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Pathways Recommended:	PROTAC PI3K/Akt/mTOR

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PROTAC AKT degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (25) Ligands for Target Protein for PROTAC (1) PROTAC Linkers (1) Apoptosis (10) Autophagy (1) Bcl-2 Family (3) Btk (1) c-Myc (2) Cannabinoid Receptor (1) Caspase (1) CDK (2) Checkpoint Kinase (Chk) (1) E3 Ligase Ligand-Linker Conjugates (5) EGFR (2) ERK (6) FAK (1) FGFR (1) FLT3 (1) HIF/HIF Prolyl-Hydroxylase (1) MEK (1) mTOR (3) Na+/K+ ATPase (1) NF-κB (1) P-glycoprotein (1) p38 MAPK (1) PDK-1 (1) PI3K (5) PIN1 (1) PROTACs (27) Ras (1) Reactive Oxygen Species (ROS) (2) Sirtuin (1) STAT (1)
By Research Areas:	Cancer (34) Inflammation/Immunology (5)
Click Chemistry:	PROTAC Synthesis (1) Alkynes (1)

Inhibitors & Agonists

Click Chemistry

Targets Recommended: Akt PROTAC-Linker Conjugates for PAC PROTAC Linkers Ligands for Target Protein for PROTAC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-148273

Setidegrasib ASP-3082; KRAS G12D inhibitor 17	PROTACs Ras ERK Akt	Cancer
Setidegrasib (KRAS G12D inhibitor 17, ASP3082) is a *PROTAC* KRAS degrader (DC₅₀: 37 nM). Setidegrasib induces the degradation of G12D-mutation KRAS protein. Setidegrasib suppresses p-ERK, *p-AKT, p-S6* levels in AsPC-1 cells. Setidegrasib exhibits anti-tumor activity in various cancer xenograft models in mice. Setidegrasib can be used for the study of KRAS(G12D)-mutated solid tumors. (Blue: VHL ligase ligand (HY-168699); Black: linker (HY-168698); Pink: G12D ligand (HY-168700)) .

HY-133120

INY-03-041 1 Publications Verification	PROTACs Akt	Cancer
INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive *AKT* inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 inhibits *AKT1, AKT2* and *AKT3* with IC₅₀s of 2.0, 6.8 and 3.5 nM, respectively .

HY-141807

MS21	PROTACs Akt	Cancer
MS21 is an effective **AKT PROTAC** degrader. MS21 can inhibit mutations in the PI3K/PTEN pathway, suppress the proliferation and induce cell cycle arrest of tumor cells. MS21 has anti-tumor activity. (Pink: AKT ligand-2 (HY-48682); Black: Linker (HY-W014125); Blue: (S,R,S)-AHPC (HY-125845)) .

HY-168555

YJ1206	PROTACs CDK Apoptosis Akt mTOR	Cancer
YJ1206 is an orally active selective CDK12/CDK13 PROTAC degrader. YJ1206 induces DNA damage and genomic instability, activates the *AKT* pathway, and triggers apoptosis. YJ1206 reduces tumor cell viability, inhibits tumor growth, and attenuates tumor cell dissemination. YJ1206 is applicable to research related to prostate cancer and high-grade serous tubo-ovarian cancer .

HY-145282

MS170 1 Publications Verification	PROTACs Akt	Cancer
MS170 is a potent and selective **PROTAC AKT** degrader. MS170 depletes cellular total *AKT* (T-AKT) with the DC₅₀ value of 32 nM. MS170 binds to AKT1, AKT2, and AKT3 with K_ds of 1.3 nM, 77 nM, and 6.5 nM, respectively .

HY-151613A

MS15 TFA	PROTACs Akt	Cancer
MS15 TFA is a potent and selective **AKT PROTAC** degrader. MS15 TFA inhibits the AKT1, -2, and -3 activities, with IC₅₀ values of 798 nM, 90 nM, and 544 nM, respectively .

HY-133120A

INY-03-041 trihydrochloride 1 Publications Verification	PROTACs Akt	Cancer
INY-03-041 trihydrochloride is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive *AKT* inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003). INY-03-041 trihydrochloride inhibits *AKT1, AKT2* and *AKT3* with IC₅₀s of 2.0, 6.8 and 3.5 nM, respectively .

HY-177008

PROTAC HER2 degrader-1	PROTACs EGFR Apoptosis Akt ERK	Cancer
PROTAC HER2 degrader-1 is a highly selective HER2 *PROTAC* degrader, with a DC₅₀ of 69 nM and a D_max of 96%. PROTAC HER2 degrader-1 inhibits HER2-positive cell proliferation and tumor growth through persistent HER2 degradation and potent inhibition of downstream pathways (AKT and ERK). PROTAC HER2 degrader-1 induces apoptosis in BT-474 cells. PROTAC HER2 degrader-1 can be used for research of HER2-positive cancers. (Pink: HER2 ligand: (HY-177009); Black: Linker; Blue: CRBN ligand: (HY-W023573) .

HY-143883

MS143	PROTACs Akt	Cancer
MS143 is a potent PROTAC *AKT* degrader (DC₅₀=46 nM and GI₅₀=0.8 μM in PC3 cells). MS143 induces rapid and robust AKT degradation in a concentration- and time-dependent manner via hijacking the ubiquitin-proteasome system. MS143 can suppress cancer cell growth (Pink: AKT ligand (HY-15431); Blue: E3 ligase ligand (HY-125845); Black: linker) .

HY-174461

PROTAC PI3Kα degrader-1	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-154860

PTD10	PROTACs Btk Apoptosis Caspase Bcl-2 Family NF-κB Akt	Inflammation/Immunology Cancer
PTD10 is a selective and potent BTK *PROTAC* degrader (DC₅₀ = 0.5 nM, K_D = 2.28 nM). PTD10 can recruit cereblon (CRBN) E3 ligase and form a ternary complex with BTK, thereby mediating the ubiquitination and proteasome-dependent degradation of BTK. PTD10 inhibits cancer cells proliferation, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 potently inhibits the BCR, *AKT* and NF-κB signaling pathway. PTD10 can be used for researches of B-cell malignancies and autoimmune disease .

HY-133487B

(S,R,S)-AHPC-C8-NH2 VH032-C8-NH2	E3 Ligase Ligand-Linker Conjugates	Inflammation/Immunology Cancer
(S,R,S)-AHPC-C8-NH2 (VH032-C8-NH2) is a synthesized?E3 ligase ligand-linker conjugate?that incorporates the VH032 based VHL ligand and a linker used for *AKT* PROTAC degrader. (S,R,S)-AHPC-C8-NH2 is XF038-164A, example 8, extracted from patent WO2019173516A1 .

HY-151613

MS15	PROTACs Akt	Cancer
MS15 is a potent and selective **AKT PROTAC** degrader. MS15 inhibits the AKT1, -2, and -3 activities, with IC₅₀ values of 798 nM, 90 nM, and 544 nM, respectively .

HY-W998345

SMART1	PROTACs PDK-1 Akt	Cancer
SMART1 is a highly specific and CRBN-dependent *PROTAC* that can effectively degrade Smurf1. SMART1 can block the *PDK1-Akt* signaling pathway in KRAS mutant colorectal cancer. SMART1 can inhibit tumor growth in KRAS mutant colorectal cancer (CRC) xenograft models.(Blue: CRBN ligand; Black: linker; Pink: Smurf1 ligand (Smurf1-L)) .

HY-175975

PROTAC Akt3 Degrader-1	PROTACs Akt	Cancer
PROTAC Akt3 Degrader-1 is a highly efficient and selective *PROTAC* degrader targeting *Akt3. PROTAC* Akt3 Degrader-1 shows weak antiproliferative activity in 36 cell lines. PROTAC Akt3 Degrader-1 can be used for the study of Triple-negative breast cancer and melanoma .

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-145281

MS98	PROTACs Akt	Cancer
MS98 is a potent and selective **PROTAC AKT** degrader. MS98 depletes cellular total *AKT* (T-AKT) with the DC₅₀ value of 78 nM. MS98 binds to AKT1, AKT2, and AKT3 with K_ds of 4 nM, 140 nM, and 8.1 nM, respectively .

HY-163709

PROTAC FAK degrader 2	PROTACs FAK Akt ERK	Cancer
PROTAC FAK degrader 2 is an orally active PROTAC FAK degrader with a DC₅₀ of 60.10 nM. PROTAC FAK degrader 2 forms a ternary complex with FAK and CRBN E3 ubiquitin ligase, driving proteasome-mediated degradation of total and phosphorylated FAK. PROTAC FAK degrader 2 inhibits phosphorylation of *AKT* and ERK, suppressing their downstream signaling pathways. PROTAC FAK degrader 2 reduces cancer cell viability, adhesion, migration, and invasion. PROTAC FAK degrader 2 exerts anti-tumor activity in HCT8/T tumor xenografts in mice. PROTAC FAK degrader 2 can be used for the research of breast cancer, colorectal cancer, lung cancer .

HY-178176

PROTAC CB1R Degrader-1	PROTACs Cannabinoid Receptor Akt ERK Bcl-2 Family Apoptosis	Cancer
PROTAC CB1R Degrader-1 is a potent and selective CB1R *PROTAC* degrader that exploits the ubiquitin-proteasome system (UPS) achieving a DC₅₀ of 3.37 μM in MCF-7 cells and showing no impact on CB2R. PROTAC CB1R Degrader-1 reduces CB1R-associated downstream signaling (p-AKT, p-ERK, BCL2, and MCM5), thereby inhibiting breast cancer cell proliferation and inducing apoptosis. PROTAC CB1R Degrader-1 can be used for breast cancer research. (Blue: CRBN ligand (HY-41547); Black: linker (HY-178198); Pink: CB1R ligand (HY-134497)) .

HY-130985

9-Decyn-1-ol	PROTAC Linkers	Cancer
9-Decyn-1-ol is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs. 9-Decyn-1-ol can be used to conjugate GDC-0068 with Lenalidomide to generate INY-03-041. INY-03-041 is a potent, highly selective and PROTAC-based pan-Akt degrader. INY-03-041 inhibits Akt1, Akt2 and Akt3 with IC₅₀s of 2.0 nM, 6.8 nM and 3.5 nM, respectively . 9-Decyn-1-ol 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-178858

PROTAC FLT3/CHK1 Degrader-1	PROTACs FLT3 Checkpoint Kinase (Chk) STAT ERK c-Myc Akt	Cancer
PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC₅₀ values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), *AKT* (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces apoptosis in MV-4-11 cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/CHK1 ligand (HY-178869 ), Blue: CRBN Ligand (HY-W093272), Black: Linker, E3 ligase ligand-linker conjugate (HY-W998238)) .

HY-136006A

(S,R,S)-AHPC-C6-NH2 hydrochloride VH032-C6-NH2 hydrochloride	E3 Ligase Ligand-Linker Conjugates	Inflammation/Immunology Cancer
(S,R,S)-AHPC-C6-NH2 hydrochloride (VH032-C6-NH2 hydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for *AKT* PROTAC degrader. (S,R,S)-AHPC-C6-NH2 hydrochloride is XF038-161A, example 6, extracted from patent WO2019173516A1 .

HY-179424

PROTAC HIF-1α degrader-2	PROTACs HIF/HIF Prolyl-Hydroxylase p38 MAPK Akt PI3K MEK Apoptosis	Cancer
PROTAC HIF-1α degrader-2 is a highly efficient and selective *PROTAC* degrader targeting HIF-1α. PROTAC HIF-1α degrader-2 promotes HIF-1α degradation via the ubiquitin-proteasome pathway by facilitating the formation of a HIF-1α/VHL ternary complex. PROTAC HIF-1α degrader-2 inhibits HeLa cell proliferation, migration, and colony formation, and induces apoptosis. PROTAC HIF-1α degrader-2 reduces p-MEK and *p-AKT* expression in the MAPK and *PI3K/AKT* pathways. PROTAC HIF-1α degrader-2 can be used for the study of cervical cancer .

HY-143882

MS5033	PROTACs Akt	Cancer
MS5033 is a potent PROTAC-based AKT (protein kinase B) degrader, with a DC₅₀ of 430 nM in PC3 cells .

HY-179388

PROTAC Sirt2 Degrader-2	PROTACs Sirtuin Apoptosis Akt mTOR	Cancer
PROTAC Sirt2 Degrader-2 is a highly efficient and selective *PROTAC* degrader targeting SIRT2. PROTAC Sirt2 Degrader-2 demonstrates the most potent anti-proliferative activity both in vitro and in vivo. PROTAC Sirt2 Degrader-2 leads to a marked increase in H4K16Ac levels. PROTAC Sirt2 Degrader-2 significantly suppresses clonogenic formation and migration, induces cell cycle arrest, and promotes apoptosis. PROTAC Sirt2 Degrader-2 inhibits the *AKT/mTOR* signaling pathway by indirectly degrading SIRT2 and blocking downstream protein phosphorylation, thereby disrupting the signaling cascade and suppressing tumor development. PROTAC Sirt2 Degrader-2 can be used for the study of ovarian cancer .

HY-174469

PROTAC PI3K/110β degrader-2	PROTACs P-glycoprotein Apoptosis Reactive Oxygen Species (ROS) Akt Bcl-2 Family Na+/K+ ATPase PI3K	Cancer
PROTAC PI3K/110β degrader-2 is a selective PI3K/p110β PROTAC degrader. PROTAC PI3K/110β degrader-2 can significantly degrade 110β protein and inhibit the expression of P-glycoprotein. PROTAC PI3K/110β degrader-2 can increase the level of reactive oxygen species (ROS). PROTAC PI3K/110β degrader-2 exerts anti-tumor effects by activating the endoplasmic reticulum stress (ERS)-mediated mitochondrial apoptosis pathway and inhibiting the *AKT/Bcl-2* signaling pathway. PROTAC PI3K/110β degrader-2 can be used for research on cancer. (Pink: PI3K/110β Ligand (HY-75124); Blue: VHL Ligand (HY-125845); Black: Linker (HY-W002042)) .

HY-174415

ZSH-2117	PROTACs EGFR Akt ERK	Cancer
ZSH-2117 is a covalent and selective EGFR *PROTAC* degrader with a DC₅₀ of 45 nM in Ba/F3-EGFR ^{L858R/T790M/C797S} cells. ZSH-2117 significantly inhibits cell proliferation and reduces the downstream EGFR signaling proteins level of *AKT* and ERK. ZSH-2117 effectively inhibits tumor growth in Ba/F3-EGFR ^{L858R/T790M/C797S} xenograft mice model . Pink: EGFR ligand (HY-175162); Blue: NEDD4 ligase ligand (HY-175159); Black: linker

HY-136006

(S,R,S)-AHPC-C6-NH2 dihydrochloride VH032-C6-NH2 dihydrochloride	E3 Ligase Ligand-Linker Conjugates	Inflammation/Immunology Cancer
(S,R,S)-AHPC-C6-NH2 dihydrochloride (VH032-C6-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT* PROTAC* degrader. (S,R,S)-AHPC-C6-NH2 dihydrochloride is XF038-161A, example 6, extracted from patent WO2019173516A1 .

HY-133487

(S,R,S)-AHPC-C8-NH2 dihydrochloride VH032-C8-NH2 dihydrochloride	E3 Ligase Ligand-Linker Conjugates	Inflammation/Immunology Cancer
(S,R,S)-AHPC-C8-NH2 dihydrochloride (VH032-C8-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT* PROTAC* degrader. (S,R,S)-AHPC-C8-NH2 is XF038-164A, example 8, extracted from patent WO2019173516A1 .

HY-175976

Akt3 ligand-1	Akt Ligands for Target Protein for PROTAC	Cancer
Akt3 ligand-1 is an *Akt3* inhibitor (IC₅₀ = 0.1 nM) and a ligand for the target protein for PROTAC (Akt3). Akt3 ligand-1 can be used to synthesize PROTAC Akt3 Degrader-1(HY-175975) .

HY-133487A

(S,R,S)-AHPC-C8-NH2 hydrochloride VH032-C8-NH2 hydrochloride	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-C8-NH2 (VH032-C8-NH2) hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology .

HY-171334A

P1D-34	PROTACs PIN1 CDK Akt c-Myc Apoptosis Reactive Oxygen Species (ROS)	Cancer
P1D-34 is a Pin1 *PROTAC* degrader with a DC₅₀ value of 177 nM. P1D-34 also down-regulates Pin1 client proteins such as Cyclin D1, Rb, Mcl-1, Akt, and c-Myc. P1D-34 shows anti-proliferative activities in a panel of acute myeloid leukemia (AML) cell lines. P1D-34 induces cell DNA damage and apoptosis by releasing ROS generation. Pink: PIN1 ligand (HY-171442A), Blue: CRBN ligand (HY-14658), Black: Linker (HY-W014883) .

HY-181153

PROTAC FGFR3 Degrader-1	PROTACs FGFR	Cancer
PROTAC FGFR3 Degrader-1 is a fibroblast growth factor receptor 3 (FGFR3) PROTAC degrader, promotes FGFR3 degradation via the ubiquitin-proteasome pathway, and inhibits the downstream FGFR3/PI3K/AKT signaling pathway. PROTAC FGFR3 Degrader-1 can be used for the research of hepatocellular carcinoma .

HY-180261

GP262	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) .

Cat. No.	Product Name		Classification

HY-130985

9-Decyn-1-ol		PROTAC Synthesis Alkynes
9-Decyn-1-ol is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs. 9-Decyn-1-ol can be used to conjugate GDC-0068 with Lenalidomide to generate INY-03-041. INY-03-041 is a potent, highly selective and PROTAC-based pan-Akt degrader. INY-03-041 inhibits Akt1, Akt2 and Akt3 with IC₅₀s of 2.0 nM, 6.8 nM and 3.5 nM, respectively . 9-Decyn-1-ol 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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