PKMYT1 Inhibitor

lunresertib (RP-6306) is a potent, selective and orally active PKMYT1 inhibitor with an IC₅₀ of 14 nM. lunresertib shows a high degree of selectivity over other kinases in cellular binding assays. lunresertib shows anticancer effects.

PD173952 is a tyrosine kinases inhibitor with IC₅₀s of 0.3, 1.7 and 6.6 nM against Lyn, Abl and Csk, respectively. PD173952 is also a potent Myt1 kinase inhibitor with a K_i of 8.1 nM. PD173952 induces apoptosis.

(Rac)-lunresertib (compound 181) is a potent membrane-associated tyrosine and threonine-specific cdc2-inhibitory kinase (Myt1) (Gene name PKMYT1) inhibitor with an IC₅₀ of <10 nM. (Rac)-lunresertib (compound 181) has anticancer effects.

PKMYT1-IN-8 (Compound 137) is the inhibitor for PKMYT1 with an IC₅₀ of 9 nM. PKMYT1-IN-8 inhibits EPHB3, EPHA1, KIT, EPHB1, EPHA2, EPHA3, and EPHB2with IC₅₀s of 1.79, 3.17, 4.29, 6.32, 6.83, 8.10, and 10.9 μM, respectively. PKMYT1-IN-8 inhibits the proliferation of cancer cell OVCAR3 with GI₅₀ of 2.02 μM.

Myt1-IN-1 is a potent membrane-associated tyrosine and threonine-specific cdc2-inhibitory kinase (Myt1) (Gene name PKMYT1) inhibitor with an IC₅₀ of <10 nM. Myt1-IN-1 has anticancer effects (WO2021195782A1; compound 132).

PKMYT1-IN-15 is an orally active PKMYT1 inhibitor with an IC₅₀ of 6.02 nM. PKMYT1-IN-15 inhibits the phosphorylation of CDK1 at Thr14. As an antiproliferative agent, DNA damage inducer and antitumor agent, PKMYT1-IN-15 triggers replication-associated DNA damage and cell death in CCNE1-amplified cancer cells, and suppresses tumor growth in the OVCAR3 xenograft model. PKMYT1-IN-15 can be used for the research of CCNE1-amplified cancers (e.g., ovarian cancer, breast cancer).

BAA-065 is a selective and orally active PKMYT1 inhibitor with an IC₅₀ of <50 nM. BAA-065 inhibits cancer cells proliferation, induces γH2AX expression and DNA damage. BAA-065 inhibits tumor growth in OVCAR3 xenograft mice. BAA-065 can be used for the research of cancer, such as ovarian cancer.

WEE1/PKMYT1-IN-4 is a selective WEE1/PKMYT1 inhibitor, with IC₅₀ values of 0.185 μM and 2.2 nM for human WEE1 and PKMYT1, respectively. WEE1/PKMYT1-IN-4 inhibits phosphorylation of CDK1 at T14 and Y15, disrupting the G2/M cell cycle checkpoint. WEE1/PKMYT1-IN-4 can be used for the research of colorectal cancer and amplified breast cancer.

Myt1-IN-3 is a potent membrane-associated tyrosine and threonine-specific cdc2-inhibitory kinase (Myt1) (Gene name PKMYT1) inhibitor with an IC₅₀s of <10 nM (WO2021195782 A1, compound 95).

PKMYT1-IN-1 (Compound 1) is an inhibitor for membrane-associated tyrosine and threonine kinase (PKMYT1), with an IC₅₀ of 8.8 nM. PKMYT1-IN-1 inhibits proliferation of tumor cell HCC1569 with IC₅₀ of 42 nM.

(R)-lunresertib is a membrane-associated tyrosine and threonine-specific cdc2-inhibitory kinase (Myt1) (Gene name PKMYT1) inhibitor, with IC₅₀ of 1360 nM. (R)-lunresertib can be used in the study of Myt1-mediated cancers.

WEE1/PKMYT1-IN-1 (compound 75) is a potent and orally active WEE1 and PKMYT1 inhibitor. WEE1/PKMYT1-IN-1 shows antiproliferation activity.

Myt1-IN-2 is a potent membrane-associated tyrosine and threonine-specific cdc2-inhibitory kinase (Myt1) (Gene name PKMYT1) inhibitor with an IC₅₀ of <10 nM. Myt1-IN-2 has anticancer effects (WO2021195782A1; compound 28).

PKMYT1-IN-9 is a highly selective and orally active PKMYT1 inhibitor (IC₅₀: 4.4 nM). PKMYT1-IN-9 shows more selective for PKMYT1 than WEE1 (IC₅₀: 32.4 μM). PKMYT1-IN-9 exhibits antitumor activity.

PKMYT1-IN-2 (compound 2) is a potent PKMYT1 inhibitor with an IC₅₀ of 5.7 nM. PKMYT1-IN-2 inhibits the growth of HCC1569 cells with an IC₅₀ of 22 nM.

WEE1/PKMYT1-IN-2 is the axial chiral P configuration of WEE1/PKMYT1-IN-1 (HY-169946). WEE1/PKMYT1-IN-1 is a potent and orally active WEE1 and PKMYT1 inhibitor. WEE1/PKMYT1-IN-1 shows antiproliferation activity.

PKMYT1-IN-10 is a selective PKMYT1 inhibitor with an IC₅₀ of 3 nM. PKMYT1-IN-10 inhibits colony formation, induces apoptosis, and induces S-phase cancer cell cycle arrest. PKMYT1-IN-10 exhibits liver microsomal stability, favorable plasma stability, minimal CYPs inhibition. PKMYT1-IN-10 can be used for the studies of ovarian cancer and breast cancer.

WEE1/PKMYT1-IN-3 is the axial chiral M configuration of WEE1/PKMYT1-IN-1 (HY-169946). WEE1/PKMYT1-IN-1 is a potent and orally active WEE1 and PKMYT1 inhibitor. WEE1/PKMYT1-IN-1 shows antiproliferation activity.

PKMYT1-IN-12 (Compound 4) is a selective inhibitor of PKMYT1, with an IC₅₀ of 2.6 nM. PKMYT1-IN-12 can effectively inhibit the phosphorylation of CDK1, with an IC₅₀ of 44 nM. PKMYT1-IN-12 is a target protein ligand that can be used for the synthesis of PROTAC D16-M1P2 (HY-180485).

PD-166285 is a PKMYT1 inhibitor, with an IC₅₀ value of 17 nM. PD166285 shows strong antiproliferative effects against CCNE1-amplified OVCAR3 cells (IC₅₀ = 0.14 μM) and HCC1569 cells (IC₅₀ = 0.21 μM). PD166285 induces apoptosis and arrests CCNE1-amplified HCC1569 cells at the G1/S phase of the cell cycle. PD166285 can be used for the research of PKMYT1-targeted therapies for CCNE1-amplified cancers.