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KRAS degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (2) Apoptosis (3) ATTECs (1) Autophagy (2) E3 Ligase Ligand-Linker Conjugates (4) EGFR (1) ERK (1) Ferroptosis (1) Ligands for E3 Ligase (1) Ligands for Target Protein for PROTAC (3) MDM-2/p53 (1) Molecular Glues (3) mTOR (1) PDK-1 (1) PERK (1) Phosphodiesterase (PDE) (2) PI3K (1) PROTAC Linkers (5) PROTAC-Linker Conjugates for PAC (1) PROTACs (28) Ras (36) SOS1 (6) Target Protein Ligand-Linker Conjugates (7)
By Research Areas:	Cancer (57) Infection (1)

By Targets:

Akt (2)

Apoptosis (3)

ATTECs (1)

Autophagy (2)

E3 Ligase Ligand-Linker Conjugates (4)

EGFR (1)

ERK (1)

Ferroptosis (1)

Ligands for E3 Ligase (1)

Ligands for Target Protein for PROTAC (3)

MDM-2/p53 (1)

Molecular Glues (3)

mTOR (1)

PDK-1 (1)

PERK (1)

Phosphodiesterase (PDE) (2)

PI3K (1)

PROTAC Linkers (5)

PROTAC-Linker Conjugates for PAC (1)

PROTACs (28)

Ras (36)

SOS1 (6)

Target Protein Ligand-Linker Conjugates (7)

By Research Areas:

Cancer (57)

Infection (1)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-162960

*pan-KRAS* degrader 1**	Ras	Cancer
pan-KRAS degrader 1 (Compound 1) is a panKRAS degrader with a surface plasmon resonance (SPR) dissociation constant K_i value of 25 nM for KRAS ^G12V .pan-KRAS degrader 1 has antitumor activity .

HY-129523

*PROTAC K-Ras* Degrader-1** 2 Publications Verification	PROTACs Ras	Cancer
PROTAC K-Ras Degrader-1 (Compound 518) is a PROTAC. PROTAC K-Ras Degrader-1 can effectively degrades *K-Ras* based on Cereblon E3 ligand, exhibits ≥70% degradation efficacy in SW1573 cells .

HY-159788

*PROTAC K-Ras* Degrader-4**	PROTACs Ras	Cancer
PROTAC K-Ras Degrader-4 (Compound 4) is a PROTAC degrader for *KRAS* that degrades KRAS ^G12D in GP5d and degrades KRAS ^G12V in cell SW620 with DC₅₀s of 1 nM and 13 nM. PROTAC K-Ras Degrader-4 inhibits MAPK signaling pathway . (Pink: ligand for target protein pan-KRAS degrader 1 (HY-162960); Black: linker (HY-159790); Blue: ligand for E3 ligase VHL (HY-W998248))

HY-139186

*PROTAC KRAS* G12C degrader-1**	PROTACs	Cancer
PROTAC KRAS G12C degrader-1 is a Cereblon-based KRAS ^G12C PROTAC degrader. PROTAC KRAS G12C degrader-1 induces CRBN/ KRAS ^G12C dimerization and degrades GFP- KRAS ^G12C in reporter cells .

HY-153880

KRAS degrader-1	PROTACs Ras	Cancer
KRAS degrader-1 (compound 1) is a potent *KRAS* degrader. KRAS degrader-1 target specific proteins for degradation through the autophagy-lysosomal degradation pathway .

HY-164365

*PROTAC K-Ras* Degrader-2**	PROTACs Ras	Cancer
PROTAC K-Ras degrader-2 (compound 48) is a pan-KRAS-mutant PROTAC degrader with an IC₅₀ of ≤200 nM for KRAS G12V/RAF1. PROTAC K-Ras degrader-2 degrades SW620 KRAS G12D with a DC₅₀ of ≤200 nM. PROTAC K-Ras degrader-2 inhibits cell growth of SW620 3D cell with an IC₅₀ of ≤20 nM. (Pink: KRAS inhibitor-30 (HY-164366)) .

HY-168678

*PROTAC K-Ras* Degrader-6**	PROTACs Ras	Cancer
pan-KRAS degrader 5 (compound 102) is a potent cereblon-based KRAS PROTAC degrader, with a DC50 of <100 nM. pan-KRAS degrader 5 shows anticancer effects. (Pink: ligand for target protein (HY-168679); Black: linker (HY-168670); Blue: E3 ligase ligand (HY-W580113)) .

HY-168669

*PROTAC K-Ras* Degrader-5**	PROTACs Ras	Cancer
pan-KRAS degrader 4 (compound 69) is a potent cereblon-based KRAS PROTAC degrader, with a DC50 of <100 nM. pan-KRAS degrader 4 shows anticancer effects. (Pink: ligand for target protein (HY-168671); Black: linker (HY-168670); Blue: E3 ligase ligand (HY-W733895)) .

HY-176489

*PROTAC pan-KRAS* degrader-1**	PROTACs Ras	Cancer
PROTAC pan-KRAS degrader-1 is a *pan-KRAS* PROTAC degrader for degrading different KRAS mutation types, such as G12D, G12C, G12V, and G13D. PROTAC pan-KRAS degrader-1 potently degrades KRAS mutation (G12D) in AGS cells, with a DC₅₀ of 1.1 nM, D_max of 95%. PROTAC pan-KRAS degrader-1 can be used to search diseases caused by KRAS mutation or amplification, especially cancers such as breast cancer, bladder cancer, gastric cancer, etc . Pink: pan-KRAS ligand (HY-176490); Blue: VHL ligase ligand (HY-170353); Black: linker (HY-176491);

HY-168054

*PROTAC K-Ras* Degrader-3**	PROTACs Ras	Cancer
PROTAC K-Ras Degrader-3 (compound 40) is a PROTAC degrader of *K-Ras* with a DC₅₀ of ≤ 1 nM against SW620 KRAS G12D, and a GI₅₀ of ≤ 10 nM against SW620 3D cell growth. PROTAC K-Ras Degrader-3 can be utilized in cancer research .

HY-153881

KRAS G12C degrader-1	Ras	Cancer
KRAS G12C degrader-1 (Compound 283) is a potent KRAS G12C degrader (DC₅₀: < 100 nM) for cancer research. KRAS G12C degrader-1 is a chaperone (HSP90)-mediated protein degrader (CHAMPs) .

HY-161176

*PROTAC KRAS* G12D degrader 1**	PROTACs	Cancer
PROTAC KRAS G12D degrader 1 (compound 8o) is a potent, rapid, and selective degrader of protac KRAS ^G12D with DC ⁵⁰ of 38.06 nM. PROTAC KRAS G12D degrader 1 showes significant antitumor efficacy .

HY-153821

*PROTAC KRAS* G12C degrader-2**	Ras PROTACs	Cancer
PROTAC KRAS G12C degrader-2 (compound 432) is a modulator of *K-Ras* protein hydrolysis. PROTAC KRAS G12C degrader-2 is a bifunctional compound, which contain on one end a cereblon inhibitor of apoptosis proteins (IAP) and on the other end a moiety which binds KRAS .

HY-161177

*PROTAC KRAS* G12D degrader 2**	PROTACs Ras	Infection
PROTAC KRAS G12D degrades SARS-CoV-2, 3-curd trypsin-like protease (3CLPro). Protac KRAS G12D degrades SARS-CoV-2, 3-curd trypsin-like protease (3CLPRO). The PROTAC molecule is designed by partially coupling a GC-376-based dipeptidyl 3CLPro ligand with pomadomide via a piperazine-piperidine linker .

HY-157228

ACBI3	PROTACs Ras	Cancer
ACBI3 (compound 7) is a PROTAC targeting *KRAS. ACBI3 is composed of PROTAC target protein ligand pan-KRAS* degrader 1 (HY-162960) (red part), E3 ligase ligand E3 ligase Ligand 43 (HY-401613) (blue part) and PROTAC Linker 1-Bromo-4-(ethynyloxy)butane (HY-169992) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 143 (HY-169995). ACBI3 achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models .

HY-161236

KRAS ligand 4	Molecular Glues SOS1 Ras	Cancer
KRAS ligand 4 (compound 2) is a bifunctional molecular glue degrader based on SOS1. KRAS ligand 4 reduces downstream signaling markers pERK and pS6 and displays anti-additional activity in cells with multiple KRAS mutations .

HY-130820

THP-PEG4-Pyrrolidine(N-Boc)-CH2OH	PROTAC Linkers	Cancer
THP-PEG4-Pyrrolidine(N-Boc)-CH2OH is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523) .

HY-161233

BTX-6654	SOS1 PROTACs ERK	Cancer
BTX-6654 is a target-dependent and -specific cereblon-based bifunctional SOS1 PROTAC degrader. BTX-6654 reduces downstream signaling markers pERK and pS6, and displays antiproliferative activity in cells harboring various KRAS mutations .

HY-168056

KRAS ligand 5	Others	Others
KRAS ligand 5 is the target protein ligand for PROTAC K-Ras Degrader-3 (HY-168054). PROTAC K-Ras Degrader-3 can specifically degrade KRAS mutated proteins .

HY-176490

pan-KRAS ligand 3	Ligands for Target Protein for PROTAC Ras	Cancer
Pan-KRAS ligand 3 is a *pan-KRAS* inhibitor. Pan-KRAS ligand 3 can be used for synthesis of PROTAC pan-KRAS degrader-1 (HY-176489) .

HY-129776

K-Ras ligand-Linker Conjugate 2	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 2 incorporates a ligand for *K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras* ligand-Linker Conjugate 2 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .

HY-129775

K-Ras ligand-Linker Conjugate 1	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 1 incorporates a ligand for *K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras* ligand-Linker Conjugate 1 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .

HY-168055

(S)-Deoxy-thalidomide	Ligands for E3 Ligase	Cancer
(S)-Deoxy-thalidomide is an E3 ubiquitin ligase ligand. (S)-Deoxy-thalidomide can be linked to the target protein ligand through a linker to form PROTAC K-Ras Degrader-3 (HY-168054). PROTAC K-Ras Degrader-3 can target KRAS mutant proteins for degradation .

HY-145615

Pomalidomide-C12-NH2 hydrochloride	E3 Ligase Ligand-Linker Conjugates	Cancer
Pomalidomide-C12-NH2 hydrochloride is the E3 ligase ligand-linker conjugate of PROTAC KRAS G12C degrader-1 (HY-139186). PROTAC KRAS G12C degrader-1 is a Cereblon-based KRAS ^G12C degrader .

HY-130822

K-Ras ligand-Linker Conjugate 4	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 4 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 4 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .

HY-130823

K-Ras ligand-Linker Conjugate 5	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 5 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 5 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .

HY-130991

K-Ras ligand-Linker Conjugate 6	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 6 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 6 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .

HY-130707

K-Ras ligand-Linker Conjugate 3	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 3 (Compound 001371) incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 3 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .

HY-168671

pan-KRAS ligand 1	Ligands for Target Protein for PROTAC Ras	Cancer
pan-KRAS ligand 1 is a Ligand for Target Protein for PROTAC. pan-KRAS ligand 1 can be used for synthesis PROTAC pan-KRAS degrader 4 (HY-168669) .

HY-174379

KRAS IN-44	Phosphodiesterase (PDE) Ras PI3K Akt mTOR Apoptosis	Cancer
KRAS IN-44 (Compound S2C2M2) is a PDE6D degrader. KRAS IN-44 inhibits PDE6D-dependent *KRAS* trafficking and *KRAS* downstream signaling pathways. KRAS IN-44 down-regulates EGF-induced the phosphorylation of PI3K, AKT, and mTOR. KRAS IN-44 increases Apoptosis. KRAS IN-44 has antitumor activity against hepatoblastoma .

HY-148273

Setidegrasib KRAS G12D inhibitor 17	PROTACs Ras	Cancer
Setidegrasib (KRAS G12D inhibitor 17, Example 8) is a PROTAC *KRAS* degrader (DC₅₀: 37 nM). Setidegrasib induces the degradation of G12D-mutation *KRAS* protein. Setidegrasib has antitumor effect. (Blue: E3 ligase ligand (HY-168699); Black: linker (HY-168698); Pink: G12D ligand (HY-168700)) .

HY-137516

LC-2 2 Publications Verification	PROTACs Ras	Cancer
LC-2 is a potent and first-in-class von Hippel-Lindau-based PROTAC capable of degrading endogenous KRAS G12C, with DC₅₀s between 0.25 and 0.76 μM . LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines .

HY-176134

RP03707	PROTACs Ras	Cancer
RP03707 is a PROTAC based KRAS ^G12D degrader (Red: KRAS ^G12D inhibitor (HY-134813), black: linker, Blue: E3 ligase ligand) .

HY-130819

Tos-PEG4-THP	PROTAC Linkers	Cancer
Tos-PEG4-THP is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523) .

HY-145737

PROTAC SOS1 degrader-1	PROTACs Ras	Cancer
PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader with an DC₅₀ of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity .

HY-145737A

PROTAC SOS1 degrader-1 TFA	PROTACs Ras	Cancer
PROTAC SOS1 degrader-1 (TFA) is a potent PROTAC SOS1 degrader with an DC₅₀ of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity .

HY-176491

Alkyne-pyrazine-O-piperidine-(1-methylcyclopropyl)methanol	PROTAC Linkers
Alkyne-pyrazine-O-piperidine-(1-methylcyclopropyl) methanol is a PROTAC linker that can be used in the synthesis of PROTACs, such as PROTAC pan-KRAS degrader-1 (HY-176489) .

HY-162809

XMU-MP-9	Ras	Cancer
XMU-MP-9 is a bifunctional compound that binds to the C2 domain of Nedd4-1 and the allosteric site of *K-Ras. XMU-MP-9 enhances the interaction between Nedd4-1* and *K-Ras, induces conformational changes in the Nedd4-1/K-Ras* complex, promotes the ubiquitination and degradation of multiple *K-Ras* mutants, and inhibits the proliferation of cells carrying *K-Ras* mutants. XMU-MP-9 can be used in cancer research .

HY-130821

THP-PEG4-Pyrrolidine(N-Me)-CH2OH	PROTAC Linkers	Cancer
THP-PEG4-Pyrrolidine(N-Me)-CH2OH is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523) .

HY-168075

Boc-PIP-Me-CH2-2,7-diazaspiro[3.5]nonane	PROTAC Linkers	Others
Boc-PIP-Me-CH2-2,7-diazaspiro[3.5]nonane is the linker of PROTAC K-Ras Degrader-3 (HY-168054), which can be used in the synthesis of PROTACs .

HY-168577

KRAS G12D inhibitor 25	Ras EGFR	Cancer
KRAS G12D inhibitor 25 (Compound 148) is an inhibitor for KRAS G12C and HSP90α with IC₅₀ of < 0.1 μM and 0.1-1 μM, respectively. KRAS G12D inhibitor 25 inhibits the proliferation of MIA PaCa-2 and NCI-H358 with EC₅₀ of < 0.1 μM and 0.1-1 μM, respectively. KRAS G12D inhibitor 25 degrades ERBB2 with a DC₅₀ of 0.1-1 μM .

HY-144323

YF135	PROTACs PERK	Cancer
YF135 is an efficient and reversible-covalent KRAS ^G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS ^G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway .

HY-157458

PDEδ autophagic degrader 1	ATTECs Phosphodiesterase (PDE) Autophagy	Cancer
PDEδ autophagic degrader 1 (compound 12c), an autophagosome-tethering compound (ATTEC). is a potent PDEδ autophagic degrader. PDEδ autophagic degrader 1 reduces the PDEδ protein level through lysosome-mediated autophagy without affecting the PDEδ mRNA expression. PDEδ autophagic degrader 1 suppresses the growth in KRAS mutant pancreatic cancer cells .

HY-139403

MRTX849 ethoxypropanoic acid	Target Protein Ligand-Linker Conjugates Ras	Cancer
MRTX849 ethoxypropanoic acid incorporates a ligand for KRAS G12C, and a PROTAC linker. MRTX849 ethoxypropanoic acid can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (IC₅₀s between 0.25 and 0.76 μM) .

HY-170428

IPS-06061	Molecular Glues Ras	Cancer
IPS-06061 is an orally active molecule glue, that forms a ternary complex of CRBN-KRASG12D-IPS06061, and degrades KRAS G12D with a DC₅₀ <500 nM .

HY-168672

E3 Ligase Ligand-linker Conjugate 133	E3 Ligase Ligand-Linker Conjugates	Cancer
E3 Ligase Ligand-linker Conjugate 133 is a conjugate of E3 ligase ligand and linker that serve as a key intermediate for the synthesis of complete PROTAC molecule pan-KRAS degrader 4 (HY-168669) .

HY-168680

E3 Ligase Ligand-linker Conjugate 135	E3 Ligase Ligand-Linker Conjugates	Cancer
E3 Ligase Ligand-linker Conjugate 135 is a conjugate of E3 ligase ligand and linker that serve as a key intermediate for the synthesis of complete PROTAC molecule pan-KRAS degrader 5 (HY-168678) .

HY-161235

BTX-7312	SOS1 Molecular Glues Ras	Cancer
BTX-7312 is a cereblon-based SOS1 bifunctional degrader and a molecular glue. BTX-7312 reduces downstream signaling markers pERK and pS6 and shows antiproliferative activity in various *KRAS*-mutated cells .

HY-176492

E3 Ligase Ligand-linker Conjugate 193	E3 Ligase Ligand-Linker Conjugates	Cancer
E3 Ligase Ligand-linker Conjugate 193 is an E3 ligase ligand-linker conjugate that incorporates the VHL Ligase Ligand (HY-170353) and linker (HY-176491). E3 Ligase Ligand-linker Conjugate 193 can be used for synthesis of PROTAC pan-KRAS degrader-1 (HY-176489) .

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)) .

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KRAS degrader

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