PI3K-IN-1

By Targets:	PI3K (15) Antibiotic (1) Apoptosis (3) ATM/ATR (1) c-Fms (1) COX (1) FAK (1) MEK (1) MMP (1) mTOR (2) PARP (1) PERK (1) Src (1)
By Research Areas:	Cancer (14) Infection (1) Inflammation/Immunology (4)

Targets Recommended: PI3K AIM2 NEKs

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12068

*PI3K-IN-1* 5+ Cited Publications XL-147 derivative 1	PI3K	Cancer
PI3K-IN-1 (XL-147 derivative 1) is a potent inhibitor of *PI3K. PI3K-IN-1* (25 μM) blocks PI3K/Akt signaling pathways .

HY-133124

PARP/PI3K-IN-1	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-136806

PI3K-IN-12

PI3K Cancer

PI3K-IN-12 (comp 76) is a PI3K inhibitor .

PI3K-IN-12	PI3K	Cancer
PI3K-IN-12 (comp 76) is a *PI3K* inhibitor .

HY-144692

MEK/PI3K-IN-1	MEK PI3K PERK	Cancer
MEK/PI3K-IN-1 (compound 6r) is a potent *MEK/PI3K* inhibitor, with IC₅₀ values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines .

HY-147911

COX-2/PI3K-IN-1	PI3K COX	Inflammation/Immunology Cancer
COX-2/PI3K-IN-1 (compound 5d) is a potent *PI3K* inhibitor with IC₅₀ value of 1.14 nM. COX-2/PI3K-IN-1 is a selective COX-2 inhibitor with K_i value of 3.24 nM. COX-2/PI3K-IN-1 has anti-inflammatory and anti-cancer properties.

HY-160458

PI3Kα-IN-17

PI3K Others

PI3Kα-IN-17 (example 4) is a potent inhibitor of PI3Kα .
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-18650

KU 59403

ATM/ATR Cancer

KU 59403 is a potent ATM inhibitor, with IC₅₀ values of 3 nM, 9.1 μM and 10 μM for ATM, DNA-PK and PI3K, respectively .
HY-124647

PI3Kα-IN-1

PI3K Cancer

PI3Kα-IN-1 is a PI3Kα inhibitor (IC₅₀ < 0.5 nM), and also inhibits mTOR (IC₅₀: 104 nM) .
HY-145338

PI3Kβ-IN-1

PI3K Cancer

PI3Kβ-IN-1 (compound (P)-14) is a selective and orally active PI3Kβ inhibitor, with an IC₅₀ of 2 nM .
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.

PI3Kα-IN-17	PI3K	Others
PI3Kα-IN-17 (example 4) is a potent inhibitor of *PI3K*α .

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

KU 59403	ATM/ATR	Cancer
KU 59403 is a potent ATM inhibitor, with IC₅₀ values of 3 nM, 9.1 μM and 10 μM for ATM, DNA-PK and PI3K, respectively .

PI3Kα-IN-1	PI3K	Cancer
PI3Kα-IN-1 is a PI3Kα inhibitor (IC₅₀ < 0.5 nM), and also inhibits mTOR (IC₅₀: 104 nM) .

PI3Kβ-IN-1	PI3K	Cancer
PI3Kβ-IN-1 (compound (P)-14) is a selective and orally active PI3Kβ inhibitor, with an IC₅₀ of 2 nM .

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

HY-136512

Streptazolin	Antibiotic	Infection Inflammation/Immunology
Streptazolin is an antibiotic. Streptazolin increases bacterial killing and elaboration of immunostimulatory cytokines by macrophages in vitro. Streptazolin stimulates the macrophage NF-κB pathway via PI3K signaling .

HY-107365

PQR530	PI3K mTOR	Cancer
PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar K_d toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity .

HY-157287

(S)-Phe-A110/B319	Others	Inflammation/Immunology
(S)-Phe-A110/B319 is a selective binde that has 20-fold higher affinity towards the H1047R mutant of p110α in the p110α/p85α *PI3K* complex .

HY-U00326

PI3Kα/mTOR-IN-1	PI3K mTOR	Cancer
PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC₅₀ of 7 nM for PI3Kα in a cell assay, and K_is of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.

HY-158050

PXB17	c-Fms
PXB17 can inhibit CSF1R (IC₅₀ = 1.7 nM) by blocking the activation of PI3K/ AKT/mTORC1 signaling. PXB17 is orally effective. PXB17 significantly inhibits the growth of CRC, improves PD-1 mAb efficacy and reduces tumor recurrence in CRC .

HY-101562

Inavolisib 2 Publications Verification GDC-0077; RG6114	PI3K Apoptosis	Cancer
GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC₅₀=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα .

HY-108418

PI3Kδ-IN-15	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-120213

YH-306	FAK Src PI3K MMP Apoptosis	Cancer
YH-306 is an antitumor agent. YH-306 suppresses colorectal tumour growth and metastasis via FAK pathway. YH-306 significantly inhibits the migration and invasion of colorectal cancer cells. YH-306 potently suppresses uninhibited proliferation and induces cell apoptosis. YH-306 suppresses the activation of FAK, c-Src, paxillin, and PI3K, Rac1 and the expression of MMP2 and MMP9. YH-306 also inhibita actin-related protein (Arp2/3) complex-mediated actin polymerization .

Cat. No.	Product Name

HY-L079

Anti-Blood Cancer Compound Library	2676 compounds
Blood cancers, also called hematologic cancers, occur when abnormal blood cells start growing out of control, interrupting the function of normal blood cells, which fight off infection and produce new blood cells. Most blood cancers start in the bone marrow, which is where blood is produced. There are three main types of blood cancers: leukemia, lymphoma and myeloma, which afflict millions of children and adults every year, and are often deadly. Some common blood cancer treatments include stem cell transplantation, chemotherapy, radiation therapy, targeted therapy, immunotherapy or a combination thereof. As we begin to understand the key signaling pathways and molecular drivers of malignant transformation in haematological disorders, new treatment strategies will continue to be developed. MCE offers a unique collection of 2676 compounds with identified and potential anti-blood cancer activity. These compounds target blood cancer’s major targets and signaling pathways. MCE anti-blood cancer compound library is a useful tool for anti-blood cancer drugs screening and other related research.

Anti-Blood Cancer Compound Library

2676 compounds

Blood cancers, also called hematologic cancers, occur when abnormal blood cells start growing out of control, interrupting the function of normal blood cells, which fight off infection and produce new blood cells. Most blood cancers start in the bone marrow, which is where blood is produced. There are three main types of blood cancers: leukemia, lymphoma and myeloma, which afflict millions of children and adults every year, and are often deadly.

Some common blood cancer treatments include stem cell transplantation, chemotherapy, radiation therapy, targeted therapy, immunotherapy or a combination thereof. As we begin to understand the key signaling pathways and molecular drivers of malignant transformation in haematological disorders, new treatment strategies will continue to be developed.

MCE offers a unique collection of 2676 compounds with identified and potential anti-blood cancer activity. These compounds target blood cancer’s major targets and signaling pathways. MCE anti-blood cancer compound library is a useful tool for anti-blood cancer drugs screening and other related research.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-136512

Streptazolin	Structural Classification Microorganisms Anti-inflammation/Immunoregulatory Classification of Application Fields Antibiotics Source classification Antibacterial Disease Research Inflammation/Immunology Disease Research Fields Other Antibiotics	Antibiotic
Streptazolin is an antibiotic. Streptazolin increases bacterial killing and elaboration of immunostimulatory cytokines by macrophages in vitro. Streptazolin stimulates the macrophage NF-κB pathway via PI3K signaling .

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