyrimidin-2-yl)aminopyrimidine, is a potent pan-PI3K inhibitor with IC50s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC50=750 nM). GNE-490 shows potent suppression efficacy profile against MCF7.1 breast cancer xenograft model .
|
-
-
- HY-10681R
-
|
|
PI3K
mTOR
Reference Standards
|
Cancer
|
|
Gedatolisib (Standard) is the analytical standard of Gedatolisib. This product is intended for research and analytical applications. Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively . Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2 .
|
-
- HY-118521
-
|
|
PI3K
|
Inflammation/Immunology
|
|
AS-041164 is a potent, selective and orally active PI3Kγ isoform inhibitor with an IC50 of 70 nM. AS-041164 shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). AS-041164 has anti-inflammatory effects .
|
-
- HY-132299
-
|
|
PI3K
|
Inflammation/Immunology
|
|
PI3Kγ inhibitor 4 is a potent, selective and orally active inhibitor of PI3Kγ, with an IC50 of 40 nM. PI3Kγ inhibitor 4 shows ∼7, 43, and 18-fold selectivity for PI3Kγ over the α, β, and δ isoforms, respectively. PI3Kγ inhibitor 4 can be used for the research of airway inflammation .
|
-
- HY-133907
-
-
- HY-18085S2
-
-
- HY-150638
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3Kδ/γ-IN-3 (Compound 58) is a potent and orally active PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 16 nM, respectively. PI3Kδ/γ-IN-3 induces tumor cell apoptosis and can be used for B-cell malignancies research .
|
-
- HY-139880
-
|
|
PI3K
|
Cancer
|
|
PI3Kγ inhibitor 5 is an inhibitor of phosphoinositide 3-kinase γ (PI3Kγ) with an IC50 value of 34 nM.
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-
- HY-112286
-
|
|
PI3K
|
Inflammation/Immunology
|
|
PI3Kγ inhibitor 2 (Compound 16) is an orally bioavailable, CNS-penetrant, isoform selective PI3Kγ inhibitor with a Ki of 4 nM .
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-
- HY-153703
-
|
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PI3K
|
Cancer
|
|
PI3Kγ inhibitor 7 (compound 2) is a potent and orally active PI3Kγ inhibitor with IC50 values of 4768, 878.1, 3.42, 355.2 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively. PI3Kγ inhibitor 7 shows antitumor activity . PI3Kγ inhibitor 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
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- HY-10549
-
|
|
PI3K
|
Cancer
|
|
PI3Kγ inhibitor 1 is a PI3Kδ and PI3Kγ inhibitor extracted from patent WO2014004470A1, Compound 168 in Table 4, has IC50s of <100 nM.
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- HY-168319
-
-
- HY-143403
-
|
|
PI3K
|
Cancer
|
|
PI3K-IN-31 (Compound 6b) is a potent PI3K inhibitor with IC50s of 3.7 nM, 74 nM, 14.6 nM, and 9.9 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. PI3K-IN-31 has anticancer effects .
|
-
- HY-123849
-
|
|
PI3K
mTOR
|
Cancer
|
|
SN32976 is a potent and selective class I PI3K and mTOR inhibitor with IC50s of 15.1 nM, 461 nM, 110 nM, 134 nM and 194 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR, respectively. SN32976 shows high selectivity among other 442 kinases. SN32976 shows anticancer effects .
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- HY-131345A
-
|
|
PI3K
|
Cancer
|
|
(S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC50 of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer .
|
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- HY-161366
-
|
|
PI3K
|
Cancer
|
|
OMS14 is exhibits inhibitory activity for phosphoinositide 3-kinase γ (PI3Kγ) and PIK3CD/PIK3R1, which inhibits 19% PI3Kγ and 65% PIK3CD/PIK3R1 activity at 100 μM. OMS14 exhibits anticancer efficacy in various cancer cells .
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- HY-18085S
-
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PI3K
Autophagy
Mitophagy
Apoptosis
|
Cancer
|
|
Quercetin-d5 is a deuterium labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively .
|
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- HY-100694
-
|
|
PI3K
|
Inflammation/Immunology
|
|
GS-9901 is a highly selective and orally active PI3Kδ inhibitor with an IC50 of 1 nM. GS-9901 has ≥100 fold selectivity for PI3Kα (IC50 of 750 nM), PI3Kβ (IC50 of 100 nM) and PI3Kγ (IC50 of 190 nM). GS-9901 can be used for the study of rheumatoid arthritis .
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- HY-N0146R
-
|
|
Reference Standards
PI3K
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Quercetin (dihydrate) (Standard) is the analytical standard of Quercetin (dihydrate). This product is intended for research and analytical applications. 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 .
|
-
- HY-130133
-
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|
PI3K
mTOR
Akt
Apoptosis
Paraptosis
p38 MAPK
Mitochondrial Metabolism
P-glycoprotein
CDK
MMP
HIF/HIF Prolyl-Hydroxylase
VEGFR
|
Cancer
|
|
DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research [3].
|
-
- HY-112614
-
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ATM/ATR
|
Cancer
|
|
ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM, shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM). ATM Inhibitor-1 exhibits anti-tumor activity .
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- HY-16122A
-
|
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PI3K
|
Cancer
|
|
CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC50s of 1.3 and 6.1 nM, respectively.
|
-
- HY-N0451R
-
|
5,7-Dihydroxy-4'-methoxyflavone (Standard)
|
Reference Standards
Apoptosis
Autophagy
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Acacetin (Standard) is the analytical standard of Acacetin. This product is intended for research and analytical applications. Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an orally active flavonoid derived from Dendranthema morifolium. Acacetin docks in the ATP binding pocket of PI3Kγ. Acacetin causes cell cycle arrest and induces apoptosis and autophagy in cancer cells. Acacetin has potent anti-cancer and anti-inflammatory activity and has the potential for pain-related diseases research .
|
-
- HY-120438
-
|
|
PI3K
Akt
|
Inflammation/Immunology
|
|
TASP0415914 is a potent and orally active PI3Kγ inhibitor with an IC50 of 29 nM. TASP0415914 also shows potent Akt inhibitory activities with an IC50 of 294 nM. TASP0415914 can be used for inflammatory diseases research .
|
-
- HY-17651
-
|
|
PI3K
|
Inflammation/Immunology
Cancer
|
|
PI3K-IN-60 (Compound 34) is a highly selective phosphatidylinositol 3-kinase gamma (PI3Kγ) inhibitor. PI3K-IN-60 is promising for research of autoimmune diseases (e.g., multiple sclerosis) and cancers (e.g., breast cancer, pancreatic ductal adenocarcinoma) .
|
-
- HY-P10093
-
|
|
PI3K
|
Others
|
|
Penetratin-PI3Kγ(126-150) is a peptide inhibitor of ΡI3Κγ that plays an important role in respiratory system diseases .
|
-
- HY-16122B
-
|
|
PI3K
|
Cancer
|
|
CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC50s of 1.3 and 6.1 nM, respectively.
|
-
- HY-112172
-
|
RP6530 R Enantiomer
|
PI3K
|
Cancer
|
|
Tenalisib R Enantiomer (RP6530 R Enantiomer) is an R enantiomer of Tenalisib. Tenalisib is a potent and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively .
|
-
- HY-177908
-
|
|
STING
PI3K
|
Cancer
|
|
SH-273 is a dual targeting compound. SH-273 has dual function to stimulate STING function (EC50: 100 nM) and inhibits PI3Kγ (IC50: 7 nM). SH-273 can be used in the research of pancreatic cancer .
|
-
- HY-146159
-
|
|
PI3K
HDAC
|
Cancer
|
|
PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC50s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC50s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects .
|
-
- HY-D0254R
-
|
Pyrogallol phthalein (Standard)
|
PI3K
Reference Standards
|
Cancer
|
|
Gallein (Standard) is the analytical standard of Gallein. This product is intended for research and analytical applications. Gallein is a Gβγ subunit signaling inhibitor that can interfere with the interaction between Gβγ subunit and PI3Kγ, regulate platelet function, and exhibit anti-tumor activity [3].
|
-
- HY-15271A
-
|
|
mTOR
PI3K
|
Cancer
|
|
WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM . WYE-687 dihydrochloride concurrently inhibits activation of mTORC1 and mTORC2 . WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively .
|
-
- HY-101517
-
|
|
PI3K
|
Cancer
|
|
PI3K-IN-2 (compound 10) is a potent and orally active PI3Kβ/δ (IC50=7.1/8.6 nM) inhibitor with excellent selectivity versus PI3Kσ and PI3Kγ (IC50=13/190 nM, respectively) .
|
-
- HY-162848
-
|
|
PI3K
|
Cancer
|
|
IHMT-PI3K-315 (20e) is a potent and selective PI3Kγ/δ inhibitor with IC50 values for PI3Kγ and PI3Kδ of 4.0 and 9.1 nM, respectively. IHMT-PI3K-315 has antitumor activity .
|
-
- HY-18085AS
-
-
- HY-155996
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
FD2157 is a photosensitive PI3K inhibitor, with IC50s of 43 nM, 83 nM, 84 nM, 14 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ respectively. FD2157 potently inhibits cancer cell proliferation and induces cell apoptosis when exposed to 365 nm UV light .
|
-
- HY-108958
-
|
|
PI3K
|
Cancer
|
|
Rac)-AZD8186 is the racemate of AZD8186 (HY-12330), a PI3K inhibitor that inhibits PI3Kβ (IC50=4 nM), PI3Kδ (IC50=12 nM), PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM) .
|
-
- HY-16526R
-
|
XL-147 (Standard); SAR245408 (Standard)
|
PI3K
Reference Standards
|
Cancer
|
|
Pilaralisib (Standard) is the analytical standard of Pilaralisib. This product is intended for research and analytical applications. Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.
|
-
- HY-147285
-
|
|
mTOR
PI3K
|
Neurological Disease
|
|
PI3K/mTOR Inhibitor-9 (Compound 1) is a potent mTOR and PI3K inhibitor with IC50 values of 38 nM, 6.6 μM, 6.6 μM and 0.8 μM against mTOR (phospho-S6 cellular assay), PI3Kα, PI3Kγ and PI3Kδ, respectively .
|
-
- HY-146789
-
|
|
PI3K
|
Cancer
|
|
PI3Kδ/γ-IN-2 is a potent PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 4.3 nM, respectively. PI3Kδ/γ-IN-2 has favorable oral bioavailability. PI3Kδ/γ-IN-2 has potential for battling B-cell malignancies .
|
-
- HY-108418
-
|
|
PI3K
|
Cancer
|
|
PI3Kδ-IN-15 (compound 6b) is a selective PI3Kδ inhibitor with an IC50 of 0.5 nM for p110δ. PI3Kδ-IN-15 inhibits PI3Kδ with >30-fold higher potency than PI3Kγ, PI3Kβ, and PI3Kα .
|
-
- HY-10109A
-
|
|
PI3K
Akt
|
Inflammation/Immunology
|
|
AS-605240 (potassium) is an orally active PI3Kγ inhibitor (IC50: 8 nM; Ki: 7.8 nM). AS-605240 (potassium) inhibits MCP-1- and CSF1-induced PKB phosphorylation (IC50 values are 0.181 and 0.550 µM, respectively). AS-605240 (potassium) reduces neutrophil recruitment in RANTES (CCL5)- and thioglycolate-induced peritonitis mouse models (EC50 values are 9.1 and 10 mg/kg, respectively). AS-605240 (potassium) ameliorates αCII-IA-induced arthritis in mice .
|
-
- HY-175083
-
|
|
Drug Derivative
PI3K
|
Others
|
|
PtdIns-(4,5)-P2-biotin trisodium is a Biotin-labeled PtdIns-(4,5)-P2 analog. PtdIns-(4,5)-P2-biotin trisodium is an affinity probe of PI3Kγ. PI3Kγ can catalyse the phosphorylation of PtdIns-(4,5)-P2 at the 3′-OH group, giving rise to the second messenger PtdIns(3,4,5)-P3 .
|
-
- HY-107387
-
|
|
PI3K
|
Metabolic Disease
Inflammation/Immunology
|
|
PF-376304 is an orally active non-specific class I phosphoinositide 3-kinase (PI3K) inhibitor with an IC50 of 0.197 μM against PI3Kγ. PF-376304 induces dose-dependent glucose and lipid metabolic disorders in rats, causes rapid death at high doses, and leads to metabolic abnormalities that are self-reversible at low doses. PF-376304 is applicable to the research of metabolic and inflammatory diseases .
|
-
- HY-118903
-
|
|
PI3K
|
Cancer
|
|
PIK-124 is a thiazolidinone-based PI3Kγ-biased PI3K inhibitor, with an IC50 of 3 nM against PI3Kγ. PIK-124 exhibits cross-reactivity with PI3Kα (IC50 = 23 nM), PI3Kδ (IC50 = 340 nM), PI3KC2α (IC50 = 140 nM) and PI3KC2β (IC50 = 370 nM). PIK-124 is applicable to breast cancer-related research .
|
-
- HY-10109R
-
|
|
PI3K
Reference Standards
Autophagy
|
Cancer
|
|
AS-605240 (Standard) is the analytical standard of AS-605240 (HY-10109). This product is intended for research and analytical applications. AS-605240 is a specific and orally active inhibitor of the PI3Kγ, with an IC50 of 8 nM, and a Ki of 7.8 nM.
|
-
- HY-183770
-
|
|
Akt
PI3K
Epigenetic Reader Domain
c-Myc
|
Cancer
|
|
LCI40 is an orally active dual PI3K/BRD4 inhibitor (PI3Kα IC50 = 0.071 μM, PI3Kβ IC50 = 0.17 μM, PI3Kγ IC50 = 0.66 μM, PI3Kδ IC50 = 0.072 μM, BRD4 BD1 IC50 = 0.19 μM, and BRD4 BD2 IC50 = 1.88 μM. LCI40 inhibits phosphorylation of pAKT (S473) and suppresses c-MYC levels in mantle cell lymphoma cells. LCI40 displays immunomodulatory capacity with minimal toxicity to normal mouse immune cells. LCI40 can be used for the research of mantle cell lymphoma .
|
-
- HY-100716R
-
|
IPI-549 (Standard)
|
PI3K
Reference Standards
|
Cancer
|
|
Eganelisib (Standard) is the analytical standard of Eganelisib (HY-100716). This product is intended for research and analytical applications. Eganelisib (IPI549) is a potent and selective PI3Kγ inhibitor with an IC50 of 16 nM. Eganelisib shows >100-fold selectivity over other lipid and protein kinases .
|
-
- HY-101146R
-
|
|
PI3K
Reference Standards
Epigenetic Reader Domain
DNA-PK
|
Cancer
|
|
SF2523 (Standard) is the analytical standard of SF2523 (HY-101146). This product is intended for research and analytical applications. SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
|
-
- HY-10681S
-
|
PKI-587-d8; PF-05212384-d8
|
Isotope-Labeled Compounds
PI3K
mTOR
|
Cancer
|
|
Gedatolisib-d8 (PKI-587-d8) is the deuterium labeled Gedatolisib (HY-10681). Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2 .
|
-
- HY-10811R
-
|
|
Reference Standards
PI3K
mTOR
|
Cancer
|
|
GNE-493 (Standard) is the analytical standard of GNE-493 (HY-10811). This product is intended for research and analytical applications. GNE-493 is a potent, selective, and orally available dual pan-PI3-Kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
|
-
- HY-10683R
-
|
|
Reference Standards
PI3K
mTOR
|
Cancer
|
|
PKi-402 (Standard) is the analytical standard of PKi-402 (HY-10683). This product is intended for research and analytical applications. PKi-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC50=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).
|
-
- HY-150618
-
-
- HY-134472
-
|
|
PI3K
|
Cancer
|
|
PI3Kδ-IN-8 is a potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 3.3 nM. PI3Kδ-IN-8 shows selectivity for PI3Kδ over PI3Kα, PI3Kβ, and PI3Kγ (IC50=377.2, 241.6, 17.9 nM, respectively). PI3Kδ-IN-8 has anti-tumor activity .
|
-
- HY-115814
-
|
|
PI3K
|
Inflammation/Immunology
|
|
AM-1430 is an efficient, highly selective and orally active small molecule inhibitor of PI3Kδ with an IC50 of 4.6 nM. AM-1430 exhibits IC50s for PI3Kα, PI3Kβ and PI3Kγ of 14.18, 2.2 and 3.22 μM, respectively. AM-1430 inhibits B cell proliferation and exhibits excellent in vivo activity in pAKT inhibition models and the hemoglobin (KLH) immune response model. AM-1430 can be used for the study of inflammation and autoimmune diseases .
|
-
- HY-137340
-
|
|
PROTACs
Casein Kinase
|
Cancer
|
|
WH-10417-099 is a CRBN-based PROTAC multi-kinase degrader that induces the degradation of the maximum number of unique kinases (over 125 unique kinases, such as CSNK1E and PI3Kγ) simultaneously. WH-10417-099 induces protein degradation via the ubiquitin biotinylation (E-STUB) pathway, exhibits synergistic effects with SB-405483 (HY-W1135319). The E3 ligase ligand and linker of WH-10417-099 can form the conjugate Pomalidomide 4'-PEG5-acid (HY-131647) .
|
-
- HY-13246R
-
|
GDC-0980 (Standard); GNE 390 (Standard); RG 7422 (Standard)
|
PI3K
mTOR
Apoptosis
Reference Standards
|
Cancer
|
|
Apitolisib (Standard) is the analytical standard of Apitolisib. This product is intended for research and analytical applications. Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a Ki of 17 nM for mTOR.
|
-
- HY-15346R
-
|
BAY 80-6946 (Standard)
|
Reference Standards
PI3K
Apoptosis
|
Cancer
|
|
Copanlisib (Standard) is the analytical standard of Copanlisib. This product is intended for research and analytical applications. Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity .
|
-
- HY-133124
-
|
|
PARP
PI3K
Apoptosis
|
Cancer
|
|
PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases .
|
-
- HY-149521
-
|
|
PI3K
|
Cancer
|
|
PI3K-IN-47 (Compound 27) is a bivalent PI3K inhibitor (IC50: 0.44 nM for PI3Kα, 7.18 nM, 13.92 nM, 22.83 nM for PI3Kβ, PI3Kγ, PI3Kδ). PI3K-IN-47 induces cell cycle arrest in G1 phase, inhibits colony formation and cell migration. PI3K-IN-47 inhibits tumor growth in HGC-27 xenograft mice .
|
-
- HY-11080A
-
|
|
PI3K
mTOR
|
Cancer
|
|
PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 hydrochloride also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride shows anti-tumor activity in vivo .
|
-
- HY-11080
-
PKI-179
1 Publications Verification
|
PI3K
mTOR
|
Cancer
|
|
PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo .
|
-
- HY-149493
-
|
|
PI3K
|
Inflammation/Immunology
Cancer
|
|
IHMT-PI3K-455 (Compound 15u) is a potent, selective, orally active PI3Kγ/δ dual inhibitor with IC50s of 7.1 nM and 0.57 nM for PI3Kγ and PI3Kδ, respectively. IHMT-PI3K-455 suppresses the AKT phosphorylation. IHMT-PI3K-455 inhibits tumor growth by recruiting and activating more CD8 + killing T cells.IHMT-PI3K-455 is used in cancer research .
|
-
- HY-106006
-
|
|
PI3K
|
Others
Inflammation/Immunology
|
|
RV-1729 is an inhibitor of the phosphatidylinositol 3-kinase-δ (PI3Kδ). RV-1729 identifies inhibition of the PI3K isotype by quantifying the release of phosphatidylinositol 3,4, 5-triphosphate (PIP3) (IC50=12 nM), showing twice the selectivity for PI3Kδ relative to PI3Kγ. RV-1729 is also 16 times more selective to PI3Kα. RV-1729 regulates immune and inflammatory responses by inhibiting PI3Kδ. RV-1729 can be used in studies of asthma and chronic obstructive pulmonary disease (COPD) .
|
-
- HY-153894
-
|
|
CDK
Epigenetic Reader Domain
PI3K
NF-κB
SARS-CoV
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
SRX3177 is a triple inhibitor of CDK4/6, PI3K, and BRD4, with IC50s of <2.5 nM (CDK4), 3.3 nM (CDK6), 33 nM (BRD4 BD1), 89 nM (BRD4 BD2), 79 nM (PI3Kα), 83 nM (PI3Kδ), 3.18 μM (PI3Kγ) , respectively. SRX3177 blocks the interaction between the SARS-CoV-2 E protein and the BRD2/4 BD1 domain, restores E protein-attenuated NF-κB activity. SRX3177 exerts broad cytotoxic activity against cancer cells. SRX3177 can be used for the study of anti-SARS-CoV-2 and cancer .
|
-
- HY-177277
-
|
|
PI3K
|
Inflammation/Immunology
|
|
HM5023507 is an orally active and selective PI3Kδ/γ inhibitor with IC50s of 4 and 5 μM for PI3Kδ and PI3Kγ over PI3Kβ and PI3Kα. HM5023507 attenuates the PI3Kδ/γ signaling in human basophils. HM5023507 also attenuates the activation and function of human B and T cells and cytokine and IgG production during cocultures, and Th17 differentiation of CD4 T cells. HM5023507 inhibited semiestablished collagen-induced arthritic inflammation in the rat models. HM5023507 can be used for inflammatory diseases like rheumatoid arthritis research .
|
-
- HY-178485
-
|
|
PI3K
HDAC
Akt
Histone Methyltransferase
|
Cancer
|
|
SJY26 is a PI3K/HDAC dual-target inhibitor with IC50s of 0.59 nM (PI3Kα and PI3Kδ), 2.02 nM (PI3Kγ), 12.69 nM (PI3Kβ) and 114 nM (HDAC1). SJY26 exhibits potent broad-spectrum anti-proliferative activity, and is particularly sensitive to Jurkat and PC9R cells. SJY26 inhibited the migration of PC9R cells, arrested the cell cycle and induced cell apoptosis. SJY26 reduces AKT phosphorylation, and decreases histone H3 deacetylation (Ac-H3). SJY26 can be used for the studies of non-small cell lung cancer and leukemia .
|
-
- HY-180261
-
|
|
PROTACs
mTOR
PI3K
Apoptosis
|
Cancer
|
GP262 is a PI3K/mTOR PROTAC degrader targeting PI3Kγ, PI3Kα and mTOR with DC50 values of 42.23 nM, 227.4 nM and 45.4 nM, respectively in MDA-MB-231 cells. GP262 induces degradation of p110α and p110γ with a DC50 of 227.4 and 42.23 nM. GP262 efficient modulates the PI3K/AKT/mTOR pathway, achieving degradation through the ubiquitin-proteasome system (UPS). GP262 also exhibits robust antiproliferative activity and induces apoptosis in vitro. GP262 exhibits tumor growth suppression capability and biosafety profile. GP262 can be used for leukemia and triple-negative breast cancer (TNBC) .
|
-
- HY-120281
-
|
|
MEK
PI3K
Akt
Apoptosis
Caspase
|
Cancer
|
|
ST-168 is an orally active MEK/PI3K inhibitor with an IC50 of 182 nM against MEK1 and IC50 values of 69.2, 41.7, 1482 and 2293 nM against PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ respectively. ST-168 completely inhibits the phosphorylation of ERK1/2 and AKT and induces cancer cell death in a 3D tumor sphere model. ST-168 demonstrates significant antitumor effects in the A375 melanoma mouse model. ST-168 improves the ocular toxicity profile of MEK inhibitors, showing lower caspase activation levels, indicating reduced apoptosis induction. ST-168 can be used in melanoma research .
|
-
- HY-124760
-
|
|
mTOR
PI3K
CDK
|
Cancer
|
|
hSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with an IC50 of <0.05 nM. hSMG-1 inhibitor 11e shows >900-fold selectivity over mTOR (IC50 of 45 nM), PI3Kα/γ (IC50s of 61 nM and 92 nM) and CDK1/CDK2 (IC50s of 32 μM and 7.1 μM) .
|
-
- HY-155232
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3Kδ-IN-16 is a potent and selective PI3Kδ inhibitor with an IC50 value of 0.9 nM. PI3Kδ-IN-16 has a strong anti-proliferative effect on SU-DHL-6 cells, causing cell cycle arrest and inducing apoptosis. PI3Kδ-IN-16 tightly bins to PI3Kδ protein with a planar-shaped conformation. The kinase activity of PI3Kδ-IN-16 which is ~378-fold over PI3Kα, 412-fold over PI3Kβ, and 10-fold over PI3Kγ. PI3Kδ-IN-16 can be used for the study of hematologic malignancies .
|
-
- HY-13514
-
|
|
PI3K
|
Cancer
|
|
TG 100713 is an inhibitor of PI3K, with IC50s of 24, 50, 165, and 215 nM for PI3Kδ, γ, α and β isoforms respectively .
|
-
- HY-113572
-
|
|
PI3K
|
Cancer
|
|
PX-866-17OH is the metabolite of PX-866 (Sonolisib, HY-N6775) and a pan-isoform inhibitor of PI3K with IC50s of 14, 57, 131, and 148 nM against PI3Kα, PI3Kβ, PI3K , and PI3Kδ, respectively .
|
-
- HY-175369
-
|
|
PI3K
Akt
PD-1/PD-L1
Interleukin Related
CD3
|
Inflammation/Immunology
Cancer
|
|
PI3Kδ-IN-25 is an orally active selective PI3Kδ inhibitor (IC50 = 2.1 nM). PI3Kδ-IN-25 has IC50s of 272, 285, and 1171 nM for PI3Kα, PI3Kγ, and PI3Kβ, respectively. PI3Kδ-IN-25 inhibits AKT Ser473 phosphorylation, suppresses Treg cell proliferation, and downregulates PD-L1 expression in B16F10 cells. PI3Kδ-IN-25 exhibits anticancer effects in B16F10 melanoma and Lewis lung cancer mouse models by reducing tumor-infiltrating Treg cells and enhancing immune responses. PI3Kδ-IN-25 is potentially useful in the study of melanoma, lung cancer, and other cancers .
|
-
- HY-112608
-
|
|
PI3K
|
Cancer
|
|
CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells .
|
-
- HY-174461
-
|
|
PROTACs
PI3K
|
Cancer
|
|
PROTAC PI3Kα degrader-1 is a PI3Kα PROTAC degrader (DC50 = 0.08 μM), demonstrating good selectivity for PI3Kα degradation over PI3Kβ, PI3Kγ, and PI3Kδ. PROTAC PI3Kα degrader-1 effectively degrades PI3Kα in a time- and concentration-dependent, over PI3Kβ, PI3Ky and PI3Kδ, and potently inhibited the phosphorylation of AKT at the Ser473site. PROTAC PI3Kα degrader-1 shows significant in vivo anticancer efficacy in HGC-27 and DOHH2 xenograft models. (Pink: PI3Kα ligand : (HY-174798), Blue: E3 ligase CRBN Ligand (HY-10984), Black: Linker, E3 ligase ligand-linker conjugate (HY-W940885)) .
|
-
- HY-128633
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
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PI3K-IN-4 is a potent Pan-PI3K inhibitor. PI3K-IN-4 has high activity for three PI3K isoforms with the IC50 values of picomole. PI3K-IN-4 shows superior inhibitory activity against PI3Kα (IC50 = 0.20 nM), PI3Kβ (IC50 = 2.99 nM), PI3Kδ (IC50 = 0.48 nM) and PI3Kγ (IC50 = 0.58 nM) and has no significant activity against EGFR. PI3K-IN-4 inhibits cancer cell growth though PI3K/Akt signaling pathway, leading to the inhibition of colony formation and the induction of apoptosis. PI3K-IN-4 can be used for lung, colon and breast cancer research .
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- HY-124719
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PI3K
mTOR
GSK-3
CDK
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Cancer
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hSMG-1 inhibitor 11j, a pyrimidine derivative, is a potent and selective inhibitor of hSMG-1, with an IC50 of 0.11 nM. hSMG-1 inhibitor 11j exhibits >455-fold selectivity for hSMG-1 over mTOR (IC50=50 nM), PI3Kα/γ (IC50=92/60 nM) and CDK1/CDK2 (IC50=32/7.1 μM). hSMG-1 inhibitor 11j can be used for the research of cancer .
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- HY-13440
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AMG 511
5 Publications Verification
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PI3K
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Cancer
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AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model .
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- HY-182368
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PI3K
Akt
Apoptosis
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Cancer
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PI3Kα-IN-30 is an orally active, selective PI3Kα inhibitor with an IC50 of 2.8 nM. PI3Kα-IN-30 inhibits cancer cell proliferation, as well as the phosphorylation of Akt (S473) and pS6 (S240/244). PI3Kα-IN-30 shows low growth inhibitory activity against normal somatic cell lines at a concentration of 30 μM. PI3Kα-IN-30 induces cancer cell apoptosis and exerts anti-tumor efficacy in xenograft models. PI3Kα-IN-30 can be used for the research of breast cancer .
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- HY-181581
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PI3K
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Cancer
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IMM-H012 is a specific PI3K inhibitor with an IC50 of 0.80 nM against PI3Kα. IMM-H012 combined with [ 177Lu]Lu-P4 shows synergistic antitumor effects against stomach cancer and lung cancer .
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- HY-181076
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PI3K
CDK
Apoptosis
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Cancer
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FOXM1-IN-3 is a potent FOXM1 inhibitor. FOXM1-IN-3 downregulates FOXM1 expression at protein and mRNA levels, suppressing downstream effectors CCNB1 and CDC25. FOXM1-IN-3 induces G2/M cell cycle arrest and apoptosis in colorectal cancer cells. FOXM1-IN-3 inhibits colony formation and cell migration in colorectal cancer cells. FOXM1-IN-3 targets the cancer stem cell phenotype in colorectal cancer cells, reducing cancer stem cell marker expression. FOXM1-IN-3 reduces tumor growth in a zebrafish xenograft model. FOXM1-IN-3 can be used for the research of colorectal cancer .
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- HY-183787
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PI3K
Akt
mTOR
Apoptosis
CDK
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Cancer
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PI3Kα-IN-33 is an orally active and selective PI3Kα inhibitor with an IC50 of 9.9 nM. PI3Kα-IN-33 blocks the PI3K/Akt/mTOR signaling pathway. PI3Kα-IN-33 induces apoptosis and triggers G2/M-phase arrest via Cyclin B1 and CDK1 downregulation. PI3Kα-IN-33 can be used for the research of colorectal cancer .
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- HY-100424
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PI3K
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Cancer
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PI3K-IN-63 (compound 9) is a PI3Kα inhibitor with a Ki of 0.35 nM against human targets. PI3K-IN-63 inhibits the phosphorylation of AKT at the S473 site in cellular assays. PI3K-IN-63 reduces the viability of non-small cell lung cancer cell lines carrying PIK3CA mutations. PI3K-IN-63 can be used in studies related to non-small cell lung cancer .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P10093
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PI3K
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Others
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Penetratin-PI3Kγ(126-150) is a peptide inhibitor of ΡI3Κγ that plays an important role in respiratory system diseases .
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Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-18085S1
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1 Publications Verification
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Quercetin-d3 is the deuterium labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively .
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- HY-18085S2
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Quercetin- 13C3 is the 13C-labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively .
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- HY-18085S
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Quercetin-d5 is a deuterium labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively .
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- HY-18085AS
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1 Publications Verification
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Quercetin-d3 hydrate is a deuterium labeled Quercetin hydrate (HY-18085A), a flavonoid which can stimulate recombinant SIRT1 and also 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 .
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- HY-10681S
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Gedatolisib-d8 (PKI-587-d8) is the deuterium labeled Gedatolisib (HY-10681). Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2 .
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