CRK12-IN-1 is a potent CRK12 inhibitor.CRK12-IN-1 has insecticidal activity, with inhibitory effects on Trypanosoma brucei (T.b. brucei) and Trypanosoma congolense (T. congolense) with EC50s of 1.3 and 18 nM, respectively.CRK12-IN-1 kills the pathogenic cells rapidly.

CRK12-IN-2 is a potent inhibitor of CRK12.CRK12-IN-2 inhibits the parasite, with EC50 values of 3.2 and 0.08 nM for Trypanosoma congolense and Trypanosoma vivax, respectively.CRK12-IN-2 can be used for the prevention and treatment of trypanosomiasis in animals.

GSK126 (GSK2816126A) is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 nM).

CDK12-IN-6, a pyrazolotriazine compound, is a powerful inhibitor of CDK12. Its inhibitory activity is significant with an IC50 value of 1.19 μM when tested at high ATP concentration (2 mM). Notably, CDK12-IN-6 does not exhibit any inhibitory effect on CDK2/Cyclin E (IC50 >20 μM) and CDK9/Cyclin T1 (IC50 >20 μM) when tested under the same high ATP conditions (2 mM) (WO2021116178A1).

CDK12-IN-2 (CDK12 inhibitor 2) is an effective and selective inhibitor of CDK12 with an IC50 of 52 nM, >100 μM, >10 μM and 16 μM for CDK12, CDK2, CDK7, and CDK9. CDK12-IN-2 can be used in studies about the function of CDK12.

GSK121 is an inhibitor of selective PAD4.

CDK12-IN-3 is a selective CDK12 inhibitor (IC50: 491 nM in an enzymatic assay).

GSK1292263 is a GPR119 agonist and has been investigated for the treatment of DIABETES MELLITUS, TYPE 2.

CDK12-IN-5 is a potent CDK12 inhibitor with potential anticancer and antitumor activity, and can be used orally in the study of breast and ovarian cancer.

Histone H2BK12ac (1-22)-GGK-biotin amide (trifluoroacetate salt) can be used in related research in the field of life sciences, and its product number is T36095.

CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and non-covalent CDK9 inhibitor while avoiding ABC transporter-mediated efflux. It has a weak binding ability to CDK7/CyclinH complex (IC50> 1 μM).

UK122 is a highly effective and specific inhibitor of urokinase-type plasminogen activator (uPA) with an IC50 value of 0.2 μM. It displays negligible to minimal inhibition towards tissue-type plasminogen activator (tPA), plasmin, thrombin, and trypsin (all IC50 >100 μM). Functioning as a 4-oxazolidinone analogue, UK122 is an anticancer agent that effectively inhibits cancer cell migration and invasion.

GSK124576A is a bioactive chemical.

ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1]. In the in vitro kinase assay ASK120067 potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of ASK120067 against wild-type EGFR (EGFRWT) is 6 nM[1].ASK120067 selectively inhibits the growth of EGFR-mutant cell lines and exhibits potent antiproliferative activity in the mutant EGFR NSCLC cells, with IC50 values of 12 nM, 6 nM and 2 nM against NCI-H1975 (T790M mutation), PC-9, and HCC827 cells (sensitizing mutations), respectively. However, it shows moderate or weak anti-growth activities in A431, LoVo and A549 cells (EGFRWT), with IC50 values ranging from 338 nM to 1541 nM[1].ASK120067 (0.1-100 nM) inhibits the phosphorylation of EGFR at Tyrosine residue 1068 and its downstream signaling proteins AKT and ERK in NCI-H1975 cells (EGFRL858R/T790M) even at low dosage (0.1-1 nM). Additionally, ASK120067 inhibits p-EGFR and p-Akt and p-erk in EGFR WT A431 cell until the concentration reaches 10 to 100 nM[1]. ASK120067 (oral gavage; 5-20 mg/kg; once daily; 21 days) results in significantly regressed tumor growth, with a tumor growth inhibition (TGI) rate of 85.7%, and administration of 10 mg/kg ASK120067 causes dramatic tumor shrinkage with a TGI rate of 99.3%, exhibiting a similar potency with Osimertinib[1]. [1]. Tao Zhang, et al. Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance. Mol Cancer. 2020 May 13;19(1):90.

CDK12-IN-4, a pyrazolotriazine compound, exhibits potent inhibition of CDK12 by achieving an IC50 value of 0.641 μM, utilizing high ATP levels (2 mM). Notably, CDK12-IN-4 does not impact CDK2/Cyclin E (IC50 > 20 μM) or CDK9/Cyclin T1 (IC50 > 20 μM) under the influence of high ATP (2 mM) levels (WO2021116178A1).

PROTAC CDK12/13 Degrader-1 (7f) is a potent and selective dual degrader of the cell cycle protein-dependent kinases CDK12 (DC50: 2.2 nM) and CDK13 (DC50: 2.1 nM). Breast cancer.

L-Fucitol (1-Deoxy-D-galactitol) is a galactitol analogue isolated from Myristica fragrans (Nutmeg), inhibits galactitol-positive strains of Escherichia coli K12.

MraY-IN-1 (compound 12a) is a potent inhibitor (IC50: 140 μM) of the bacterial translocase MraY. MraY-IN-1 has antibacterial activity against Escherichia coli K12 (MIC50: 7 μg/ml), Bacillus subtilis W23 (MIC50: 12 μg/ml) and Pseudomonas fluorescens Pf-5 (MIC50: 46 μg/ml). /MraY-IN-1 can be used for antimicrobial studies.

MraY-IN-3 (12a) is a potent inhibitor of the bacterial translocase MraY (IC50: 140 μM). 46 μg/ml).

MraY-IN-1 (compound 12a) is a potent inhibitor of MraY, exhibiting an IC50 of 140 µM. This compound demonstrates antimicrobial activity, with MIC50 values of 7 µg/mL against Escherichia coli K12, 12 µg/mL for Bacillus subtilis W23, and 46 µg/mL in the case of Pseudomonas fluorescens Pf-5. MraY-IN-1 is utilized in anti-bacterial research [1].