KRAS-IN-48 (Compound 1-01) is a KRAS mutant inhibitor, with Kd values of 2.58 nM and 5.49 μM for KRAS-G12D and KRAS-G12V, respectively. KRAS-IN-48 can be used in the research of cancer.

EED-IN-5 is an orally active, EZH2-selective trisubstituted pyridine-based EED-H3K27me3 inhibitor and immunomodulator with anti-inflammatory activity. The IC50 value of EED-IN-5 against EED is 28.21 nM. In mouse models, EED-IN-5 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-5 decreases the infiltration of specific dendritic cells, macrophages and T cells into the spinal cord and brain. EED-IN-5 exhibits hERG inhibitory activity, shows negative results in the Mini-Ames test, and causes no obvious toxicity upon long-term high-dose administration. EED-IN-5 can be used for the research of multiple sclerosis.

KRASG12C IN-17 is an orally active covalent KRASG12C inhibitor, showing strong inhibitory activity in KRASG12C-mutant cancer cells (NCI-H23 IC50 = 0.7 nM; NCI-H358 IC50 = 0.5 nM). KRASG12C IN-17 covalently and irreversibly binds to KRASG12C with > 96% modification efficiency in both GDP-bound and GMPPNP-bound conformations. KRASG12C IN-17 can be used for studies of KRAS-driven cancers, including colorectal cancer.

KRASG12C IN-19 is a selective and orally active KRASG12C inhibitor. KRASG12C IN-19 exerts potent antiproliferative activity against the KRASG12C-mutant non small cell lung cancer (NSCLC) cell line H358 with an IC50 of 7.6 nM, and effectively suppresses downstream ERK phosphorylation (IC50 = 24.06 nM). KRASG12C IN 19 has no significant inhibitory activity against KRASG12V and KRASG12D-mutant cancer cells (PANC 1, Panc, AsPC 1, and GP2d cells) with IC50 > 10,000 nM. KRASG12C IN-19 rapidly forms a covalent bond with KRASG12V-GDP, leading to dose-dependent inhibition of the downstream KRAS pathway. KRASG12C IN 19 can be employed for research in KRASG12C driven cancers, including non small cell lung cancer, pancreatic cancer, and colorectal cancer.

KMO-IN-1 is a KMO inhibitor with a mean pIC50 of 8.5 against KMO. KMO-IN-1 can be used in the research of acute pancreatitis.

KIF18A-IN-18 (Compound I) is a KIF18A inhibitor. KIF18A-IN-18 can be used in the research of chromosomally unstable tumors.

KG-FP-003 is a highly potent, selective, and durable TEAD PROTAC degrader (TEAD1 DC50 = 6 ± 4 nM, TEAD2 DC50 = 68 ± 15 nM, TEAD3 DC50 = 12 ± 5 nM, TEAD4 DC50 = 7 ± 5 nM). KG-FP-003 promotes ubiquitination and degradation of TEAD. KG-FP-003 exhibits anticancer activity against mesothelioma and ovarian cancer. (Pink: Ligands for Target Protein for PROTAC and TEAD ligand ; Blue: Ligands for E3 Ligase and Cereblon E3 ligase ligand; Black: linker).

Ketopantolactone is a biochemical reagent. Ketopantolactone interacts with modified Pt/Al2O3.

Keap1/Nrf2/ARE activator 2 is an activator of Keap1/Nrf2/ARE pathway and non-competitively inhibits AChE with an IC50 of 14.79 μM and a Ki of 1.35 μM. Keap1/Nrf2/ARE activator 2 promotes Nrf2 nuclear translocation, leading to antioxidant gene upregulation and enhanced cellular defense against oxidative stress. Keap1/Nrf2/ARE activator exhibits robust neuroprotection against both H2O2- and Scopolamine (SCA)-induced injury in PC12 cells. Keap1/Nrf2/ARE activator 2 ameliorates memory impairment and the neuro-inflammation associated with SCA-initiated cognitive dysfunction in a zebrafish model. Keap1/Nrf2/ARE activator 2 can be used for the research of Alzheimer's disease.

KB528 is a p300/CBP histone acetyltransferase (KAT) inhibitor with low nM IC50 values against human p300 and CBP, and exhibits selectivity over other KAT family members. KB528 modulates the IRF4 transcriptional network, downregulates the expression of IRF4, MYC, CAV2 and IGLL5, and reduces the protein level of IKZF3. KB528 potently induces apoptosis in multiple myeloma cells. KB528 is applicable to research related to multiple myeloma.

JNK3-IN-10 is a blood-brain barrier-impermeable JNK3 inhibitor (IC50=0.257 nM) with over 400-fold selectivity over JNK1. JNK3-IN-10 blocks the JNK3-mediated signaling pathway downstream of TGF-β1, inhibits TGF-β1-induced phosphorylation of c-Jun, reduces the expression of pro-fibrotic markers, and restores the expression of the epithelial protein E-cadherin. JNK3-IN-10 exhibits low cytotoxicity, anti-fibrotic, cytoprotective and renoprotective effects, and alleviates albuminuria, glomerulosclerosis and podocyte foot process fusion. JNK3-IN-10 can be used for the research of chronic kidney disease, glomerulosclerosis and adriamycin-induced nephropathy.

JAK2-IN-15 is an orally active, potent, selective JAK2 inhibitor (IC50 = 1.17 nM). JAK2-IN-15 can inhibit the AK2-STAT signaling pathway. JAK2-IN-15 significantly improves key pathological indicators such as hematocrit and splenomegaly in an Epoetin beta (rhEPO)-induced mouse model. JAK2-IN-15 can be used for the study of Polycythemia Vera (PV).

J-104118 is a potent and orally active squalene synthase (SQS) inhibitor with an IC50 of 0.52 nM. J-104118 inhibits cholesterol synthesis in mice. J-104118 can be used for cholesterol-lowering research.

ITRI-90 is an orally active androgen receptor (AR) PROTAC degrader. ITRI-90 effectively degrades both full-length AR (AR-FL) and the splice variant AR-V7 protein via the ubiquitin-proteasome system, thereby inhibiting AR transcriptional activity and the target gene expression. ITRI-90 significantly inhibits the proliferation of prostate cancer cells and induces apoptosis, include Enzalutamide-resistant growth cell. ITRI-90 exhibits favorable pharmacokinetic properties and demonstrates potent antitumor efficacy in vivo. ITRI-90 can be used for prostate cancer research.

ISR activator 3 (Compound cc81) is the active metabolite of A8. ISR activator 3 activates the integrated stress response (ISR) by binding to RIG-I (KD ≈ 0.55 μM), without inducing lipid droplet clearance. ISR activator 3 enhances the interferon response under viral mimicry signals. ISR activator 3 can be used for research on neurodegenerative diseases and immune stress.

Iprazochrome is a serotonin antagonist. Iprazochrome can be used in prophylaxis of migraine.

Inolitazone hydrochloride hydrate (Efatutazone hydrochloride hydrate) is a novel PPARγ high-affinity agonist, with an EC50 value one-fiftieth that of Rosiglitazone, and shows no inhibitory effect on RIE cells that do not express PPARγ. Inolitazone hydrochloride hydrate can be used in the research of cancer.

IL-17-IN-7 (Compound 23) is a IL-17 inhibitor with a pIC50 of 7.1 against IL-17A.

IKKβ-IN-7 is an IKKβ inhibitor with an IC50 value of 9.44 μM. IKKβ-IN-7 induces DNA damage, S-phase cell cycle arrest, ROS accumulation, mitochondrial membrane potential loss, and apoptosis. IKKβ-IN-7 inhibits phosphorylation of p65 and IκBα, suppresses p65 nuclear translocation, and regulates NF-κB-controlled genes. IKKβ-IN-7 suppresses tumor growth in xenograft models and shows activity against colorectal cancer with low normal cell cytotoxicity. IKKβ-IN-7 can be used for the research of colorectal cancer.

IDO1-IN-30 (Compound (R)-100) is a potent and highly selective IDO1 inhibitor. IDO1-IN-30 has an IC50 of 4.8 nM to IDO1 in SKOV3 cells. IDO1-IN-30 does not show significant cytotoxicity at 25 µM in HepG2 cells. IDO1-IN-30 can eliminate inhibition of CYP450 enzymes (such as 3A4, 2C9, 2D6). IDO1-IN-30 can be used for research on cancer and inflammatory conditions.

IDO1/TDO-IN-11 (Compound Y-13) is a dual IDO1 and TDO inhibitor, with an IC50 of 2.87 μM against hIDO1 and an IC50 of 0.08 μM against hTDO. IDO1/TDO-IN-11 inhibits NO production and ROS production. IDO1/TDO-IN-11 alleviates cellular neuroinflammatory damage and ameliorates Parkinson's disease. IDO1/TDO-IN-11 is applicable to research related to Parkinson's disease.

ICI-170777 is an orally active cardiotonic agent. ICI-170777 enhances cardiac contractility and induces arteriovenous dilation in animal models of congestive heart failure. ICI-170777 can be used in research on cardiovascular and cerebrovascular diseases such as heart failure.

ICD inducer-2 is a immunogenic cell death inducer. ICD inducer-2 binds to the colchicine binding site on tubulin to inhibit tubulin polymerization. ICD inducer-2 exhibits broad-spectrum antiproliferative activity across multiple cancer cell lines. ICD inducer-2 inhibits cells migration, causes G2/M phase and induces apoptosis. ICD inducer-2 promotes infiltration of CD4+ and CD8+ T cells into the tumor microenvironment. ICD inducer-2 downregulates antiapoptotic protein Bcl-2, upregulates proapoptotic proteins Bax and Bim-1, and increases cleaved caspase 3, cleaved caspase 9, and cleaved PARP levels. ICD inducer-2 overcomes paclitaxel resistance in xenograft models and achieves tumor growth inhibition. ICD inducer-2 can be used for the research of cancer, such as lung carcinoma.

IC-87361 is a DNA-dependent protein kinase (DNA-PKcs) inhibitor and radiosensitizer. IC-87361 inhibits the catalytic activity of DNA-PKcs and blocks non-homologous end joining (NHEJ) DNA double-strand break repair. IC-87361 can be used for the research of lung cancer and melanoma.

Ibopamine (SB 7505) hydrochloride is an orally active dopamine derivative. Ibopamine hydrochloride exerts agonistic effects on α, β adrenergic receptors and dopaminergic receptors. Ibopamine hydrochloride can be hydrolyzed to produce the active metabolite Epinine. Ibopamine hydrochloride possesses positive inotropic and vasodilatory effects, which can improve hemodynamics and renal function in heart failure models. Ibopamine hydrochloride has good safety profile and can be used in the research of diseases such as congestive heart failure.

IACS-56676 is a selective NRASG12D inhibitor with a target Kd of 0.031 μM. IACS-56676 stabilizes the p-loop, maintains key interactions with Asp12, Gly60 and Asp69, and achieves selectivity over wild-type KRAS through substitution targeting Leu95. IACS-56676 can be used for research on melanoma, hematologic malignancies and thyroid cancer.

Hydrotecan-NH-L-Ala-L-Val-L-Gln(CO-C5-succinimide)-D-glucitol (Example 9) is a conjugate of the ADC toxic molecule and the linker, where the toxic molecule part is Hydrotecan, and the linker part is Mc-Glu(D-Glucamine)-val-ala .

H-Tyr-AMC is a fluorogenic substrate for tyrosine aminopeptidases. H-Tyr-AMC is an inhibitor of tobacco and potato hydroxycinnamoyl-CoA:tyramine N-(hydroxycinnamoyl)transferase (THT) with Ki values of 0.72 μM (tobacco) and 0.42 μM (potato).

Hsp90-IN-47 (Compound C15) is a Hsp90 inhibitor and antifungal agent, with an IC50 of 0.014 μM against Hsp90α. When combined with Fluconazole, Hsp90-IN-47 exerts significant synergistic antifungal effects against fluconazole-resistant Candida albicans 0304103. Hsp90-IN-47 exhibits antitumor activity against acute myeloid leukemia and non-small cell lung cancer.

Hsp90-IN-43 (Compound 12) is a Hsp90-TPR2A interaction inhibitor with an IC50 of 360 nM and a Kd of 928 nM. Hsp90-IN-43 effectively inhibits the proliferation of BT474 cells. Hsp90-IN-43 can be used for the study of breast cancer.