SRI-011381 hydrochloride is an agonist of the transforming growth factor-beta (TGF-β) signalling pathway and exhibits neuroprotective effects with the potential to treat Alzheimer's disease. It also increases fibronectin expression in the NIH‐3T3 cells stimulated by metformin.

ZCL279 is a small molecule modulator (SMM) that inhibits Cdc42-intersectin (ITSN) interaction. ZCL279 can activate Cdc42 (a cytoplasmic small GTPase in the Ras superfamily) at lower concentrations (<10 μM) and significantly inhibit it at higher concentrations (<10 μM).

VVD-699 is a covalent RAS-PI3K inhibitor. VVD-699 covalently binds to cysteine 242 in the RAS binding domain of PI3K p110α, thereby blocking the ability of RAS to activate PI3K activity. VVD-699 is able to inhibit the growth of RAS-mutated and HER2-overexpressing tumors. VVD-699 can be used to study cancers associated with RAS mutations (e.g., H358 lung cancer cells, A549 cells, FaDu cells).

Sosimerasib is the inhibitor for kirsten rat sarcoma viral oncogene homolog (KRAS) and exhibits antineoplastic activity.

SOF-436 is a KRAS inhibitor that inhibits SOS1-mediated KRAS nucleotide exchange (IC50 = 60 μM) and the binding of KRAS to the effector protein RAF. SOF-436 can be used in cancer research.

RMC-5127 is an orally active and brain-penetrant mutant-selective tri-complex RASG12V inhibitor. RMC-5127 non-covalently binds to cyclophilin A (CypA), forming a binary complex that engages RASG12V(ON) to form a high-affinity tri-complex, sterically inhibiting RAS binding . RMC-5127 inhibits the RAS pathway in KRASG12V mutant cancer cells, reducing cell proliferation and inducing apoptosis. RMC-5127 is promising for research of cancers with RAS mutations, such as non-small cell lung cancer.

RMC-4998 formic is an orally active inhibitor targeting the active or GTP-bound state of the KRASG12C mutant. RMC-4998 formic can form a ternary complex with intracellular CYPA and the activated KRASG12C mutant, with an IC50 value of 28 nM. RMC-4998 formic can inhibit ERK signaling in KRASG12C mutant cancer cells and induce apoptosis. RMC-4998 formic can be used for tumor research.

KRASG12C IN-16 (Compound SK-17) is a selective, covalent and an orally active KRASG12C inhibitor. KRASG12C IN-16 induces Apoptosis. KRASG12C IN-16 effectively prevents the activation of MAPK and PI3K/mTOR signaling pathways. KRASG12C IN-16 displays anti-tumor activity against pancreatic cancer.

KRASG12C IN-15 (Compound 21) is the orally active inhibitor for KRASG12C, and inhibits SOS1-mediated GDP/GTP exchange with an IC50 of 19 nM. KRASG12C IN-15 inhibits the phosphorylation of ERK with IC50 of 0.051 μM. KRASG12C IN-15 inhibits the cell viability of KRASG12C mutated MIA PaCa-2 with IC50 of 0.023 μM. KRASG12C IN-15 exhibits antitumor effect in MIA PaCa-2 xenograft mouse models.

INCB159020 is an orally active KRAS G12D inhibitor with a KRAS G12D SPR value of 2.2 nM. INCB159020 has antitumor activity.

Ibetazol is an inhibitor for importin β1 (KPNB1), that inhibits that binds to Cys585 of importin β1, inhibits the importin β1 mediated nuclear import with an EC50 of 6.1 µM.

AZD0022 is a selective and orally active KRASG12D inhibitor. AZD0022 inhibits KRAS pathway suppression in the GP2D xenograft model.

AMG410 is a non-covalent and selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D. AMG410 shows greater than 100-fold selectivity against both HRAS and NRAS. AMG410 is a dual GTP(on)- and GDP(off)-state inhibitor (Kd(GDP-state) of 1 nM; Kd(GTP-state) of 22 nM). AMG410 blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells. AMG410 can be used for the study of colorectal, pancreatic, and lung cancers.

6-Thio-GTP (tetrasodium) is a Vav1-Rac inhibitor. 6-Thio-GTP (tetrasodium) inhibits TCR-stimulated T cell proliferation and CD28-mediated T cell survival. 6-Thio-GTP (tetrasodium) has an immunosuppressive effect in a mouse cardiac allograft transplant model and prolongs cardiac allograft survival.

Flezurafenib is an oral inhibitor of pan-RAF with potential antineoplastic activity.

Methylcarbamyl PAF C-8 is resistant to the degradation function of platelet-activating factor acetylhydrolase (PAF-AH). It has a half-life of more than 100 minutes in platelet-poor plasma and possesses the activity of inducing platelet aggregation. In NRK-49 cells overexpressing the PAF receptor, Methylcarbamyl PAF C-8 can induce the expression of c-myc and c-fos, and activate mitogen-activated protein kinase (MAPK). Additionally, Methylcarbamyl PAF C-8 can induce cell cycle arrest in the G1 phase. Methylcarbamyl PAF C-8 holds promise for research in the fields of cardiovascular diseases and anti-cancer therapy.

JX10 is a senomorphic agent. JX10 suppresses the expression of p38 MAPK and NF-κB. JX10 exhibits competent antiaging effects in C. elegans, senescent cells, and aged mice.

JD123 inhibits JNK1 activity and the expression of cJun (1-135). JD123 is a ATP-competitive p38-γ MAPK inhibitor, but not effect to ERK1, ERK2, or p38-α, p38-β or p38-δ..

DB-10 is a pro-agent of 3-nbutylphthalide (NBP). DB-10 has significantly high uptake ability via pyrilamine cationic transporters in the temperature and energy dependent manner in cells. DB-10 improves the survival rate of cells. DB-10 could rapidly convert into active original agent and increase the accumulation in the brain in vivo. DB-10 can be used for ischemic stroke study.

NUCC-0200808 (Compound 12g) is an inhibitor of MNK1 with an IC50 of 42 nM. NUCC-0200808 reduces eIF4E phosphorylation and cell viability in AML cells, and induces apoptosis. NUCC-0200808 holds promise for research in the field of leukemia.

HSND80 (Compound 1) is an orally active inhibitor of MNK/p70S6K, with Kd values of 44 nM against MNK1 and 4 nM against MNK2. HSND80 has a longer target residence time of 45 mins and 58 mins against MNK1 and MNK2 respectively. HSND80 can suppress non-small cell lung cancer (NSCLC) both in vitro and in vivo, and suppress Triple-Negative Breast Cancer (TNBC) in vitro.

Famlasertib is a potent, brain-penetrant MAP4K inhibitor with IC50s value of 0.3 nM, 23.7 nM, and 44.7 nM for HGK (MAP4K4), MLK3, and MLK1, respectively. Famlasertib shows motor neuron protection and anti-inflammatory properties. Famlasertib can be used for the study of amyotrophic lateral sclerosis (ALS).

AZ3246 is an orally active and selective inhibitor of HPK1 with an IC50 < 3 nM. AZ3246 induces IL-2 secretion in T cells with an EC50 of 90 nM. AZ3246 is a low-clearance antitumor compound.

SET-171 is a JNK (c-Jun N-terminal kinase) inhibitor that exhibits significant anticancer activity and lipid metabolism regulation by inhibiting liver pyruvate kinase (PKL) expression. In anticancer studies, SET-171 shows IC50 values of 8.82 μM and 2.97 μM against HepG2 and Huh7 cell lines, respectively, indicating high cytotoxicity. Additionally, in non-alcoholic fatty liver disease (NAFLD)-related studies, SET-171 significantly reduces triacylglycerol (TAG) levels and inhibits the expression of steatosis-related proteins. SET-171 holds promise for research on hepatocellular carcinoma (HCC) and NAFLD.

JD118 is a JNK inhibitor. JD118 inhibits JNK1 activity and the expression of cJun (1–135).

(3S)-Tanzisertib (hydrochloride) ((3S)-CC-930 (hydrochloride)) is an orally active JNK inhibitor (IC50 values for JNK1, JNK2, and JNK3 are 61, 7, and 6 nM, respectively). (3S)-Tanzisertib (hydrochloride) selectively inhibits ERK1, p38α, and EGFR (IC50 = 0.48, 3.4, and 0.38 μM, respectively). (3S)-Tanzisertib (hydrochloride) inhibits LPS-induced TNFα production in an acute rat PK-PD model. (3S)-Tanzisertib (hydrochloride) can be used in idiopathic pulmonary fibrosis (IPF) research.

SKLB-D18 is a potent and selective inhibitor of ERK1/2 and ERK5, with IC50s of 38.69, 40.12 and 59.72 nM, respectively. SKLB-D18 is also an autophagy agonist, plays a role in mTOR/p70S6K and NCOA4-mediated ferroptosis, which may mitigate multidrug resistance. SKLB-D18 exhibits significantly superior efficacy in vitro and in vivo against triple-negative breast cancer (TNBC).

ERK2 IN-5 (Compound 5g) is an inhibitor for ERK2, and exhibits good affinity to ERK2 and JNK3 with Ki of 86 and 550 nM.

Boc3Arg is the tert-butyl carbamate-protected arginine. Boc3Arg is an efficient tag to induce degradation through directly localizing the protein to the 20S proteasome.

bpV(bipy) hydrate is the inhibitor for phosphoinositide 3-phosphatase (PTEN) and protein tyrosine phosphatases (PTP-β and PTP-1B) with IC50s of 18, 60.3, and 164 nM, respectively.