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Pakt Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (7) Apoptosis (6) Autophagy (1) Caspase (1) EGFR (3) FAK (1) Ferroptosis (2) Glutaminase (1) HCV (2) HSP (1) MEK (2) mTOR (5) Nucleoside Antimetabolite/Analog (1) Parasite (2) PERK (2) PI3K (6) Ras (2) SHP2 (1) Src (1) TAM Receptor (2)
By Research Areas:	Cancer (27) Cardiovascular Disease (2) Infection (2) Inflammation/Immunology (1) Neurological Disease (3)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

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Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0789

SU6656 Maximum Cited Publications 12 Publications Verification	Src FAK Akt	Cancer
SU6656 is a Src family kinases inhibitor with IC₅₀s of 280, 20, 130, 170 nM for Src, Yes, Lyn, and Fyn, respectively. SU6656 inhibits FAK phosphorylation at Y576/577, Y925, Y861 sites. SU6656 also inhibits p-AKT.

HY-153663

TH-Z827	Ras	Cancer
TH-Z827 is a mutant selective KRAS(G12D) inhibitor with an IC₅₀ of 2.4 μM. TH-Z827 does not bind KRAS(WT) or KRAS(G12C). TH-Z827 blocked the KRAS(G12D)-CRAF interaction with an IC₅₀ value of 42 μM .

HY-162141

MD102	Glutaminase Apoptosis	Cancer
MD102 is a potent TG2 inhibitor with an IC₅₀ value of 0.35 μM. MD102 stabilizes p53 by inhibiting TG2, inducing a decrease in p-AKT and p-mTOR downstream signaling, leading to tumor cell apoptosis .

HY-111370

mTOR inhibitor-2	mTOR	Cancer
mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC₅₀ of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates .

HY-157413

YS-67	EGFR	Cancer
YS-67 is a potent inhibitor of EGFR with an IC ₅₀ of 5.2 nM. YS-67 significantly inhibits p-EGFR and *p-AKT. YS-67 inhibits* the proliferation of A549, PC-9, and A431cells with IC ₅₀s of 4.1, 0.5, and 2.1 μM, respectively .

HY-102071

KIN59 5'-O-Tritylinosine; 5'-O-Trityl-inosine	Nucleoside Antimetabolite/Analog	Cancer
KIN59 (5’-O-Tritylinosine) is a potent thymidine phosphorylase allosteric inhibitor. KIN59 inhibits FGF2-stimulated cell growth. KIN59 inhibits the expression of p-FGFR1, P-Akt in FGF2 (10 ng/mL) stimulated cells. KIN59 shows anti-tumor activity .

HY-155098

CNBCA	SHP2	Cancer
CNBCA is a potent, selective, competitive SHP2 enzyme inhibitor, with the IC₅₀ of 0.87 μM. CNBCA binds to full-length SHP2 and inhibits enzyme activity. CNBCA inhibits pAkt and pERK1/2, and the cell growth of BT474 and MDA-MB468 cells. CNBCA can be used for breast cancer study .

HY-152075

AXL-IN-14	TAM Receptor	Cancer
AXL-IN-14 is a potent and orally active AXL inhibitor with an IC₅₀ value of 0.8 nM. AXL-IN-14 inhibits Gas6/AXL-mediated cell migration and invasion. AXL-IN-14 decreases the expression of p-AXL and p-AKT proteins. AXL-IN-14 shows anti-tumor activity .

HY-B0094

Artemisinin 10+ Cited Publications Qinghaosu; NSC 369397	HCV Parasite Akt Ferroptosis	Infection Neurological Disease Cancer
Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing *pAKT* in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .

HY-162112

KRB-456	Ras	Cancer
KRB-456 is a small molecule that binds a dynamic allosteric binding pocket within the switch-I/II region of KRAS G12D. KRB-456 inhibits P-MEK, P-AKT, and P-S6 levels in vivo and inhibits the growth of cancer. KRB-456 can be used for the research of pancreatic cancer .

HY-139296

PP2A Cancerous-IN-1	Akt	Cancer
PP2A Cancerous-IN-1 is a strong and potent CIP2A (Cancerous inhibitor of PP2A) and *p-Akt* inhibitor. PP2A Cancerous-IN-1 shows the most potent antiproliferative activities . PP2A Cancerous-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-147513

AKT-IN-12	Akt Apoptosis	Cancer
AKT-IN-12 (compound 3e) is a potent Akt kinase inhibitor with an IC₅₀ value of 0.55 μM. AKT-IN-12 induces G0/G1 cell cycle arrest and apoptosis. AKT-IN-12 also inhibits p-AKT, p-ERK, and activates p-JNK, JNK. AKT-IN-12 can be used for researching leukemia .

HY-149092

Anticancer agent 109	TAM Receptor	Cancer
Anticancer agent 109 (compound 6-15) is an inhibitor of the Gas6-Axl axis with anti-cancer activity. Anticancer agent 109 inhibits the expression of Gas6 and Axl, and the expression p-PI3K and p-AKT in cancer cells, leads to G1 phase arrest and promotes cancer cells apoptosis, and inhibits tumor growth significantly in nude mouse tumor bearing models .

HY-B0094S

Artemisinin-d3 Qinghaosu-d₃; NSC 369397-d₃	Akt Ferroptosis HCV Parasite	Infection Neurological Disease Cancer
Artemisinin-d₃ is the deuterium labeled Artemisinin. Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants[1]. Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects[2].

HY-161373

PI3Kα-IN-22	PI3K	Cancer
PI3Kα-IN-22 (Compound 17) is an orally active, potent and selective inhibitor of PI3Kα ^H1047R, with an IC₅₀ of 1 nM for pAKT T47D AlphaLISA. PI3Kα-IN-22 can induce tumor regressions in the HCC1954 tumor model in mice .

HY-N0265

Asperosaponin VI 1 Publications Verification	Caspase Apoptosis	Cardiovascular Disease
Asperosaponin VI, A saponin component from Dipsacus asper, induces osteoblast differentiation through BMP‐2/p38 and ERK1/2 pathway . Asperosaponin Ⅵ inhibits apoptosis in hypoxia-induced cardiomyocyte by increasing the Bcl-2/Bax ratio and decreasing active caspase-3 expression, as well as enhancing of p-Akt and p-CREB .

HY-13440

AMG 511 2 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 PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model .

HY-132168

RMC-5552	mTOR	Cancer
RMC-5552 is a potent and selective mTORC1 inhibitor. RMC-5552 inhibits phosphorylation of mTORC1 pS6K and p4EBP1 with IC₅₀s of 0.14 nM and 0.48 nM, respectively. RMC-5552 shows much lower pAKT inhibition (IC₅₀ of 19 nM), resulting in mTORC1/mTORC2 selectivity approaching 40-fold. RMC-5552 has anti-cancer activity .

HY-124798

Rheb inhibitor NR1 1 Publications Verification	mTOR	Neurological Disease Inflammation/Immunology Cancer
Rheb inhibitor NR1 is a Rheb inhibitor with an IC₅₀ of 2.1 µM in the Rheb-IVK assay. Rheb inhibitor NR1 can directly bind Rheb in the switch II domain and selectively inhibit the activation of mechanistic target of rapamycin complex 1 (mTORC1). Rheb inhibitor NR1 inhibits the phosphorylation of mTORC1 driven ^T389pS6K1 and increases the phosphorylation of ^S473pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influence mTORC2 activity . ^{(Rheb-IVK: Rheb-dependent mTORC1 kinase activity)}

HY-113916

Onalespib lactate AT13387 lactate	HSP	Cancer
Onalespib lactate is a potent and cross the blood-brain barrier heat-shock-protein-90 (Hsp90) inhibitor with an K_d value of 0.71 nM. Onalespib lactate inhibits the proliferation, survival and migration. Onalespib lactate decreases the expression of EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, P-S6 protein. Onalespib lactate shows antitumor activity. Onalespib lactate has the potential for the research of non-small cell lung cancer (NSCLC) .

HY-134903

(32-Carbonyl)-RMC-5552	mTOR	Cancer
(32-Carbonyl)-RMC-5552 is a potent mTOR inhibitor. (32-Carbonyl)-RMC-5552 inhibits mTORC1 and mTORC2 substrate (p-P70S6K-(T389), p-4E-BP1-(T37/36), AND p-AKT1/2/3-(S473)) phosphorylation with pIC₅₀s of > 9, >9 and between 8 and 9, respectively (patent WO2019212990A1, example 2) .

HY-145931

CC214-2	mTOR Autophagy	Cancer
CC214-2 is an oral active and selective mTOR kinase inhibitor. CC214-2 targets to both of mTORC1 (pS6) and mTORC2 (pAktS473). CC214-2 induces autophagy, which is a potential target for host-directed therapy (HDT) in tuberculosis. CC214-2 exhibits synergistic bactericidal and sterilizing activity agasinst tuberculosis (TB), and shortens the treatment duration. CC214-2 also inhibits Rapamycin (HY-10219)-resistant signaling and the growth of glioblastomas in vitro and in vivo .

HY-132231

FD223	PI3K Apoptosis	Cancer
FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC₅₀=1 nM) and good selectivity over other isoforms (IC₅₀s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML .

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-144693

MEK/PI3K-IN-2	MEK PI3K PERK	Cancer
MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC₅₀ values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines .

HY-156080

PI3K-IN-48	PI3K Akt	Cancer
PI3K-IN-48 is a PI3K inhibitor with IC₅₀ value of 1.55 ± 0.18 μM for A549 cells. PI3K-IN-48 can induce G0/G1 phase arrest, cell apoptosis, and down-regulate expression of p-PI3K and p-Akt. PI3K-IN-48 can be used for human lung cancers diseases research .

HY-108052

Delphinidin 3-glucoside chloride Delphinidin 3-O-glucoside chloride; Delphinidin 3-O-β-glucoside chloride	EGFR Apoptosis Akt	Cardiovascular Disease Cancer
Delphinidin 3-glucoside chloride (Delphinidin 3-O-glucoside chloride) is an active anthocyanin found in Hibiscus sabdariffa extract. Delphinidin 3-glucoside chloride induces a pro-apoptotic effect in B cell chronic lymphocytic leukaemia (B CLL) . Delphinidin 3-glucoside chloride exerts phytoestrogen activity by binding to ERβ, with an IC₅₀ of 9.7 μM . Delphinidin-3-O-glucoside chloride inhibits EGFR with an IC₅₀ of 2.37 µM . Delphinidin 3-glucoside chloride exhibits antitumor effects through pAKT/IRF1/HOTAIR pathway. Delphinidin 3-glucoside chloride exhibits efficacy against oxidative stress, inhibits platelet activation and endothelial dysfunction .

HY-149824

EGFR T790M/L858R-IN-2	EGFR Apoptosis	Cancer
EGFRT790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC₅₀ values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively. EGFRT790M/L858R-IN-2 decreases the expression of p-EGFR, P-AKT, P-ERK1/2. EGFRT790M/L858R-IN-2 induces Apoptosis and cell cycle arrest in the G1 phase. EGFRT790M/L858R-IN-2 shows anti-cancer activity .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B0094

Artemisinin 10+ Cited Publications Qinghaosu; NSC 369397	Infection Structural Classification Piscidia erythrina L. Neurological Disease Classification of Application Fields Terpenoids Sesquiterpenes Source classification Plants Compositae Disease Research Fields	HCV Parasite Akt Ferroptosis
Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants . Artemisinin inhibits AKT signaling pathway by decreasing *pAKT* in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects .

HY-N0265

Asperosaponin VI 1 Publications Verification	Cardiovascular Disease Triterpenes Classification of Application Fields Terpenoids Dipsacaceae Source classification Plants Dipsacus asper Disease Research Fields	Caspase Apoptosis
Asperosaponin VI, A saponin component from Dipsacus asper, induces osteoblast differentiation through BMP‐2/p38 and ERK1/2 pathway . Asperosaponin Ⅵ inhibits apoptosis in hypoxia-induced cardiomyocyte by increasing the Bcl-2/Bax ratio and decreasing active caspase-3 expression, as well as enhancing of p-Akt and p-CREB .

HY-108052

Delphinidin 3-glucoside chloride Delphinidin 3-O-glucoside chloride; Delphinidin 3-O-β-glucoside chloride	Malvaceae Structural Classification Anthocyans Flavonoids Microorganisms Classification of Application Fields Hibiscus sabdariffa Linn. Source classification Plants Disease Research Fields Cancer	EGFR Apoptosis Akt
Delphinidin 3-glucoside chloride (Delphinidin 3-O-glucoside chloride) is an active anthocyanin found in Hibiscus sabdariffa extract. Delphinidin 3-glucoside chloride induces a pro-apoptotic effect in B cell chronic lymphocytic leukaemia (B CLL) . Delphinidin 3-glucoside chloride exerts phytoestrogen activity by binding to ERβ, with an IC₅₀ of 9.7 μM . Delphinidin-3-O-glucoside chloride inhibits EGFR with an IC₅₀ of 2.37 µM . Delphinidin 3-glucoside chloride exhibits antitumor effects through pAKT/IRF1/HOTAIR pathway. Delphinidin 3-glucoside chloride exhibits efficacy against oxidative stress, inhibits platelet activation and endothelial dysfunction .

Cat. No.	Product Name	Chemical Structure

HY-B0094S

Artemisinin-d3
Artemisinin-d₃ is the deuterium labeled Artemisinin. Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants[1]. Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects[2].

Artemisinin-d3

Artemisinin-d₃ is the deuterium labeled Artemisinin. Artemisinin (Qinghaosu), a sesquiterpene lactone, is an anti-malarial agent isolated from the aerial parts of Artemisia annua L. plants[1]. Artemisinin inhibits AKT signaling pathway by decreasing pAKT in a dose-dependent manner. Artemisinin reduces cancer cell proliferation, migration, invasion, tumorigenesis and metastasis and has neuroprotective effects[2].

PP2A Cancerous-IN-1		Alkynes
PP2A Cancerous-IN-1 is a strong and potent CIP2A (Cancerous inhibitor of PP2A) and *p-Akt* inhibitor. PP2A Cancerous-IN-1 shows the most potent antiproliferative activities . PP2A Cancerous-IN-1 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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