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Results for "

PROTAC-based

" in MedChemExpress (MCE) Product Catalog:

By Targets:	AAK1 (1) Adrenergic Receptor (1) Akt (3) Anaplastic lymphoma kinase (ALK) (3) Apoptosis (11) Aurora Kinase (1) Autophagy (1) Bcl-2 Family (4) Bcr-Abl (1) Btk (2) c-Met/HGFR (2) c-Myc (4) CaMK (1) Casein Kinase (1) CCR (1) CDK (5) Discoidin Domain Receptor (1) E1/E2/E3 Enzyme (1) E3 Ligase Ligand-Linker Conjugates (6) EGFR (2) Enterovirus (1) Ephrin Receptor (2) Epigenetic Reader Domain (16) Ferroptosis (2) FKBP (3) Glutathione Peroxidase (1) HDAC (2) Hedgehog (1) Histone Acetyltransferase (1) Histone Methyltransferase (1) HSV (1) Huntingtin (1) IKK (1) Integrin (1) Interleukin Related (1) IRAK (4) JAK (2) Ligands for E3 Ligase (4) Ligands for Target Protein for PROTAC (6) LIM Kinase (LIMK) (1) LRRK2 (1) MAP4K (2) MDM-2/p53 (1) Molecular Glues (1) p38 MAPK (1) PARP (1) PD-1/PD-L1 (1) PDGFR (1) PI3K (1) PIN1 (1) PROTAC Linkers (1) PROTACs (72) Ras (2) Reference Standards (1) RIP kinase (1) Salt-inducible Kinase (SIK) (1) SOS1 (2) Src (1) STAT (3) STING (1) ULK (1) VEGFR (2) VSV (1) YAP (1)
By Research Areas:	Cancer (80) Infection (2) Inflammation/Immunology (8) Metabolic Disease (2) Neurological Disease (4)
Click Chemistry:	PROTAC Synthesis (4) Alkynes (1)

Inhibitors & Agonists

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100972

ARV-771 Maximum Cited Publications 29 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with K_ds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), 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-129180

XY028-133	PROTACs CDK	Cancer
XY028-133 (example 14) is a *PROTAC*-based CDK4/6 degrader with anti-tumor activity, which consists of ligands for von Hippel-Lindau and CDK .

HY-161157

dTAG-13-NEG	PROTACs	Cancer
dTAG-13-NEG is a negative control of dTAG-13 (HY-114421). dTAG-13, a PROTAC-based heterobifunctional degrader, is a selective degrader of FKBP12 ^F36V with expression of FKBP12F36V in-frame with a protein of interest .

HY-114421

*FKBP12 PROTAC* dTAG-13** 5+ Cited Publications dTAG-13	PROTACs FKBP	Cancer
FKBP12 PROTAC dTAG-13 (dTAG-13), a PROTAC-based heterobifunctional degrader, is a selective degrader of FKBP12 ^F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 effectively engages FKBP12 ^F36V and CRBN, thereby selectively degrading FKBP12 ^F36V .

HY-130714

TD-165 1 Publications Verification	PROTACs	Cancer
TD-165 is a PROTAC-based cereblon (CRBN) degrader. TD-165 comprises a?cereblon (CRBN)?ligand binding group, a linker and an?von Hippel-Landau (VHL)?binding group .

HY-125877

PROTAC Mcl1 degrader-1 1 Publications Verification	PROTACs Bcl-2 Family	Cancer
PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC₅₀ of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC₅₀ of 0.54 μM .

HY-111866

PROTAC RIPK degrader-2 1 Publications Verification	PROTACs RIP kinase	Metabolic Disease Cancer
PROTAC RIPK degraders -2 is a non-peptide *PROTAC* based on von Hippel-Lindau and targets serine-threonine kinase RIPK2, which is highly selective to the degradation of RIPK2. PROTAC RIPK degrader-2 acts as an activator to increase cell death and activate ion channels in cancer cells. PROTAC RIPK degrader-2 also can inhibit protein interactions, such as receptors and ligands, involved in a variety of diseases, such as cancer and diabetes .

HY-103634

dFKBP-1 1 Publications Verification	PROTACs FKBP	Cancer
dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF (HY-114872) of FKBP12, the Thalidomide based Cereblon ligand and a linker .

HY-150251

SD-91 STAT3 degrader-2	PROTACs STAT	Cancer
SD-91 (STAT3 degrader-2), a product of the hydrolysis of SD-36 (HY-129602), is a selective PROTAC-based STAT3 degrader with a K_i of 5.5 nM. SD-91 displays >300-fold selectivity over other STAT family protein members. SD-91 potently induces degradation of STAT3 protein in cells. SD-91 has anticancer effects, such as myeloid leukemia, lymphoma (Pink: ligand for target protein (HY-150895); Black: linker; Blue: E3 ligase ligand; E3 ligase ligand+linker: HY-176506) .

HY-125876

PROTAC Bcl2 degrader-1 1 Publications Verification	PROTACs Bcl-2 Family	Cancer
PROTAC Bcl2 degrader-1 (Compound C5) is a *PROTAC* based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC₅₀, 4.94 μM; DC₅₀, 3.0 μM) and Mcl-1 (IC₅₀, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1 (Blue: CRBN ligand, Black: linker；Pink: Mcl-1/Bcl-2 inhibitor, Nap-1).

HY-131183

PROTAC PD-1/PD-L1 degrader-1	PROTACs PD-1/PD-L1	Inflammation/Immunology
PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC₅₀ of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner .

HY-129610

KB02-SLF	PROTACs FKBP	Cancer
KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF .

HY-149236

PROTAC GPX4 degrader-1	PROTACs Glutathione Peroxidase Ferroptosis	Cancer
PROTAC GPX4 degrader-1 (DC-2) is a PROTAC-based GPX4 degrader, with a DC₅₀ of 0.03 μM in HT1080 cells .

HY-162412

PROTAC AR/AR-V7 degrader-1	PROTACs Adrenergic Receptor Apoptosis	Cancer
PROTAC AR/AR-V7 degrader-1 (27c) is a *PROTAC*-based and dual AR, AR-V7 degrader, with DC₅₀ values of 2.67 and 2.64 μM for AR and AR-V7, respectively. PROTAC AR/AR-V7 degrader-1 (27c) induces apoptosis (Red: AR antagonist; Blue: E3 ligase ligand; Black: linker) .

HY-129917

KB02-JQ1 4 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1 .

HY-173679

RBN012811	PROTACs PARP Interleukin Related STAT Integrin HSV VSV	Infection Cancer
RBN012811 is a highly selective *PROTAC*-based PARP14 degrader. RBN012811 forms a ternary complex with cereblon by binding to the NAD ⁺site of PARP14, and mediates the specific degradation of PARP14 via the ubiquitin-proteasome pathway (IC₅₀=10 nM). RBN012811 effectively depletes endogenous PARP14 in various cell lines and primary human macrophages, thereby downregulating IL-10 production and IFN-β mRNA levels, increasing phosphorylated STAT1 levels to enhance inflammatory signaling, and inhibiting interferon-induced ADPr condensate formation. RBN012811 also modulates viral replication, exhibiting increased HSV1 replication while reducing VSV replication. RBN012811 has important application value in research related to cancer and viral infections .

HY-125834

GMB-475	PROTACs Bcr-Abl Apoptosis STAT JAK	Cancer
GMB-475 is a potent BCR-ABL1 PROTAC based on Von Hippel-Lindau (VHL). GMB-475 targets the nutmeg pocket of ABL1 in an ectopic manner and degrades BCR-ABL1 protein through the ubiquitin proteasome pathway. GMB-475 inhibits the proliferation of human K562 cells and mouse Ba/F3 cells, and is used for the study of chronic myeloid leukemia. (Blue: VHL ligand (HY-125845); Black: Linker; Pink: BCR-ABL1 ligand (HY-11007)) .

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-170859

AH078	PROTACs Casein Kinase	Cancer
AH078 is a *PROTAC*-based CK1δ/ε degrader (DC₅₀=0.55 μM, D_max=70%) that lacks subtype selectivity between CK1δ and CK1ε. AH078 induces target protein degradation either by recruiting the CUL4-CRBN E3 ligase complex and proteasome, or via the VHL- and ubiquitin-dependent pathway. AH078 also exhibits selectivity for CK1α, and is widely applicable to research related to colon cancer, pancreatic cancer, breast cancer, ovarian cancer, chronic lymphocytic leukemia, acute myeloid leukemia, glioma, and metastatic breast adenocarcinoma .

HY-155218

TMX-2172	PROTACs CDK	Cancer
TMX-2172 is a selective bivalent cereblon-recruiting *PROTAC*-based dual CDK2 and CDK5 degrader with IC₅₀ values of 6.5 nM and 6.8 nM, respectively. TMX-2172 shows selectivity for CDK2 and CDK5 over other cell cycle CDKs (CDK1, CDK4, and CDK6) and transcriptional CDKs (CDK7 and CDK9). TMX-2172 inhibits CDK2/CDK5 enzymatic activity, induces their proteasomal degradation, reduces ASCL1 protein levels and half-life, induces cancer cell death, and exerts antiproliferative effects. TMX-2172 can be used for the research of ovarian cancer and small cell lung cancer .

HY-160506

PRO-6E	PROTACs c-Met/HGFR Apoptosis	Cancer
PRO-6E is an oral active *PROTAC* based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker；Pink: ALK/c-Met inhibitor Crizotinib (HY-50878)) .

HY-158048

UNC9036	PROTACs STING	Inflammation/Immunology
UNC9036 is a *PROTAC*-based STING degrader, with a DC₅₀ of 227 nM. UNC9036-mediated STING degradation is proteasome and VHL dependent (Structure Note: Red, STING agonist diABZI (HY-112921A); Blue, VHL ligand VH032 (HY-120217); Black, linker) .

HY-176184

PROTAC DDR1 degrader-1	PROTACs Discoidin Domain Receptor	Cancer
PROTAC DDR1 degrader-1 is a PROTAC based DDR1 degrader (Red: DDR1 inhibitor (HY-176185), black: linker, Blue: E3 ligase ligand) .

HY-168221

YD54	PROTACs	Cancer
YD54 is a *PROTAC* based SMARCA2 degrader with a DC₅₀ of 3.5 nM (Red: SMARCA2 degrader (HY-44012B), black: linker, Blue: E3 ligase ligand) .

HY-148063

DB0614	PROTACs AAK1 Aurora Kinase CaMK CDK Ferroptosis Salt-inducible Kinase (SIK) LIM Kinase (LIMK) ULK	Metabolic Disease
DB0614 is a *PROTAC* based on Cereblon ligand, which is a selective and potent targeted protein degrader of NEK9 inhibitor. DB0614 can degrade ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2 and ULK1. DB0614 can be used for research of disease or disorder mediated by aberrant kinase activity .(Blue: Thalidomide-4-OH (HY-103596), Black: linker, Pink: FLT3-IN-17 (HY-148070))

HY-146231

SS47	PROTACs MAP4K	Inflammation/Immunology Cancer
SS47, a *PROTAC*-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the antitumor efficacy .

HY-156774

CCW 28-3	PROTACs Epigenetic Reader Domain	Others
CCW 28-3 is a PROTAC-based BRD4 degrader in a proteasome- and RNF4-dependent manner (Pink: JQ-1 (carboxylic acid) (HY-78695); Black: linker (HY-170384); Blue: RNF4 ligand CCW16 (HY-143346)) .

HY-147219A

SIAIS164018 hydrochloride	PROTACs Anaplastic lymphoma kinase (ALK) EGFR Apoptosis	Cancer
SIAIS164018 hydrochloride is a *PROTAC*-based ALK and EGFR degrader, with IC₅₀ value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857) .

HY-146231A

SS47 TFA	MAP4K PROTACs	Inflammation/Immunology Cancer
SS47 TFA, a *PROTAC*-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the in vivo antitumor efficacy of BCMA CAR-T cell research. HPK1, an immunosuppressive regulatory kinase, is a promising target for cancer immunotherapies . SS47 (TFA) 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-115568

BETd-246 2 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
BETd-246 is a second-generation and *PROTAC*-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity .

HY-163152

PROTAC BRM degrader-1	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRM degrader-1 (compound 17) is a *PROTAC*-based BRM and BRG1 degrader, with DC₅₀ values of 93 pM and 4.9 nM, respectively .

HY-155393

PROTAC BRD4 Degrader-22	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-22 (Compd 44h) is a PROTAC-based BRD4 degrader, with a pDC₅₀ (MOLT4, 24 h) of 9.2 .

HY-162676

SJ45566	PROTACs Src	Cancer
SJ45566 a potent and orally active PROTAC-based LCK degrader, with a DC₅₀ of 1.21 nM. SJ45566 can be used in the research for T‑Cell Acute Lymphoblastic Leukemia .

HY-139707

PROTAC CBP/P300 Degrader-3 Thalidomide-NH-CBP/p300 ligand 2	PROTACs Molecular Glues Epigenetic Reader Domain	Cancer
PROTAC CBP/P300 Degrader-3 (P-007) is a *PROTAC*-based CBP and p300 degrader (extracted from patent WO2020173440) .

HY-170413

PROTAC BTK Degrader-12	PROTACs Btk	Cancer
PROTAC BTK Degrader-12 (EXAMPLE 19) is a *PROTAC*-based BTK degrader (Pink & black: BTK ligand & linker (HY-170414); Black: linker (HY-30105); Blue: CRBN ligand ( HY-W245311)) .

HY-147219

SIAIS164018	PROTACs Anaplastic lymphoma kinase (ALK) EGFR Apoptosis	Cancer
SIAIS164018 is a *PROTAC*-based ALK and EGFR degrader, with IC₅₀ value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib (HY-12857) .

HY-135382

PROTAC IRAK4 degrader-2	PROTACs IRAK	Inflammation/Immunology Cancer
PROTAC IRAK4 degrader-2 (Compound 9) is a PROTAC-based IRAK4 degrader that affords potent IRAK4 degradation with a DC₅₀ in peripheral blood mononuclear cells (PBMCs) cells of 151 nM. PROTAC IRAK4 degrader-2 induce a reduction of IRAK4 protein levels with a DC₅₀ of 36 nM in PBMC cells. PROTAC IRAK4 degrader-2 also leads to the inhibition of multiple cytokines in PBMCs .

HY-171334

(Rac)-P1D-34	PROTACs PIN1	Cancer
PROTAC PIN1 degrader-2 (1) is a *PROTAC*-based PIN1 degrader (Pink: PIN1 ligand HY-171442, Blue: cereblon ligand Thalidomide (HY-14658), Black: linker HY-W014883). PROTAC PIN1 degrader-2 (1) possesses anti-cancer activity, with IC₅₀ values of 2248 nM (MV-4-11 cells), 3984 nM (MOLM-13), 3925 nM (HL-60), 3925 nM (HL-60), 3925 nM (HL-60), 3925 nM (HL-60) and 3925 nM (HL-60) respectively .

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-114405

SJFδ	PROTACs p38 MAPK Autophagy	Cancer
SJFδ is a 10-atom linker *PROTAC* based on von Hippel-Lindau ligand. SJFδ degrades p38δ with a DC₅₀ of 46.17 nM, but does not degrade p38α, p38β, or p38γ .

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-170335

PROTAC c-Met degrader-2	PROTACs c-Met/HGFR	Others
PROTAC c-Met degrader-2 (PROTAC2) is a PROTAC-based c-Met degrader, with a DC₅₀ of 50 nM (Pink: Foretinib (HY-10338); Black: linker (HY-45124); Blue: CRBN ligand Thalidomide-4-O-C2-NH2 (HY-136162A)) .

HY-162835

PROTAC SMARCA2/4-degrader-28	PROTACs Epigenetic Reader Domain	Cancer
PROTAC SMARCA2/4-degrader-28 (PROTAC 1) is a *PROTAC*-based partial degrader of SMARCA2 and SMARCA4(Bliue: CRL2 ^VHL ligand (S,R,S)-AHPC (HY-125845); Black: linker (HY-159680); Pink: a SMARCA-BD ligand (+)-JQ-1 (HY-13030)) .

HY-156814

HPP-9	Hedgehog	Cancer
HPP-9 is a Proteolysis-Targeting Chimeras （PROTACs） based on Hedgehog Pathway Inhibitor-1 (HPI-1), with the pIC₅₀ of 6.71, that can degrade BET bromodomains. HPP-9 has antitumor activity ^[1[.

HY-173467

PROTAC MTP3 degrader-1	PROTACs c-Myc	Cancer
PROTAC MTP3 degrade-1 is a PROTAC based MYC degrader (Red: MYC inhibitor (HY-173469), black: linker (HY-W008296), Blue: E3 ligase ligand (HY-14658)) .

HY-155684

SA-PA	PROTACs VEGFR PDGFR Ephrin Receptor	Cancer
SA-PA is an intracellular self-assembled *PROTAC* based on azide and alkyne. SA-PA is able to selectively degrade VEGFR-2, PDGFR-β and EphB4 proteins in U87 cells. SA-PA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues .

HY-176421

PROTAC PI3K/110β degrader-1	PROTACs PI3K	Cancer
PROTAC PI3K/110β degrader-1 (J-9) is a PROTAC based PI3K/110β degrader (Red: PI3K/110β inhibitor (HY-75124), black: linker, Blue: E3 ligase ligand) .

HY-155398

PRO-HD3	PROTACs HDAC	Cancer
PRO-HD3 is a cell-specific, PROTAC-based HDAC6 degrader .

HY-155397

PRO-HD2	PROTACs HDAC	Cancer
PRO-HD2 is a cell-specific, PROTAC-based HDAC6 degrader .

Cat. No.	Product Name		Classification

HY-150251

SD-91 STAT3 degrader-2		PROTAC Synthesis
SD-91 (STAT3 degrader-2), a product of the hydrolysis of SD-36 (HY-129602), is a selective PROTAC-based STAT3 degrader with a K_i of 5.5 nM. SD-91 displays >300-fold selectivity over other STAT family protein members. SD-91 potently induces degradation of STAT3 protein in cells. SD-91 has anticancer effects, such as myeloid leukemia, lymphoma (Pink: ligand for target protein (HY-150895); Black: linker; Blue: E3 ligase ligand; E3 ligase ligand+linker: HY-176506) .

HY-146231

SS47		PROTAC Synthesis
SS47, a *PROTAC*-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the antitumor efficacy .

HY-146231A

SS47 TFA		PROTAC Synthesis
SS47 TFA, a *PROTAC*-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the in vivo antitumor efficacy of BCMA CAR-T cell research. HPK1, an immunosuppressive regulatory kinase, is a promising target for cancer immunotherapies . SS47 (TFA) 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-130985

9-Decyn-1-ol		Alkynes PROTAC Synthesis
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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