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MV4

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Anaplastic lymphoma kinase (ALK) (1) Apoptosis (17) Autophagy (1) Bcl-2 Family (3) Bcr-Abl (1) c-Fms (1) c-Myc (1) CDK (11) EGFR (1) Epigenetic Reader Domain (15) FLT3 (17) GABA Receptor (1) GSK-3 (1) HDAC (6) Histone Acetyltransferase (2) Histone Demethylase (3) IKK (1) Ligands for Target Protein for PROTAC (3) Microtubule/Tubulin (1) MNK (1) Molecular Glues (1) PAK (1) Phosphatase (1) PI3K (2) Pim (1) PKC (1) Polo-like Kinase (PLK) (1) PROTACs (9) Proteasome (1) RET (1) SHP2 (1) TAM Receptor (1)
By Research Areas:	Cancer (63) Inflammation/Immunology (3) Metabolic Disease (1) Neurological Disease (1)
Click Chemistry:	Azide (1)

Inhibitors & Agonists

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13907

TCS 359 1 Publications Verification	FLT3	Cancer
TCS 359, a 2-acylaminothiophene-3-carboxamide, is a potent and selective FLT3 inhibitor with an IC₅₀ of 42 nM. TCS 359 inhibits MV4-11 cell proliferation with an IC₅₀ of 340 nM .

HY-157213

LWY713	FLT3 Apoptosis	Cancer
LWY713 is a FLT3 degrader (DC₅₀=0.64 nM) that selectively induces FLT3 degradation in a cereblon- and proteasome-dependent manner. LWY713 inhibits cell proliferation and induces G0/G1 arrest and apoptosis in MV4-11 cells. LWY713 exhibits potent in vivo antitumor activity in an MV4-11 xenograft model .

HY-149474

HDAC-IN-63	FLT3 HDAC Apoptosis	Cancer
HDAC-IN-63 (Compound 63) is a dual FLT3/HDAC inhibitor (IC₅₀: 0.844 and 30.0 nM for FLT3 and HDAC1 respectively). HDAC-IN-63 inhibits MV4-11 cell proliferation (IC₅₀: 92 nM. HDAC-IN-63 induces apoptosis and arrests cell cycle in MV4-11 cells. HDAC-IN-63 can be used for research of acute myeloid leukemia (AML) .

HY-147572

BET-IN-10	Epigenetic Reader Domain	Cancer
BET-IN-10 is a BET inhibitor with anticancer effects. BET-IN-10 inhibits the cell growth of MV4-11 cells with an IC₅₀ of 26.5 nM (WO2022012456A1; example 6) .

HY-163834

HDAC6-IN-47	HDAC	Cancer
HDAC6-IN-47 (Compound S-29b) is inhibitor for HDAC, which exhibits high affinities to HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, HDAC10 with K_i of 60, 56, 162, 0.44, 362 and 849 nM, respectively. HDAC6-IN-47 causes tubulin hyperacetylation in MV4-11, inhibits the proliferation of MV4-11 with an EC₅₀ of 0.50 µM. HDAC6-IN-47 can be used in research of leukemia .

HY-161280

PROTAC FLT-3 degrader 3	PROTACs FLT3	Cancer
PROTAC FLT-3 degrader 3 (compound 35) is a PROTACs degrader of FLT. PROTAC FLT-3 degrader 3 has antiproliferative activity, with IC₅₀ of 7.55 nM in MV4-11 cells .

HY-157295

PI3K/HDAC-IN-3	PI3K HDAC	Cancer
PI3K/HDAC-IN-3 (36) is a PI3K and HDAC dual inhibitor, with IC₅₀ values of 0.23 nM and 172 nM for PI3Kα and HDAC1, respectively. PI3K/HDAC-IN-3 (36) suppresses AKT phosphorylation and increased H3 acetylation in MV4-11 cells. PI3K/HDAC-IN-3 (36) exhibits significant and dose-dependent anticancer efficacy in a MV4-11 xenograft model .

HY-146741

SDR-04	Epigenetic Reader Domain	Cancer
SDR-04 is a BET inhibitor and exhibits strong BRD4-BD1 affinity and inhibition activity. SDR-04 potently suppresses MV4;11 cancer cell line proliferation .

HY-144755

MC2652	Histone Demethylase	Cancer
MC2652 (compound 1a) is a potent LSD1 inhibitor. MC2652 displays high inhibiting effects in MV4-11 and NB4 leukaemia cells. MC2652 shows antiproliferative activity against prostate cancer LNCaP cells .

HY-X0009A

JSH-009 dimaleate	CDK	Cancer
JSH-009 dimaleate (Compound 1) is a potent and highly selective CDK9 inhibitor with an IC₅₀ of 0.928 nM. JSH-009 can effectively inhibit the growth of subcutaneous tumor (cute myelogenous leukemia MV4-11) mice .

HY-143889

Senexin C	CDK	Cancer
Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability .

HY-159454

PROTAC SMARCA2/4-degrader-3	PROTACs	Cancer
SMARCA2/4-degrader-3 (compound I-433) is a PROTAC *SMARCA2/4*-degrader based on VH032-NH2, with a degradation potency (DC₅₀) <100 nM in MV4-11 cells .

HY-115881

SR-1114	PROTACs	Cancer
SR-1114 is a first-in-class PROTAC ENL degrader. SR-1114 elicits rapid, CRBN-dependent degradation of ENL with DC₅₀s of 150 nM, 311 nM, and 1.65 μM in MV4;11 , MOLM-13, and OCI/AML-2 cells, respectively .

HY-143585

CDK9-IN-14	CDK	Cancer
CDK9-IN-14 is a potent and selective CDK9 inhibitor with IC₅₀ of 6.92 nM. CDK9-IN-14 has a relatively strong inhibitory effect on MV4;11 cells and in vivo tumor models, and has a good selectivity and a low toxicity and few side effects .

HY-143238

FY-56	Histone Demethylase	Cancer
FY-56 is a highly potent and selective LSD1/KDM1A inhibitor (IC₅₀=42 nM) and exhibits high selectivity over MAO-A/B. FY-56 induces differentiation of MOLM-13 and MV4-11 cell and has the potential for AML research .

HY-162293

CDK8-IN-14	CDK	Cancer
CDK8-IN-14 (compound 12) inhibits CDK8 with an IC₅₀ value of 39.2 nM and has anti-AML cell proliferation activity (molm-13 GC50 = 0.02±0.01μM, MV4-11 GC50 = 0.03±0.01μM) .

HY-162651

PROTAC BRD9 Degrader-8	PROTACs	Inflammation/Immunology
PROTAC BRD9 Degrader-8 (compound E5) is a PROTAC-based BRD9 degrader with a DC₅₀ value of 16 pM. PROTAC BRD9 Degrader-8 has antiproliferation in MV4–11 cells (IC₅₀ = 0.27 nM) and OCI-LY10 cells (IC₅₀ = 1.04 nM) .

HY-122623A

DB818 dihydrochloride	Apoptosis	Cancer
DB818 dihydrochloride is the dihydrochloride salt form of DB818 (HY-122623). DB818 dihydrochloride is an inhibitor for Homeobox A9 (HOXA9). DB818 dihydrochloride reduces the formation of HOXA9-DNA complexes, inhibits the growth and induces apoptosis in AML cell lines OCI/AML3, MV4-11, and THP-1 .

HY-12461

WS6	PI3K EGFR GABA Receptor FLT3 IKK	Neurological Disease Metabolic Disease Inflammation/Immunology
WS6 is an IkB kinase and EBP1 inhibitor, with IC₅₀ values of 0.24 nM, 0.21 nM, and 40.48 nM in MV4-11, MOLM13, and K562 cells, respectively. WS6 promotes the proliferation of alpha and beta cells in the pancreas, has antioxidant and anti-inflammatory activities, and can alleviate depression like behavior in rats ^[1][2][4].

HY-143490

PAK4-IN-2	PAK Apoptosis	Cancer
PAK4-IN-2 is a highly potent *PAK4* inhibitor with IC₅₀ value of 2.7 nM. PAK4-IN-2 can arrest MV4-11 cells at G0/G1 phase and induce cell apoptosis. PAK4-IN-2 can be used for researching cancer .

HY-153751

BRD4-IN-4	Epigenetic Reader Domain	Cancer
BRD4-IN-4 (Compound 1) is a *BRD4* inhibitor (IC₅₀=6.83 μM). BRD4-IN-4 selectively inhibits MV4-11 cell line proliferation and arrests cell at G1 phase. BRD4-IN-4 can be used for research of MLL leukemia .

HY-149595

LSD1-UM-109	Histone Demethylase	Cancer
LSD1-UM-109 is a ighly potent and reversible LSD1 inhibitor with an IC₅₀ of 3.1 nM. LSD1-UM-109 inhibits cell growth with IC₅₀ values of 0.6 nM in the MV4;11 acute leukemia cell line and 1.1 nM in the H1417 small-cell lung cancer cell line .

HY-125236

BET-IN-19	Epigenetic Reader Domain	Cancer
BET-IN-19 (Compound 146) is a BET inhibitor. BET-IN-19 inhibits hlL-6 mRNA transcription (IC₅₀ ≤ 0.3 uM), and c-myc activity in human AML MV4-11 cell (IC₅₀ ≤ 0.3 uM)。BET-IN-19 inhibits tetra-acetylated histone H4 binding to BRD4 bromodomain 1 (IC₅₀ ≤ 0.3 uM) .

HY-155489

DDO-2728	Anaplastic lymphoma kinase (ALK) Apoptosis	Cancer
DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC₅₀ of 2.97 μM. DDO-2728 increases the abundance of N ⁶ methyladenosine (m ⁶A) modifications, inducing cell apoptosis and cycle arrest. DDO-2728 suppresses tumor growth in the MV4−11 xenograft model with favorable safety profile, shows the potential of targeting ALKBH5 in cancer research .

HY-157516

CDK2-IN-22	CDK	Cancer
CDK2-IN-22 (compound 7I) is a potent CDK2 inhibitor with an IC₅₀ of 64.42 nM. CDK2-IN-22 presents a broad antiproliferative efficacy toward diverse cancer cells MV4-11, HT-29, MCF-7, and HeLa with IC₅₀ values of 0.83 μM, 2.12 μM, 3.12 μM, and 8.61 μM, respectively .

HY-151595

Menin-MLL inhibitor-22	Epigenetic Reader Domain	Cancer
Menin-MLL inhibitor-22 (compound C20) is an orally active inhibitor of the interaction between menin and mixed lineage leukemia (MLL) (IC₅₀=7 nM). Menin-MLL inhibitor-22 binds menin protein and inhibits cancer cell growth (MV4 cells, IC₅₀=0.3 μM). Menin is a putative tumor suppressor associated with multiple endocrine neoplasia type 1 (MEN-1 syndrome) .

HY-13001

Quizartinib 25+ Cited Publications AC220; AC708	FLT3 Ligands for Target Protein for PROTAC Apoptosis	Cancer
Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a K_d of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC₅₀s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .

HY-144777

FLT3-IN-14	FLT3 Apoptosis	Cancer
FLT3-IN-14 is a potent FLT3 inhibitor with IC₅₀s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model .

HY-150562

CDK9-IN-19	CDK	Cancer
CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC₅₀ value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML) .

HY-155245

A09-003	CDK Bcl-2 Family	Cancer
A09-003 is a CDK-9 inhibitor (IC₅₀: 16 nM). A09-003 inhibits leukemia cell proliferation (IC₅₀: 1.90, 0.86, 2.49, 1.84, 0.48 μM for BDCM, Molm-14, THP-1, U937, MV4-11 cells). A09-003 induces apoptosis and decreases Mcl-1 expression through Thr163 dephosphorylation .

HY-158031

PLK1/BRD4-IN-5	Apoptosis Polo-like Kinase (PLK) Epigenetic Reader Domain	Cancer
PLK1/BRD4-IN-5 (Compound SC10) is an orally active PLK1 and *BRD4* inhibitor with IC₅₀ values of 0.3  nM and 60.8  nM, respectively. PLK1/BRD4-IN-5 can induce MV4-11 cell block in S phase and apoptosis) in a dose-dependent manner. PLK1/BRD4-IN-5 can be used in cancer research .

HY-161710

XYD129	PROTACs Epigenetic Reader Domain Histone Acetyltransferase	Cancer
XYD129 is an effective CBP/p300 PROTAC degrader. XYD129 has antiproliferative activity on MV4-11 cell line (IC ₅₀=0.044 μM). XYD129 can be used for the study of acute myeloid leukemia (AML). (Srtucture Note: Pink, CBP/p300 ligand 5 (HY-161711); Blue, E3 ligase ligand (HY-41547); Black, Linker (HY-40178)) .

HY-162769

HDAC3-IN-5	HDAC Apoptosis	Cancer
HDAC3-IN-5 (9c) is a HDAC3 selective inhibitor, with IC₅₀ values of 4.2 nM, 1629 nM and 298.2 nM for HDAC3, HDAC2, HDAC1, respectively. HDAC3-IN-5 (9c) can effectively induce apoptosisin MV4-11 cells in vitro and reduce the expression of anti-apoptotic proteins, the development of HDAC3 selective inhibitors may serve as a potential lead compound to reverse Venetoclax resistance .

HY-147716

CDK8-IN-6	CDK	Cancer
CDK8-IN-6 (compound 9) is a potent cyclin-dependent kinase 8 (CDK8) inhibitor with an K_d of 13 nM. CDK8-IN-6 shows cytotoxicity for MOLM-13, OCI-AML3, MV4-11, NRK and H9c2 cells with IC₅₀s of 11.2, 7.5, 8.6, 20.5, 12.5-25 µM, respectively. CDK8-IN-6 has the potential for the research of AML-cancer .

HY-148561

CDK8-IN-12	CDK GSK-3 PKC	Cancer
CDK8-IN-12 is an orally active, potent CDK8 inhibitor with a K_i of 14 nM. CDK8-IN-12 has off-target kinase inhibition on GSK-3α, GSK-3β, PCK-θ with K_is of 13 nM, 4 nM, 109 nM, respectively. CDK8-IN-12 shows potent anti-proliferative effects selectively on MV4-11 cell. CDK8-IN-12 is an anti-cancer agent .

HY-162642

Bfl-1-IN-3	Bcl-2 Family	Cancer
Bfl-1-IN-3 (Compound 56) is a selective, competitive inhibitor for Bfl-1 on BID binding site with K_i of 105 nM. Bfl-1-IN-3 inhibits the proliferation of cell pfeiffer and MV4-11, with IC₅₀ of 6.92 μM and 12.6 μM. Bfl-1-IN-3 induces apoptosis in pfeiffer cells. Bfl-1-IN-3 overcomes Venetoclax (HY-15531) resistance at the cellular level, and shows synergistically enhanced anti-tumor activity with Venetoclax .

HY-147717

CDK8-IN-7	CDK	Cancer
CDK8-IN-7 (compound 12) is a potent and selective cyclin-dependent kinase 8 (CDK8) inhibitor with an K_d of 3.5 nM. CDK8-IN-7 shows cytotoxicity for MOLM-13, OCI-AML3, MV4-11, NRK and H9c2 cells with IC₅₀s of 5.9, 4.8, 5.4, 16.2, 12.5-25 µM, respectively. CDK8-IN-7 has the potential for the research of AML-cancer .

HY-13001R

Quizartinib (Standard)	FLT3 Ligands for Target Protein for PROTAC Apoptosis Autophagy	Cancer
Quizartinib (Standard) is the analytical standard of Quizartinib. This product is intended for research and analytical applications. Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a K_d of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC₅₀s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .

HY-143895

FLT3-IN-12	FLT3	Cancer
FLT3-IN-12 is a potent, selective and orally active FLT3 kinase inhibitor with IC₅₀s of 1.48 nM and 2.87 nM for FLT3-WT and FLT3-D835Y, respectively. FLT3-IN-12 possesses high selectivity over c-KIT (>1000-fold). FLT3-IN-12 has an excellent anti-AML (acute myeloid leukemia) activity (MV4-11, IC₅₀ of 0.75 nM) .

HY-149539

PLM-101	FLT3 RET	Cancer
PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po) .

HY-14217

Quizartinib dihydrochloride 25+ Cited Publications AC220 dihydrochloride	FLT3 Apoptosis Ligands for Target Protein for PROTAC	Cancer
Quizartinib dihydrochloride (AC220 dihydrochloride) is the dihydrochloride salt form of Quizartinib (HY-13001). Quizartinib dihydrochloride is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a K_d of 1.6 nM. Quizartinib dihydrochloride inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC₅₀s of 4.2 and 1.1 nM, respectively. Quizartinib dihydrochloride can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib dihydrochloride induces apoptosis .

HY-100388

SHP099 Maximum Cited Publications 57 Publications Verification	SHP2 Phosphatase	Cancer
SHP099 is an allosteric SHP2 inhibitor, with IC₅₀s of 0.690, 1.241, 0.416, 1.968, 2.896 μM for SHP2, SHP2 ^D61Y, SHP2E69K, SHP2 ^A72V, SHP2 ^E76K. SHP099 inhibits cancer cell growth, such as MV4-11 and TF-1 cell (IC₅₀: 0.32 and 1.73 μM). SHP099 inhibits RAS-ERK signaling and inhibits tumor growth .

HY-143894

FLT3-IN-11	FLT3	Cancer
FLT3-IN-11 (compound 30) is a potent, selective and orally active FLT3 kinase inhibitor with IC₅₀s of 7.22 nM and 4.95 nM for wild-type FLT3 and FLT3-D835Y, respectively. FLT3-IN-11 high selectivity for FLT3 over c-KIT (>1000-fold). FLT3-IN-11has excellent anti-acute myeloid leukemia (AML) activity (MV4-11 cells, IC₅₀ of 3.2 nM) .

HY-155302

FLT3-IN-22	FLT3	Cancer
FLT3-IN-22 (compound 22f) is a potent FLT3 inhibitor with IC₅₀ values of 0.941 nM and 0.199 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-22 exhibits strong antiproliferative activity against MV4-11 cells and the mutant FLT kinase expressed Ba/F3 cell lines, including FLT-D835Y and FLT3-F691L .

HY-169093

MS41	PROTACs Epigenetic Reader Domain	Cancer
MS41 is a selective eleven-nineteen leukemia (ENL) PROTAC degrader, with DC₅₀s of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1), respectively. MS41 effectively inhibits the growth of ENL-dependent leukemia cells, induces G1 cell cycle arrest and increases apoptosis. MS41 reduces the chromatin occupancy of ENL-associated transcription elongation machinery, and suppresses oncogenic gene expression and leukemia progression. Red: ENL ligand (HY-169094). Black: linker (HY-W105744). Blue: VHL ligand (HY-112078) .

HY-155770

FLT3-IN-20	FLT3	Cancer
FLT3-IN-20 (compound 34f) is a potent FLT3 inhibitor with IC₅₀ values of 1 and 4 nM for FLT3-D835Y and FLT3-ITD, respectively. FLT3-IN-20 has anti-proliferation efficacy in FLT3-ITD-positive AML cell lines MV4-11 and MOLM-13 (7 and 9 nM, respectively) and the MOLM-13 variant (4 nM) with the FLT3-ITD-D835Y mutation. FLT3-IN-20 can be used in research of cancer .

HY-156016

HDAC/CD13-IN-1	HDAC	Cancer
HDAC/CD13-IN-1 (Compound 12) is a HDAC/CD13 inhibitor (IC₅₀: 0.34 μM for hCD13, 0.53 μM for porcine CD13, 0.03, 0.06, 0.02 μM for HDAC1/2/3). HDAC/CD13-IN-1 inhibits MV4-11, K562, Jeko-1, and HL60 cell proliferation (IC₅₀: 0.25-2.04 μM). HDAC/CD13-IN-1 induces cancer cell apoptosis. HDAC/CD13-IN-1 has anti-metastasis and anti-invasion efficacy .

HY-169075

CDK/HDAC-IN-4	HDAC CDK	Cancer
CDK/HDAC-IN-4 is a high selective dual cyclin-dependent kinase (CDK)/histone deacetylase (HDAC) inhibitor with IC₅₀ values of 88.4 and 168.9 nM, respectively. CDK/HDAC-IN-4 exhibits antiproliferative capacities against hematological and solid tumor cells. CDK/HDAC-IN-4 also induces MV-4-11 cell Apoptosis and S cell cycle arrests. CDK/HDAC-IN-4 possesses a significant antitumor potency in the MV-4-11 xenograft model .

HY-116588

FT001	Epigenetic Reader Domain	Cancer
FT001 is an orally active and selective BET inhibitor. FT001 has potent anti-proliferative effects against MV-4-11. FT001 can be used for research of cancer .

HY-146615

Axl-IN-6	TAM Receptor	Cancer
Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model .

Cat. No.	Product Name		Classification

HY-159454

PROTAC SMARCA2/4-degrader-3		Azide
SMARCA2/4-degrader-3 (compound I-433) is a PROTAC *SMARCA2/4*-degrader based on VH032-NH2, with a degradation potency (DC₅₀) <100 nM in MV4-11 cells .

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