Kras4B G12D-IN-1 is a Kras4B G12D inhibitor with anticancer effects. Kras4B G12D-IN-1 decreases Kras protein expression in mouse embryonic fibroblasts (MEF) expressing Kras4B G12D (WO2016179558A1, Comp 994566)[1].
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 (DC50s between 0.25 and 0.76 μM)[1][2].
MRTF/SRF-IN-1 (example 41) is an inhibitor of both myocardin-related transcription factor and serum response factor (MRTF/SRF). MRTF/SRF-IN-1 can be used for research for preventing cancer and fibrosis[1].
(S)-JDQ-443 is an isomer of JDQ-443 (HY-139612). JDQ-443 is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). JDQ-443 shows antitumor activity[1][2].
KRAS G12D inhibitor 5 is a KRAS G12D inhibitor for the potential treatment of pancreatic cancer.
KRAS G12C inhibitor 40 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 40 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021129824A1, compound 70)[1].
EHT 1864 is a small molecule inhibitor of Rac1 signaling; modulate γ-Secretase-mediated APP processing.IC50 value:Target: Rac1 inhibitorin vitro: EHT 1864 blocks Aβ 40 and Aβ 42 production but does not impact sAPPα levels and does not inhibit γ-secretase. Rather, EHT 1864 modulates APP processing at the level of γ-secretase to prevent Aβ40 and Aβ42 generation. This effect does not result from a direct inhibition of the γ-secretase activity and is specific for APP cleavage, since EHT 1864 does not affect Notch cleavage [1]. EHT 1864 specifically inhibited Rac1-dependent platelet-derived growth factor-induced lamellipodia formation. Furthermore, our biochemical analyses with recombinant Rac proteins found that EHT 1864 possesses high affinity binding to Rac1, as well as the related Rac1b, Rac2, and Rac3 isoforms, and this association promoted the loss of bound nucleotide, inhibiting both guanine nucleotide association and Tiam1 Rac guanine nucleotide exchange factor-stimulated exchange factor activity in vitro [2].in vivo: EHT1864 significantly reduces Aβ 40 and Aβ 42 levels in guinea pig brains at a threshold that is compatible with delaying plaque accumulation and/or clearing the existing plaque in brain [1].
KRAS G12C inhibitor 16 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 39, has an IC50 of 97 nM[1].
KRAS G12C inhibitor 47 (compound 8-1-1) is a potent KRAS G12C inhibitor with an IC50 of 0.172 µM. KRAS G12C inhibitor 47 shows p-ERK inhibition activities with IC50s of 0.046, 69.8 µM in MIA PaCA-2, A549 cells, respectively. KRAS G12C inhibitor 47 has the potential for the research of pancreatic, colorectal, and lung cancers[1].
KRAS G12C inhibitor 30 is a KRAS G12C inhibitor extracted from patent WO2021252339A1, compound 2. KRAS G12C inhibitor 30 can be used for the research of cancer[1].
KRAS G12C inhibitor 19 is a potent inhibitor of KRAS G12C. KRAS G12C inhibitor 19 significantly inhibits tumor growth (extracted from patent WO2021118877A1)[1].
(E/Z)-ZINC09659342 is an inhibitor of Lbc-RhoA interaction[1].
KRAS G12C inhibitor 36 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 36 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021121367A1, compound 1-2)[1].
KRAS G12C inhibitor 49 (Compound 3-2M) is an orally active KRAS G12C inhibitor. KRAS G12C inhibitor 49 shows antitumor activity[1].
KRAS G12C inhibitor 26 is a KRAS G12C inhibitor with antitumor effects (WO2021109737)[1].
KRAS G12C inhibitor 34 is a KRAS G12C inhibitor extracted from patent WO2021239058A1, compound Z1. KRAS G12C inhibitor 34 can be used for the research of cancer[1].
KRAS G12C inhibitor 39 is a potent inhibitor of KRAS G12C. KRas is a highly attractable target of the pharmaceutical industry for cancer research. KRAS G12C inhibitor 39 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2019099524A1, compound 494)[1].
KRAS G12C inhibitor 61 (Example 3) inhibits phospho-ERK 1/2 in MIA PaCa-2 cells with an IC50 value of 9 nM. KRAS G12C inhibitor 61 can be used for research of pancreatic, colorectal, and lung cancers[1].
PAT-IN-1 is a protein acyl transferases (PAT) inhibitor. PAT-IN-1 competitively inhibits Erf2 autopalmitoylation (WO2017011518A1; compound 13)[1].
AZA197 is a selective small molecule inhibitor of Cdc42.AZA197 suppresses colon cancer cell proliferation, cell migration, invasion and increases apoptosis by down-regulating the PAK1 and ERK signaling pathways in vitro. AZA197 reduces tumor growth and significantly increases mouse survival in SW620 tumor xenografts[1].
KRAS G12C inhibitor 27 is a KRAS G12C inhibitor with antitumor effects (WO2021109737)[1].
KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
Tyrphostin 8 is a tyrosine kinase, with an IC50 of 560 μM for EGFR kinase. Tyrphostin 8 is also a GTPase inhibitor. Tyrphostin 8 can inhibit the protein serine/threonine phosphatase calcineurin (IC50=21 μM)[1][2][3].
SOS1-IN-15 (Compound 37) is an orally active SOS1 inhibitor with an IC50 of 5 nM. SOS1-IN-15 is a promising drug candidate for the research of KRAS-driven cancer[1].
Kobe0065 is a novel and effective inhibitor of Ras-Raf interaction, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46±13 μM.
6CEPN is a Cyclooxygenase-1 inhibitor that acts by suppressing colorectal cancer growth.
KRpep-2d is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research[1].
KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
pan-KRAS-IN-2 (compound 6) is a pan inhibitor of with IC50s ≤10 nM for KRAS WT and mutants (G12D, G12C, G12V, G12S, G12A, Q61H), and ＞10 μM for KRAS G13D, respectively[1].
Manumycin A is an antibiotic. Manumycin A acts as a selective, competitive inhibitor of protein farnesyltransferase (FTase) with respect to farnesylpyrophosphate (Ki =1.2 μM), and as a noncompetitive inhibitor with respect to the Ras protein. Manumycin A induces apoptosis and exerts antitumor activity[1] [2][3].