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mv4-11-cell

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (2) AMPK (1) Apoptosis (19) Bcl-2 Family (2) Bcr-Abl (1) c-Myc (4) CDK (4) Checkpoint Kinase (Chk) (2) Epigenetic Reader Domain (14) ERK (3) Eukaryotic Initiation Factor (eIF) (1) FLT3 (13) Fluorescent Dye (1) GSK-3 (1) HDAC (7) Histone Acetyltransferase (2) Histone Demethylase (3) Histone Methyltransferase (1) IKZF Family (1) JAK (1) Microtubule/Tubulin (1) MNK (1) Molecular Glues (3) PAK (2) PARP (1) PI3K (1) Pim (1) PIN1 (1) PKC (1) Polo-like Kinase (PLK) (1) PROTACs (15) Proteasome (1) SHP2 (1) STAT (1) WDR5 (1) Wee1 (1)
By Research Areas:	Cancer (49)
Click Chemistry:	Azide (1)

Inhibitors & Agonists

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-120028

GNE-207	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC₅₀ of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC₅₀ of 18 nM for MYC expression in MV-4-11 cells .

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-176428

PROTAC MNK1 degrader-1 P11-2	PROTACs MNK Apoptosis Eukaryotic Initiation Factor (eIF)	Cancer
PROTAC MNK1 degrader-1 is a selective MNK1 PROTAC degrader with a DC₅₀ of 11.92 nM, and a D_max > 96% in MV4-11 cells. PROTAC MNK1 degrader-1 significantly reduces p-eIF4E (IC₅₀: 22.07 nM), induces apoptosis, and arrests the cell cycle at the G1 phase. PROTAC MNK1 degrader-1 has potent antitumor activity. PROTAC MNK1 degrader-1 has robust antileukemic efficacy in MV4-11 xenograft mice model with acceptable drug safety . Pink: MNK1 ligand (HY-176429); Blue: CRBN ligase ligand (HY-A0003); Black: linker (HY-Y1139); CRBN + linker: HY-176430

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-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-125236

ZEN-3694 BET-IN-19	Epigenetic Reader Domain	Cancer
ZEN-3694 (Compound 146) is a BET inhibitor. ZEN-3694 inhibits hlL-6 mRNA transcription (IC₅₀ ≤0.3 uM), and c-myc activity in human AML MV4-11 cell (IC₅₀ ≤0.3 uM). ZEN-3694 inhibits tetra-acetylated histone H4 binding to BRD4 bromodomain 1 (IC₅₀ ≤0.3 uM) .

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-155361

PROTAC BRD9 Degrader-7	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD9 Degrader-7 is an orally active, selective BRD9 PROTAC degrader (DC₅₀ = 1.02 nM). PROTAC BRD9 Degrader-7 mediates BRD9 degradation via the ubiquitin-proteasome system. PROTAC BRD9 Degrader-7 exhibits proliferation inhibitory activity in the MV4-11 cells. PROTAC BRD9 Degrader-7 can be used in the research of acute myeloid leukemia and other related malignancies. (Pink: BI 7271: HY-123616, Blue: 5-Aminothalidomide: HY-W023573, Blue + Black: Thalidomide-5-piperazine: HY-W834174, Black: N,N'-Dimethylpiperazine: HY-W539783) .

HY-155195

FLT3/CHK1-IN-1	FLT3	Cancer
FLT3/CHK-IN-1 (Compound 18) is a dual inhibitor of FLT3/CHK1. FLT3/CHK-IN-1 is more than 1700 times more selective to c-KI T and greatly reduces hERG affinity with an IC₅₀ value of 58.4 μM. FLT3/CHK-IN-1 inhibits tumor growth in mouse xenotransplantation models inoculated with MV-4-11 cells .

HY-143328

PROTAC BRD4 Degrader-17	PROTACs Epigenetic Reader Domain Apoptosis	Cancer
PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC₅₀ values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells .

HY-139901

Chk1-IN-6	Checkpoint Kinase (Chk)	Cancer
Chk1-IN-6 is a selective and orally active Chk1 inhibitor with an IC₅₀ of 16.1 nM. Chk1-IN-6 shows antiproliferative activity of MV-4-11 cells. Chk1-IN-6 exerts effective response in the MV-4-11 xenograft mouse model. Chk1-IN-6 exhibits synergistic anticancer effect with Gemcitabine (HY-17026). Chk1-IN-6 can be used in the research of cancers such as acute myeloid leukemia and colorectal adenocarcinoma .

HY-173631

(S)-dHTC1	PROTACs	Cancer
(S)-dHTC1 is a molecular glue degrader targeting the transcriptional co-activator ENL. (S)-dHTC1 binds the ligase with high affinity only after forming the ENL:dHTC1 complex with an IC₅₀ value of 93 nM. (S)-dHTC1 degrades ENL in MV4;11 cells with a DC₅₀ value of 26 nM. (S)-dHTC1 can be used for acute myeloid leukemia study .

HY-173422

MS2133	PROTACs Histone Methyltransferase	Cancer
MS2133 is a DOT1L PROTAC degrader. MS2133 promotes ubiquitination and degradation of DOT1L in THP-1 and MV4-11 cells (DC₅₀: 56 nM and 25 nM, respectively), and reduces H3K79 methylation. MS2133 inhibits the growth of MLL-r leukemia cells and has anticancer activity. (Pink: DOT1L ligand (HY-173423); Blue: E3 ligase VHL ligand (HY-47070); Black: Linker (HY-79577); E3 ligase VHL ligand-linker conjugate (HY-173424)) .

HY-171334

(Rac)-P1D-34	PROTACs PIN1	Cancer
PROTAC PIN1 degrader-2 (1) is a PROTAC-based PIN1 degrader (Pink: PIN1 ligand HY-171442, Blue: cereblon ligand Thalidomide (HY-14658), Black: linker HY-W014883). PROTAC PIN1 degrader-2 (1) possesses anti-cancer activity, with IC₅₀ values of 2248 nM (MV-4-11 cells), 3984 nM (MOLM-13), 3925 nM (HL-60), 3925 nM (HL-60), 3925 nM (HL-60), 3925 nM (HL-60) and 3925 nM (HL-60) respectively .

HY-157213

LWY713	Apoptosis PROTACs FLT3	Cancer
LWY713 is a PROTAC-class FLT3 degrader (DC₅₀=0.64 nM), which selectively induces FLT3 degradation via cereblon and proteasome-dependent pathways. LWY713 inhibits cell proliferation and induces G0/G1 phase arrest and apoptosis in MV4-11 cells. LWY713 shows effective in vivo antitumor activity in MV4-11 xenograft models . LWY713 consists of a target protein ligand (red part) Gilteritinib (HY-12432), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC linker (black part) Glycolic acid (HY-W015967). E3 ubiquitin ligase and linker can form Lenalidomide-Glycolic acid (HY-169373); the active control for the target protein ligand is Naproxen Gilteritinib (HY-169374).

HY-178858

PROTAC FLT3/CHK1 Degrader-1	PROTACs FLT3 Checkpoint Kinase (Chk) STAT ERK c-Myc Akt	Cancer
PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC₅₀ values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces apoptosis in MV-4-11 cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/CHK1 ligand (HY-178869 ), Blue: CRBN Ligand (HY-W093272), Black: Linker, E3 ligase ligand-linker conjugate (HY-W998238)) .

HY-161883

JP-2-249	Molecular Glues Epigenetic Reader Domain	Cancer
JP-2-249 is a molecular glue that acts as a potent degrader of SMARCA2. JP-2-249 shows decreasing protein level of SMARCA2 in MV-4-11 cells at 1-10 μM .

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-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-179272

Wee1/HDAC-IN-1	Wee1 HDAC Apoptosis	Cancer
Wee1/HDAC-IN-1 is a dual Wee1/HDAC inhibitor with an IC₅₀ of 1.2 nM for Wee1 and IC₅₀ values of 196 nM for HDAC1, 156 nM for HDAC3, and 55 nM for HDAC6. Wee1/HDAC-IN-1 exhibits strong antiproliferative activity against MV4-11 cells with an IC₅₀ of 0.076 μM. Wee1/HDAC-IN-1 selectively binds to Wee1 and HDACs. Wee1/HDAC-IN-1 interferes with DNA damage repair pathways and induces apoptosis in MV4-11 cells. Wee1/HDAC-IN-1 Wee1/HDAC-IN-1 can be used for the research of acute myeloid leukemia (AML) .

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-143327

PROTAC BRD4 Degrader-16	PROTACs Epigenetic Reader Domain Apoptosis	Cancer
PROTAC BRD4 Degrader-16 is a potent PROTAC BRD4 Degrader, with IC₅₀ values of 34.58 nM (BRD4 (BD1)) and 40.23 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-16 ignificantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-16 significantly induces apoptosis in MV-4-11 cells .

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-170380

XY221	Epigenetic Reader Domain Apoptosis AMPK c-Myc PAK Bcl-2 Family	Cancer
XY221 (Compound 16o) selectively inhibits BRD4 BD2, with an IC₅₀ of 5.8 nM. XY221 demonstrates high pan-BD2 selectivity (667-fold over BRD4 BD1) and BRD4 BD2 domain selectivity (9−32-fold over BRD2/3/T BD2). XY221 induce Apoptosis in MV4-11 cells and shows anticancer activity .

HY-175610

PROTAC FLT3/JAK2/BRD4 Degrader-1	PROTACs FLT3 JAK Epigenetic Reader Domain	Cancer
PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC₅₀ values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC₅₀ = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939)) .

HY-174302

PIM-1/HDAC-IN-2	Pim HDAC PARP Apoptosis	Cancer
PIM-1/HDAC-IN-2 is a robust PIM/HDAC inhibitor (IC₅₀ = 0.11 μM in MV4-11cells), which exerts a synergistic antiproliferative effect through a dual mechanism of inhibiting PIM1 kinase and selectively inhibiting HDAC6. PIM-1/HDAC-IN-2 induces cell apoptosis. PIM-1/HDAC-IN-2 remarkably induces the cleavage of PARP, thereby initiating the arrest of the cell cycle in G1 phase and a reduction in S phase. PIM-1/HDAC-IN-2 demonstrates significant anticancer efficacyin the MV4-11 xenograft model without notable toxicity^[1]_.

HY-177766

GSPT1 degrader-17	Molecular Glues Apoptosis	Cancer
GSPT1 degrader-17 (Compound 9q) is a potent and selective cereblon-based molecular glue degrader that targets G1 to S phase transition 1 (GSPT1). GSPT1 degrader-17 degrades GSPT1 in U937 cells with a DC₅₀ of 35 nM and Dmax of 81.65%. GSPT1 degrader-17 has a strong inhibitory effect on U937, MOLT-4 and MV4-11 cells with IC₅₀ values of 0.019, 0.006 and 0.027 μM. GSPT1 degrader-17 can induce cells apoptosis and G0/G1 phase arrest. GSPT1 degrader-17 can be used for the research of cancer, such as acute myeloid leukemia .

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-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-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-144369

Proteasome-IN-4	Proteasome	Cancer
Proteasome-IN-4 is an excellent and non-covalent proteasome inhibitor (IC₅₀=8.39 nM). Proteasome-IN-4 has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines. Proteasome-IN-4 can be used for cancer research .

HY-178020

FLT3-IN-34	FLT3 ERK Akt Apoptosis	Cancer
FLT3-IN-34 is a FLT3 inhibitor, with an IC₅₀ value of 1.4 nM. FLT3-IN-34 blocks the phosphorylation of FLT3 and its downstream signaling molecules AKT and ERK1/2. FLT3-IN-34 induces concentration-dependent G0/G1 phase arrest and mild apoptosis in FLT3-ITD-positive MV4-11 cells. FLT3-IN-34 shows potent anti-proliferative activity against FLT3-ITD-positive MV4-11 cells (IC₅₀ = 14.95 nM) and MOLM-13 (IC₅₀ = 18.5 nM). FLT3-IN-34 can be used for the study of FLT3-positive acute myeloid leukemia (AML) .

HY-169389

OICR41114	PROTACs WDR5	Cancer
OICR41114 is a WDR5 PROTAC degrader with an EC₅₀ of 40 nM. OICR41114 binds both DCAF1 and WDR5, and its binding affinity for DCAF1 is significantly enhanced in the presence of WDR5 (K_D increases from 59 nM to 5 nM). OICR41114 exerts antiproliferative effects on MV4-11 cells. OICR41114 can be used for the research of acute myeloid leukemia .

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-146660

BRD4 Inhibitor-18	c-Myc Epigenetic Reader Domain Apoptosis	Cancer
BRD4 Inhibitor-18 is a highly potent BRD4 inhibitor with an IC₅₀ value of 110 nM. BRD4 Inhibitor-18 has a hydrophobic acetylcyclopentanyl side chain. BRD4 Inhibitor-18 can significantly suppress the proliferation of MV-4-11 cells with high BRD4 level. BRD4 Inhibitor-18 has apoptosis-promoting and G0/G1 cycle-arresting activity .

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). (Structure Note: Pink, CBP/p300 ligand 5 (HY-161711); Blue, E3 ligase ligand (HY-41547); Black, Linker (HY-40178)) .

HY-174437A

FLT3-IN-32 TFA	FLT3	Cancer
FLT3-IN-32 TFA is a potent FLT3 inhibitor with an IC₅₀s of 2.40 nM and 3.83 nM against FLT3-ITD and FLT3-D835Y. FLT3-IN-32 TFA inhibits proliferation/survival of human MV4-11 cells with an IC₅₀ of 0.07 nM. FLT3-IN-32 TFA can be used for the study of acute myeloid leukemia (AML) .

HY-169075

CDK/HDAC-IN-4	HDAC CDK Apoptosis	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-169076

FLT3/HDAC-IN-1	FLT3 HDAC Apoptosis	Cancer
FLT3/HDAC-IN-1 is a dual inhibitor of FLT3/HDAC, with IC₅₀ values of 30.4, 52.4, and 14.7 nM for FLT3, HDAC1, and HDAC3, respectively. FLT3/HDAC-IN-1 can induce apoptosis in MV-4-11 cells and has anti-proliferative effects on FLT3 mutant-transformed BaF3 cells. FLT3/HDAC-IN-1 is being researched for its potential in treating hard-to-treat solid tumors and hematological malignancies .

HY-155112

Antiproliferative agent-30	Microtubule/Tubulin FLT3 Bcr-Abl	Cancer
Antiproliferative agent-30 (Compound 8g) inhibits tubulin assembly and inhibits FLT3 and Abl1. Antiproliferative agent-30 has vascular-disrupting activity. Antiproliferative agent-30 has broad antiproliferative activities against cancer cell lines (IC₅₀s: 0.054 nM, 0.008 nM, 0.144 nM for HCT-116, K562, MV-4-11 cells respectively). Antiproliferative agent-30 also has anticancer effect against AML with FLT3-ITD-TKD mutation .

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-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-170403

LSD1-IN-38	Histone Demethylase	Cancer
LSD1-IN-38 (Compound 23e) is a reversible, orally active inhibitor for lysine specific demethylase 1 (LSD1) with an IC₅₀ of 1.2 nM. LSD1-IN-38 inhibits the proliferation of cancer cells MV4-11, Kasumi-1 and NCI-H526, with IC₅₀ of 5, 4 and 11 nM, respectively. LSD1-IN-38 activates CD86 expression with an EC₅₀ of 0.034 μM, and induces differentiation in MV4−11 cell. LSD1-IN-38 exhibits antitumor efficacy in mouse models .

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-173123

LSD1-IN-40	Histone Demethylase Apoptosis	Cancer
LSD1-IN-40 (Compound 9e) is a potent LSD1 inhibitor, with an IC₅₀ of 9.85 nM. LSD1-IN-40 exhibits exceptional selectivity for LSD1 over both MAOs and hERG. LSD1-IN-40 exhibits significant inhibitory activity against leukemia cells (MV-4-11, HL-60, and THP-1 cells). LSD1-IN-40 can induce apoptosis in MV-4-11 cells. LSD1-IN-40 has the potential for the research of acute myeloid leukemia .

HY-174322

SHP2-IN-38	SHP2 ERK Fluorescent Dye	Cancer
SHP2-IN-38 is a novel green-fluorescent SHP2 inhibitor with IC₅₀ values of 2.89 μM (SHP2), 8.73 μM (SHP1), 11.08 μM (PTP1B), 33.07 μM (TCPTP). SHP2-IN-38 blocks the SHP2-mediated ERK signaling pathway and inhibits MV4-11 cells proliferation in vitro with IC₅₀ of 7.90 μM. SHP2-IN-38 has an excitation wavelength of 360 nm, with a maximum emission wavelength of 550 nm in DMSO and 540 nm in DMF. SHP2-IN-38 shows green fluorescence imaging in HeLa cells and zebrafish.

HY-180836

DIX-01	Molecular Glues IKZF Family Apoptosis	Cancer
DIX-01 is a molecular gel degrader that can simultaneously induce the degradation of IKZF1/3 and GSPT1 mediated by CRBN. Its DC₅₀ values are: IKZF1 (19.80 nM), IKZF3 (45.31 nM), and GSPT1 (120.1 nM). DIX-01 exhibits nanomolar-level potent anti-proliferative activity in various cancer cell lines. DIX-01 induces apoptosis in MV4-11 cells and significantly inhibits the growth of leukemia cells in zebrafish. DIX-01 can be used for the study of malignant hematological tumors .

HY-179734

PROTAC BRD4 Degrader-41	PROTACs Epigenetic Reader Domain Apoptosis c-Myc	Cancer
PROTAC BRD4 Degrader-41 (Compound A5) is a BRD4 PROTAC degrader with a DC₅₀ of 0.97 nM. PROTAC BRD4 Degrader-41 exhibits potent anti-proliferative activity against various types of cancer cells such as AML, lymphoma, breast cancer, ovarian cancer, and non-small cell lung cancer. PROTAC BRD4 Degrader-41 can induce G0/G1 phase arrest and apoptosis in MV4-11 cells. PROTAC BRD4 Degrader-41 downregulates the transcriptional level of c-Myc .

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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