pocket — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T8561	Apcin		APC
	Apcin is a potent and competitive inhibitor of anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substr...		APC
T16670	PS210		PDK
	PS210 is a potent and selective activator of PDK1 (Kd: 3 μM), specifically targeting the PIF-binding pocket of PDK1, without acting against other protein kinases such as S6K, PKB/Akt, or GSK3. Its prodrug, PS423, serves ...		PDK
T2301	SB 202190	FHPI,SB202190	Apoptosis , p38 MAPK , Autophagy
	SB 202190 (FHPI) is a p38 MAPK inhibitor that inhibits p38α and p38β2 (IC50=50/100 nM) selectively and cell-permeably. SB 202190 has antitumor activity and also induces the differentiation of human embryonic stem cells i...		Apoptosis , p38 MAPK , Autophagy
T9627	PHD-1-IN-1		HIF/HIF Prolyl-Hydroxylase
	PHD-1-IN-1 is a potent inhibitor of hypoxia-inducible factor prolylhydroxylase domain-1 (PHD-1) enzyme(IC50 = 0.034 μM).		HIF/HIF Prolyl-Hydroxylase
T8719	SC99		Apoptosis , JAK , STAT
	SC99 is a selective inhibitor of JAK2-STAT3 activation. SC99 downregulates the expression of STAT3-modulated genes.SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activiti...		Apoptosis , JAK , STAT
T23969	DCAI		Others
	DCAI is an inhibitor of nucleotide exchange and nucleotide release acting by binding to the pocket adjacent to the Ras-SOS interface.		Others
T10533	BI-2852		Ras
	BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) with nanomolar affinity. BI-2852 is leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.		Ras
T15579	INDY	1-(3-ethyl-5-hydroxy-1,3-benzothiazol-2-ylidene)propan-2-one	DYRK
	INDY is an ATP-competitive inhibitor of Dyrk1A and Dyrk1B with IC50s of 0.24 μM and 0.23 μM and a Ki of 0.18 μM for Dyrk1A ATP pocket, respectively.		DYRK
T1980	HA14-1		BCL
	HA14-1, a Bcl-2/Bcl-XL antagonist, is a non-peptidic ligand of a Bcl-2 surface pocket (IC50: ~9 μM).		BCL
T9079	Apostatin-1	Apt-1	Others
	Apostatin-1 (Apt-1) is a novel TRADD inhibitor. Apostatin-1 can bind to a pocket on the N-terminal TRAF2 binding domain of TRADD.		Others
T8700	TKIM		Potassium Channel
	TKIM is a TWIK-related potassium channel 1 (TREK-1) inhibitor, binding to the pocket of the intermediate (IM) state of TREK-1.		Potassium Channel
T3163	PS 48		PDK
	PS 48 has been shown to be a PKB Kinase (PDK1) activator (Kd: 10.3 μM). This compound selectively binds to the PIF-binding pocket of PKB Kinase (PDK1).		PDK
T8659	K-Ras-PDEδ-IN-1		PDE
	K-Ras-PDEδ-IN-1 is a potent inhibitor of competitive K-Ras-PDEδ.It binds to the farnesyl binding pocket of PDEδ(Kd of 8 nM).		PDE
T35694	OD36	OD 36,OD 36 hydrochloride,OD-36	ALK , RIP kinase
	OD36 is a selective and potent RIPK2 inhibitor with an IC50 of 5.3 nM.OD36 inhibits ALK2 signaling and osteogenic differentiation (KD: 37 nM), and binds efficiently to the ALK2 kinase ATP pocket.		ALK , RIP kinase
T9095	Necrostatin-34	2-{[3-cyano-4-(4-methylphenyl)-6-oxo-1,4	RIP kinase
	Necrostatin-34 (2-{[3-cyano-4-(4-methylphenyl)-6-oxo-1,4) is a RIPK1 kinase inhibitor, stabilizing RIPK1 kinase in an inactive conformation by occupying a distinct binding pocket in the kinase domain.		RIP kinase
T17205	UNC2541		Others , FLT , TAM Receptor
	UNC2541 is a potent and Mer tyrosine kinase (MerTK)-specific inhibitor. It also binds in the MerTK ATP pocket (IC50: 4.4 nM). UNC2541 inhibits phosphorylated MerTK (pMerTK; EC50, 510 nM).		Others , FLT , TAM Receptor
T10585	Bozitinib	CBT-101,PLB-1001	c-Met/HGFR
	Bozitinib (PLB-1001) (PLB-1001) is a highly selective inhibitor of the c-MET kinase with blood-brain barrier permeability. Bozitinib binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily.		c-Met/HGFR
T27133	DCLX069	DCLX 069,DCLX-069	Histone Methyltransferase
	DCLX069 is a potent and selective PRMT1 inhibitor. DCLX069 occupies the SAM binding pocket to exert the inhibitory effect. DCLX069 effectively blocks cell proliferation in breast cancer, liver cancer and acute myeloid le...		Histone Methyltransferase
T67753	Trifluoromethyl-tubercidin		Influenza Virus
	Trifluoromethyl-tubercidin (TFMT) inhibits host MTr1 and suppresses virus replication. TFMT inhibits MTr1 through interaction at its S-adenosyl-l-methionine binding pocket to restrict influenza virus replication. TFMT wa...		Influenza Virus
T14978	CL-82198		MMP
	CL-82198, a selective MMP-13 inhibitor, serves as a pharmacological intervention to halt the progression of osteoarthritis (OA). Its mechanism of action involves binding to the S1’ pocket of MMP-13, ensuring its selectiv...		MMP