Ras Degrader

KRAS degrader-1 is a potent KRAS degrader. KRAS degrader-1 targets specific proteins for degradation via the autophagy-lysosomal degradation pathway. KRAS degrader-1 is suitable for use in cancer research. (Blue: KRAS G12C-IN-72 (HY-128414); Black: Linker (HY-175587); Pink: 5-Iodoindolin-2-one (HY-76986); Blue + Black: KRAS ligand-Linker Conjugate 7 (HY-175586)).

YF135 is a KRAS^G12C PROTAC degrader that mediates proteasomal degradation of KRAS^G12C in a reversible manner. In KRAS^G12C-mutant H358 and H23 lung cancer cells, the DC₅₀ values of YF135 for KRAS degradation are 3.61 μM and 4.53 μM, respectively. YF135 attenuates the pERK signaling pathway in cancer cells. YF135 is applicable for lung cancer-related research.

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.

CH091138 is an orally active VHL-recruiting PROTAC degrader targeting KRAS^G12D, with a DC₅₀ of 148.3 nM in HeLa cells. CH091138 inhibits cancer cell proliferation and tumor growth by mediating the ubiquitin-proteasome degradation of KRAS^G12D. CH091138 can be used in research related to pancreatic cancer and colorectal cancer.

PROTAC K-Ras Degrader-7 is a potent PROTAC K-Ras degrader. PROTAC K-Ras Degrader-7 degrades K-Ras through recruiting the Keap1 E3 ubiquitin ligase. PROTAC K-Ras Degrader-7 can be used for research in pancreatic and colorectal cancers.

RP04340 is an orally active, selective pan-KRAS PROTAC degrader. RP04340 hijacks the CRBN E3 ligase and the cellular proteasome system to degrade KRAS, without degrading HRAS, NRAS, or common CRBN neosubstrates. RP04340 inhibits KRAS downstream signaling pathways, including pERK and DUSP6. RP04340 exhibits anticancer activity in various KRAS-mutant cancers. RP04340 can be used to study kras-driven cancers, including pancreatic ductal adenocarcinoma, colorectal cancer, and lung adenocarcinoma.

YN14-H is a potent mutant KRAS^G12C PROTAC degrader. The DC₅₀ values of YN14-H in NCI-H358 and MIA PaCa-2 cells are 28.9 nM and 18.1 nM, respectively, with corresponding IC₅₀ values of 42 nM and 21 nM. YN14-H degrades KRAS^G12C in a ubiquitin-proteasome system-dependent manner, thereby significantly inducing apoptosis and inhibiting cell migration. YN14-H can be used for targeting tumors with KRAS^G12C mutations (such as non-small cell lung cancer, pancreatic cancer, etc.).

(R)-ACBI-4 is an isomer of ACBI-4 (HY-176792). ACBI-4 is a selective GTP-loaded active state of KRAS (KRAS(on)) PROTAC degrader. ACBI-4 has significant anti-proliferative effect and potently degrades multiple KRAS mutants in cancer cells, such as KRASG12R.

KRAS G12D ligand-3 is a KRAS G12D PROTAC ligand. KRAS G12D ligand-3 can be conjugated with E3 ligase Ligand (HY-170348) and linke (HY-W895436) to synthesize KRAS G12D PROTAC degrader MS243 (HY-181728). MS243 can be used for cancer research.

LC-2 epimer is a differential isomer of LC-2. LC-2 is a mutation-selective PROTAC depressant for KRAS and contains a ligand for the von Hippel Lindau E3 ligase linked to the KRAS inhibitor MRTX849.

PROTAC SOS1 degrader-10 is a SOS1 PROTAC degrader dependent on CRBN and the proteasome. PROTAC SOS1 degrader-10 degrades SOS1 in KRAS-mutant cancer cells SW620, A549 and DLD-1, with DC₅₀ values of 2.23, 1.85 and 7.53 nM, respectively. PROTAC SOS1 degrader-10 inhibits ERK phosphorylation. PROTAC SOS1 degrader-10 suppresses the proliferation of KRAS-mutant cancer cells via antiproliferative activity. PROTAC SOS1 degrader-10 can be used in studies related to KRAS-mutant cancers.

KVL‑9 is an intermediate for constructing KRAS-degrading antibody-drug conjugates (DAC), consisting of a KRAS small-molecule binder, a spacer, a VHL-recruiting ligand, and a cleavable antibody linker. By conjugating with tumor antigen-targeting antibodies, KVL‑9 enables antigen-dependent intracellular delivery and induces VHL‑mediated ubiquitin‑proteasome degradation of KRAS protein. KVL‑9 can be used for the synthesis of DACs. KVL‑9 is applicable to cancer research.

KY1022 is a small molecule destabilizing Ras via targeting the Wnt/β-catenin pathway. KY1022 can inhibit cellular EMT, metastasis and apoptosis. KY1022 can be used for the research of metastatic colorectal cancer.

YN14 mixture of diastereomers is a diastereomer mixture of YN14 (HY-155356). YN14 is a KRAS^G12C PROTAC degrader that recruits E3 ubiquitin ligase to induce the polyubiquitination and proteasomal degradation of KRAS^G12C. YN14 induces tumor cell apoptosis, cell cycle arrest, and cell migration inhibition. YN14 exhibits in vivo antitumor proliferative activity in tumor cell xenograft nude mice. YN14 can be used in cancer-related research.

BJP-06-005-3 is a selective Pin1 inhibitor with a K_i value of 48 nM. BJP-06-005-3 induces the degradation of mutant KRAS. BJP-06-005-3 inhibits pancreatic ductal adenocarcinoma via the Pin1-mediated pathway. BJP-06-005-3 is used in studies related to KRAS-mutant pancreatic ductal adenocarcinoma.