Search Result

Pathways Recommended:	PROTAC PI3K/Akt/mTOR

Results for "

PROTAC AKT degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (15) PROTAC Linkers (1) Apoptosis (5) Autophagy (1) Bcl-2 Family (1) c-Myc (1) CDK (2) E3 Ligase Ligand-Linker Conjugates (5) EGFR (2) ERK (2) FAK (1) Na+/K+ ATPase (1) P-glycoprotein (1) PDK-1 (1) PI3K (3) PIN1 (1) PROTACs (18) Reactive Oxygen Species (ROS) (2)
By Research Areas:	Cancer (24) Inflammation/Immunology (4)
Click Chemistry:	PROTAC Synthesis (1) Alkynes (1)

Inhibitors & Agonists

Click Chemistry

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

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-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-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-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-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-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-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-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, Cereblon ligand). INY-03-041 trihydrochloride inhibits *AKT1, AKT2* and *AKT3* with IC₅₀s of 2.0, 6.8 and 3.5 nM, respectively .

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-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-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-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-163709

PROTAC FAK degrader 2	PROTACs FAK	Cancer
PROTAC FAK degrader 2 (Compound F2) is a PROTAC degrader for focal adhesion kinase (FAK), with DC₅₀ of 27.72 and 60.1 nM, for total FAK and phosphorylated p-FAK. PROTAC FAK degrader 2 inhibits cell viability of cancer cells 4T1, MDA-MB-231, MDA-MB-468 and MDA-MB-435, with IC₅₀s of 0.73-5.84 μM. PROTAC FAK degrader 2 reverses the multidrug resistance (MDR) through inhibition of *AKT* and ERK signaling pathway. PROTAC FAK degrader 2 exhibits antitumor efficacy in HCT/8 xenograft mouse model. (Pink: ligand for target protein Ifebemtinib (HY-122844); Black: linker (HY-Y0681); Blue: ligand for E3 ligase Thalidomide (HY-14658))

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-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-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-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	CDK PROTACs Apoptosis	Cancer
YJ1206 is an orally active, selective CDK12/CDK13 PROTAC degrader with an IC₅₀ of 12.55 nM for in VCaP cells. YJ1206 increases DNA damage, induces apoptosis, and promotes tumor regression in orthotopic WA74 patient-derived xenograft (PDX) mice models of resistant prostate cancer. YJ1206 suppresses tumor growth in vivo in conjunction with AKT pathway inhibitors. YJ1206 is composed of the CDK12/CDK13 degradation agent (HY-168658), a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548). (Pink: Navitoclax; Blue: VHL ligand; Black: linker) .

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-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

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.

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Name
Email *

	Sorry, but the email address you supplied was invalid.