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Isoforms Recommended:	PI3Kδ

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PI3Kδ

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By Targets:	Akt (5) Apoptosis (11) Autophagy (1) Bcl-2 Family (1) Caspase (1) CD3 (1) Cytochrome P450 (1) Drug Isomer (1) Epigenetic Reader Domain (1) G Protein-coupled Receptor Kinase (GRK) (1) HDAC (1) Histone Methyltransferase (1) Interleukin Related (1) Lipase (1) Microtubule/Tubulin (1) mTOR (5) PD-1/PD-L1 (1) PI3K (53) PROTACs (1) Reactive Oxygen Species (ROS) (1)
By Research Areas:	Cancer (42) Infection (1) Inflammation/Immunology (13)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-155232

PI3Kδ-IN-16	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-108418

PI3Kδ-IN-15 1 Publications Verification	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-122593

PI3Kδ-IN-5	PI3K	Cancer
PI3Kδ-IN-5 (compound 7n) is a highly potent and selective inhibitor of PI3Kδ with an IC₅₀ of 0.9 nM .

HY-15288

PI3kδ inhibitor 1	PI3K	Cancer
PI3kδ inhibitor 1 is a potent and selective PI3Kδ inhibitor with an IC₅₀ of 3.8 nM.

HY-134472

PI3Kδ-IN-8	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-125376

PI3Kδ-IN-3	PI3K	Cancer
PI3Kδ-IN-3 (Compound 11) is a **PI3Kδ inhibitor (IC₅₀*: 9 nM). PI3Kδ-IN-3 inhibits B cell function. PI3Kδ-IN-3 has good pharmacokinetic properties .***

HY-144254

PI3Kδ-IN-10	PI3K Akt Apoptosis	Cancer
PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor with IC₅₀ of 2 nM. PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis in hepatocellular carcinoma models .

HY-143472

PI3Kδ-IN-11	PI3K Akt Apoptosis	Cancer
PI3Kδ-IN-11 is a highly potent and selective PI3Kδ inhibitor with IC₅₀ value of 27.5 nM. PI3Kδ-IN-11 dose-dependently blocks the activity of *PI3K/Akt* pathway. PI3Kδ-IN-11 can be used for researching B or T cell-related malignancies .

HY-142646

PI3Kδ-IN-9	PI3K	Cancer
PI3Kδ-IN-9 is a selective PI3Kδ inhibitor with an IC₅₀ value of 3.8 nM.

HY-162647

PI3Kδ-IN-22	PI3K	Inflammation/Immunology
PI3Kδ-IN-22 (Compound 26) is a selective inhibitor for PI3Kδ with pK_i of 9.3. PI3Kδ-IN-22 inhibits PI3Kδ-AKT signaling pathway in THP-1 cells, with pIC₅₀ of 9.4. PI3Kδ-IN-22 exhibits good pharmacokinetic characters in rats .

HY-149634

PI3Kδ-IN-17	PI3K	Cancer
PI3Kδ-IN-17 (Compound S5) is a potent inhibitor of *PI3Kδ, with IC₅₀* of 2.82?nM. PI3Kδ-IN-17 shows strong inhibitory activity of proliferation in SU-DHL-6 cells (IC₅₀ = 0.035 μM) .

HY-158147

PI3Kδ-IN-20	PI3K	Cancer
PI3Kδ-IN-20 (compound (S)-36) is a potent inhibitor of PI3Kδ, with the IC₅₀ of 6.4 nM. PI3Kδ-IN-20 has oral bioactivity. PI3Kδ-IN-20 shows significant suppression of cell proliferation and remarkable induction of apoptosis both in vitro and in vivo .

HY-149235

PI3Kδ-IN-12	PI3K	Inflammation/Immunology
PI3Kδ-IN-12 (compound 13) is a PI3Kδ inhibitor (pIC₅₀ = 5.8), with pKi values of 8.0/6.5/6.4/6.7 for PI3Kδ/γ/β/α, respectively. PI3Kδ-IN-12 can be used in the study of chronic respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD) .

HY-175369

PI3Kδ-IN-25	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-155833

PI3Kδ-IN-13	PI3K	Infection Inflammation/Immunology Cancer
PI3Kδ-IN-13 (compound 89) is a PI3Kδ inhibitor (IC₅₀=2.6 nM). PI3Kδ-IN-13 can be used in the research of cell proliferation diseases such as cancer, infection, inflammation and autoimmune diseases .

HY-158688

PI3Kδ-IN-21	PI3K	Inflammation/Immunology
PI3Kδ-IN-21 (Compound 31) is a selective inhibitor for phosphoinositide 3-kinases δ (PI3Kδ), with an IC₅₀ of 13.6 nM. PI3Kδ-IN-21 inhibits proliferation and differentation of T cells through PI3K/AKT/mTOR signaling pathway. PI3Kδ-IN-21 exhibits good pharmacokinetic characters in rat model, and attenuates the experimental autoimmune encephalomyelitis in myelin oligodendrocyte glycoprotein (MOG)-induced EAE model .

HY-157128

PI3Kδ-IN-18	PI3K	Inflammation/Immunology
Se15 is a selective inhibitor of **PI3Kδ with an IC₅₀ value less than 0.1nM. Se15 can be used in research on autoimmune .**

HY-175002

PI3Kδ-IN-24	PI3K Akt Apoptosis	Cancer
PI3Kδ-IN-24 is a selective PI3Kδ inhibitor (IC₅₀ = 0.1 nM). PI3Kδ-IN-24 exhibits significant antiproliferative effects against PI3Kδ-overexpressing cancer cell lines. PI3Kδ-IN-24 reduces p-AKT levels and induces cell cycle arrest and apoptosis in tumor cells. PI3Kδ-IN-24 is useful in cancer research, such as diffuse large B-cell lymphoma (DLBCL) .

HY-169983

PI3Kδ-IN-23	PI3K	Cancer
PI3Kδ-IN-23 (compound A11) is a potent inhibitor of PI3Kδ, with the IC₅₀ of 0.27 nM. PI3Kδ-IN-23 bounds to PI3Kδ by covalent-bonding interactions with Lys779. PI3Kδ-IN-23 plays an important role in cancer research .

HY-101921

PI3Kδ-IN-1	PI3K	Inflammation/Immunology
PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC₅₀ of 1.7 nM.

HY-155975

PI3Kδ-IN-14	PI3K	Inflammation/Immunology
PI3Kδ-IN-14 (Compound (S)-29) is a selective PI3Kδ inhibitor (IC₅₀: 0.8 nM, K_d: 84.8 nM). PI3Kδ-IN-14 binds to the ATP-binding site of the kinase domain of PI3Kδ. PI3Kδ-IN-14 has anti-inflammatory activity by inhibiting the PI3K/AKT pathway. PI3Kδ-IN-14 ameliorates acute lung injury (ALI) .

HY-172130

PI3Kδ/BET-IN-1	PI3K Epigenetic Reader Domain	Cancer
PI3Kδ/BET-IN-1 (compound 10b) shows excellent and balanced activities against PI3Kδ (IC₅₀ = 112 nM) and BRD4-BD1 (IC₅₀ = 19 nM) and exhibits strong antiproliferative activities in DLBCL cells .

HY-144993

PI3Kδ/γ-IN-1	PI3K	Cancer
PI3Kδ/γ-IN-1 is a potent, selective *PI3K-δ/γ* inhibitor for research of hematological malignancies.

HY-150638

PI3Kδ/γ-IN-3	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-146789

PI3Kδ/γ-IN-2	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-174396

PI3Kδ/HDAC6-IN-1	PI3K HDAC Bcl-2 Family Caspase Reactive Oxygen Species (ROS) Apoptosis Histone Methyltransferase Microtubule/Tubulin	Cancer
PI3Kδ/HDAC6-IN-1 (Compound 22E) is an orally active and dual inhibitor of PI3Kδ and HDAC6 with IC₅₀ values of 2.4 nM and 6.2 nM, respectively. PI3Kδ/HDAC6-IN-1 exhibits potent antiproliferative effects on non-Hodgkin lymphoma (NHL) cells and possesses in vivo antitumor activity without significant toxicity. PI3Kδ/HDAC6-IN-1 arrests the cell cycle at the G0/G1 phase and induces apoptosis. PI3Kδ/HDAC6-IN-1 blocks the PI3K/AKT/mTOR signaling pathway and increases the acetylation levels of α-tubulin and histone H3 .

HY-176239

*PROTAC PI3Kδ degrader-1*	PROTACs PI3K Akt Apoptosis Autophagy	Cancer
PROTAC PI3Kδ degrader-1 is a Lysine-targeted covalent PI3Kδ PROTAC degrader with a DC₅₀ of 3.98 nM. PROTAC PI3Kδ degrader-1 has a potent antiproliferative activity and selective PI3Kδ inhibition (IC₅₀: 8 nM). PROTAC PI3Kδ degrader-1 also significantly degrades p-AKT, induces cell cycle arrest in G1 phase and prompts cell apoptosis and autophagy. PROTAC PI3Kδ degrader-1 effectively inhibits the tumor growth in SU-DHL-6 xenograft mice model . Pink: PI3Kδ ligand (HY-169983); Blue: VHL ligase ligand (HY-112078); Black: linker (HY-W013381)

HY-147898

PI3K-IN-33	PI3K Apoptosis	Cancer
PI3K-IN-33 (Compound 6e) is a highly selective *PI3K* inhibitor with IC₅₀ values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-33 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-33 can be used in leukemia research .

HY-147899

PI3K-IN-34	PI3K Apoptosis	Cancer
PI3K-IN-34 (Compound 6g) is a highly selective *PI3K* inhibitor with IC₅₀ values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-34 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-34 can be used in leukemia research .

HY-147900

PI3K-IN-35	PI3K Apoptosis	Cancer
PI3K-IN-35 (Compound 6l) is a highly selective *PI3K* inhibitor with IC₅₀ values of 13.98, 7.22 and 10.94 μM for PI3K-α、PI3K-β and PI3K-δ, respectively. PI3K-IN-35 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-35 can be used in leukemia research .

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-11080A

PKI-179 hydrochloride 1 Publications Verification	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-131910A

*(R)-IHMT-PI3Kδ-372*	PI3K	Inflammation/Immunology
(R)-IHMT-PI3Kδ-372 (R-18) is a potent and selective PI3Kδ inhibitor with an IC₅₀ of 19 nM. (R)-IHMT-PI3Kδ-372 (R-18) can be used in chronic obstructive pulmonary disease (COPD) research .

HY-131910

*IHMT-PI3Kδ-372*	PI3K Cytochrome P450	Inflammation/Immunology
IHMT-PI3Kδ-372 is a potent and selective PI3Kδ inhibitor with an IC₅₀ of 14 nM. IHMT-PI3Kδ-372 shows high selectivity over other class I PI3Ks (56～83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research .

HY-108418A

*(R)-PI3Kδ-IN-15*	Drug Isomer PI3K	Cancer
(R)-PI3Kδ-IN-15 is the R-enantiomer of PI3Kδ-IN-15 (HY-108418) .

HY-109029

Dezapelisib INCB040093	PI3K	Cancer
Dezapelisib (NCB040093) is a potent inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ). Dezapelisib is a promising research strategy for select R/R B-cell lymphomas .

HY-15280

GSK2292767	PI3K	Inflammation/Immunology
GSK2292767 is a potent and selective inhibitor of PI3Kδ, with a pIC₅₀ of 10.1. GSK2292767 showing greater than 500-fold selective over the other PI3K isoforms. GSK2292767 can be used for the research of respiratory disease .

HY-100694

GS-9901	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 .

HY-147792

WNY1613	PI3K Apoptosis	Cancer
WNY1613 is a potent and selective PI3Kδ inhibitor with piperazinone-containing purine scaffold. WNY1613 induces cancer cell apoptosis and inhibits the phosphorylation of PI3K downstream components in NHL cell lines. WNY1613 exhibits anti-NHL activity in vitro and in vivo .

HY-109068A

Parsaclisib hydrochloride INCB050465 hydrochloride; IBI-376 hydrochloride	PI3K	Cancer
Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC₅₀ of 1 nM at 1 mM ATP. Parsaclisib hydrochloride shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib hydrochloride can be used for the research of relapsed or refractory B-cell malignancies ^[3].

HY-109068

Parsaclisib 1 Publications Verification INCB050465; IBI-376	PI3K	Cancer
Parsaclisib (INCB050465) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC₅₀ of 1 nM at 1 mM ATP. Parsaclisib shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib can be used for the research of relapsed or refractory B-cell malignancies ^[3].

HY-131345A

(S)-PI3Kα-IN-4	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 .

HY-13514

TG 100713 2 Publications Verification	PI3K	Cancer
TG 100713 is an inhibitor of *PI3K, with IC₅₀s of 24, 50, 165, and 215 nM for PI3*Kδ, γ, α and β isoforms respectively .

HY-143403

PI3K-IN-31	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-113572

PX-866-17OH	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-101798

MDVN1003	PI3K	Cancer
MDVN1003 is a Bruton's tyrosine kinase (BTK) and phosphatidylinositol-3-kinase delta (PI3Kδ) dual inhibitor which prevents the activation of B cells and inhibits the phosphorylation of protein kinase B (AKT) and extracellular signal-regulated kinase 1/2 (ERK 1/2). MDVN1003 can be used for non-Hodgkin’s lymphoma (NHL) research .

HY-143404

PI3K-IN-30 1 Publications Verification	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 .

HY-128333

PI3K/mTOR Inhibitor-4	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

GNE-490	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-13440

AMG 511 3 Publications Verification	PI3K	Cancer
AMG 511 is a potent and orally available pan inhibitor of class I *PI3Ks, with K_is of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3*K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model .

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PI3Kδ

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